Helena Danielson

Monitoring drug–target interactions through target engagement-mediated amplification on arrays and in situ

Al-Amin, Rasel A.; Johansson, Lars; Abdurakhmanov, Eldar; Landegren, Nils et al.

Part of Nucleic Acids Research, 2022

• DOI for Monitoring drug–target interactions through target engagement-mediated amplification on arrays and in situ
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Ultralarge Virtual Screening Identifies SARS-CoV-2 Main Protease Inhibitors with Broad-Spectrum Activity against Coronaviruses

Luttens, Andreas; Gullberg, Hjalmar; Abdurakhmanov, Eldar; Vo, Duy Duc et al.

Part of Journal of the American Chemical Society, p. 2905-2920, 2022

• DOI for Ultralarge Virtual Screening Identifies SARS-CoV-2 Main Protease Inhibitors with Broad-Spectrum Activity against Coronaviruses
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Discovery of an allosteric ligand binding site in SMYD3 lysine methyltransferase

Talibov, Vladimir O; Fabini, Edoardo; FitzGerald, Edward; Tedesco, Daniele et al.

Part of ChemBioChem, p. 1597-1608, 2021

• DOI for Discovery of an allosteric ligand binding site in SMYD3 lysine methyltransferase
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Discovery of fragments inducing conformational effects in dynamic proteins using a second-harmonic generation biosensor

FitzGerald, Edward A.; Butko, Margaret T.; Boronat, Pierre; Cederfelt, Daniela et al.

Part of RSC Advances, p. 7527-7537, 2021

• DOI for Discovery of fragments inducing conformational effects in dynamic proteins using a second-harmonic generation biosensor
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Unveiling the Biochemistry of the Epigenetic Regulator SMYD3

Fabini, Edoardo; Talibov, Vladimir O; Mihalic, Filip; Naldi, Marina et al.

Part of Biochemistry, p. 3634-3645, 2019

• DOI for Unveiling the Biochemistry of the Epigenetic Regulator SMYD3

Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design

Linkuviene, Vaida; Talibov, Vladimir O; Danielson, U. Helena; Matulis, Daumantas

Part of Journal of Medicinal Chemistry, p. 2292-2302, 2018

• DOI for Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design

Biophysics in drug discovery: impact, challenges and opportunities

Renaud, Jean-Paul; Chung, Chun-wa; Danielson, U. Helena; Egner, Ursula et al.

Part of Nature reviews. Drug discovery, p. 679-698, 2016

• DOI for Biophysics in drug discovery: impact, challenges and opportunities

Regulatory effects of RNA-protein interactions revealed by reporter assays of bacteria grown on solid media

Pérez-Ropero, Guillermo; Dolcemascolo, Roswitha; Pérez-Ràfols, Anna; Andersson, Karl et al.

Part of Biosensors, 2025

• DOI for Regulatory effects of RNA-protein interactions revealed by reporter assays of bacteria grown on solid media
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Integrated computational and biosensor-based strategies for the discovery of allosteric SMYD3 ligands using diperodon as a starting point

FitzGerald, Edward; Rachman, Moira; Cederfelt, Daniela; Myers, Nadine et al.

Part of Bioorganic & Medicinal Chemistry, 2025

• DOI for Integrated computational and biosensor-based strategies for the discovery of allosteric SMYD3 ligands using diperodon as a starting point
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Unraveling the Bivalent and Rapid Interactions Between a Multivalent RNA Recognition Motif and RNA: A Kinetic Approach

Pérez-Ropero, Guillermo; Perez-Rafols, Anna; Martelli, Tommasso; Danielson, U. Helena et al.

Part of Biochemistry, p. 2816-2829, 2024

• DOI for Unraveling the Bivalent and Rapid Interactions Between a Multivalent RNA Recognition Motif and RNA: A Kinetic Approach
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Multiplexed experimental strategies for fragment library screening against challenging drug targets using SPR biosensors

FitzGerald, Edward; Vagrys, Darius; Opassi, Giulia; Klein, Hanna F. et al.

Part of SLAS Discovery, p. 40-51, 2024

• DOI for Multiplexed experimental strategies for fragment library screening against challenging drug targets using SPR biosensors
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Identification of fragments targeting SMYD3 using highly sensitive kinetic and multiplexed biosensor-based screening

FitzGerald, Edward A.; Cederfelt, Daniela; Lund, Bjarte Aarmo; Myers, Nadine et al.

Part of RSC Medicinal Chemistry, p. 1982-1990, 2024

• DOI for Identification of fragments targeting SMYD3 using highly sensitive kinetic and multiplexed biosensor-based screening
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Regulatory effects of RNA-protein interactions revealed by reporter assays of bacteria grown on solid media

Pérez-Ropero, Guillermo; Dolcemascolo, Roswitha; Pérez-Ràfols, Anna; Andersson, Karl et al.

Part of Biosensors, 2025

• DOI for Regulatory effects of RNA-protein interactions revealed by reporter assays of bacteria grown on solid media
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Integrated computational and biosensor-based strategies for the discovery of allosteric SMYD3 ligands using diperodon as a starting point

FitzGerald, Edward; Rachman, Moira; Cederfelt, Daniela; Myers, Nadine et al.

Part of Bioorganic & Medicinal Chemistry, 2025

• DOI for Integrated computational and biosensor-based strategies for the discovery of allosteric SMYD3 ligands using diperodon as a starting point
• Download full text (pdf) of Integrated computational and biosensor-based strategies for the discovery of allosteric SMYD3 ligands using diperodon as a starting point

Unraveling the Bivalent and Rapid Interactions Between a Multivalent RNA Recognition Motif and RNA: A Kinetic Approach

Pérez-Ropero, Guillermo; Perez-Rafols, Anna; Martelli, Tommasso; Danielson, U. Helena et al.

Part of Biochemistry, p. 2816-2829, 2024

• DOI for Unraveling the Bivalent and Rapid Interactions Between a Multivalent RNA Recognition Motif and RNA: A Kinetic Approach
• Download full text (pdf) of Unraveling the Bivalent and Rapid Interactions Between a Multivalent RNA Recognition Motif and RNA: A Kinetic Approach

Multiplexed experimental strategies for fragment library screening against challenging drug targets using SPR biosensors

FitzGerald, Edward; Vagrys, Darius; Opassi, Giulia; Klein, Hanna F. et al.

Part of SLAS Discovery, p. 40-51, 2024

• DOI for Multiplexed experimental strategies for fragment library screening against challenging drug targets using SPR biosensors
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Identification of fragments targeting SMYD3 using highly sensitive kinetic and multiplexed biosensor-based screening

FitzGerald, Edward A.; Cederfelt, Daniela; Lund, Bjarte Aarmo; Myers, Nadine et al.

Part of RSC Medicinal Chemistry, p. 1982-1990, 2024

• DOI for Identification of fragments targeting SMYD3 using highly sensitive kinetic and multiplexed biosensor-based screening
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The Role of Water Networks in Phosphodiesterase Inhibitor Dissociation and Kinetic Selectivity

Blaazer, Antoni R.; Singh, Abhimanyu K.; Zara, Lorena; Boronat, Pierre et al.

Part of ChemMedChem, 2024

• DOI for The Role of Water Networks in Phosphodiesterase Inhibitor Dissociation and Kinetic Selectivity
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Production of stable and pure ZC3H11A-An extensively disordered RNA binding protein

Fekry, Mostafa; Stenberg, Gun; Dobritzsch, Doreen; Danielson, U. Helena

Part of Protein Expression and Purification, 2024

• DOI for Production of stable and pure ZC3H11A-An extensively disordered RNA binding protein
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The Allosteric Regulation of Β-Ureidopropionase Depends on Fine-Tuned Stability of Active-Site Loops and Subunit Interfaces

Cederfelt, Daniela; Badgujar, Dilip; Au Musse, Ayan; Lohkamp, Bernhard et al.

Part of Biomolecules, 2023

• DOI for The Allosteric Regulation of Β-Ureidopropionase Depends on Fine-Tuned Stability of Active-Site Loops and Subunit Interfaces
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The Crystal Structure of Tyrosinase from Verrucomicrobium spinosum Reveals It to Be an Atypical Bacterial Tyrosinase

Fekry, Mostafa; Dave, Khyati K.; Badgujar, Dilip; Hamnevik, Emil et al.

Part of Biomolecules, 2023

• DOI for The Crystal Structure of Tyrosinase from Verrucomicrobium spinosum Reveals It to Be an Atypical Bacterial Tyrosinase
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Amino acid substitutions in human growth hormone affect secondary structure and receptor binding

Rajkovic, Andrei; Kanchugal, Sandesh; Abdurakhmanov, Eldar; Howard, Rebecca et al.

Part of PLOS ONE, 2023

• DOI for Amino acid substitutions in human growth hormone affect secondary structure and receptor binding
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Discovery of the 4-aminopiperidine-based compound EM127 for the site-specific covalent inhibition of SMYD3

Parenti, Marco Daniele; Naldi, Marina; Manoni, Elisabetta; Fabini, Edoardo et al.

Part of European Journal of Medicinal Chemistry, 2022

• DOI for Discovery of the 4-aminopiperidine-based compound EM127 for the site-specific covalent inhibition of SMYD3

Monitoring drug–target interactions through target engagement-mediated amplification on arrays and in situ

Al-Amin, Rasel A.; Johansson, Lars; Abdurakhmanov, Eldar; Landegren, Nils et al.

Part of Nucleic Acids Research, 2022

• DOI for Monitoring drug–target interactions through target engagement-mediated amplification on arrays and in situ
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Ultralarge Virtual Screening Identifies SARS-CoV-2 Main Protease Inhibitors with Broad-Spectrum Activity against Coronaviruses

Luttens, Andreas; Gullberg, Hjalmar; Abdurakhmanov, Eldar; Vo, Duy Duc et al.

Part of Journal of the American Chemical Society, p. 2905-2920, 2022

• DOI for Ultralarge Virtual Screening Identifies SARS-CoV-2 Main Protease Inhibitors with Broad-Spectrum Activity against Coronaviruses
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Sensitive protein detection using site-specifically oligonucleotide-conjugated nanobody reagents

Al-Amin, Rasel Abdullah; Muthelo, Phathutshedzo M.; Abdurakhmanov, Eldar; Vincke, Cecile et al.

Part of Analytical Chemistry, p. 10054-10061, 2022

• DOI for Sensitive protein detection using site-specifically oligonucleotide-conjugated nanobody reagents
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Discovery of an allosteric ligand binding site in SMYD3 lysine methyltransferase

Talibov, Vladimir O; Fabini, Edoardo; FitzGerald, Edward; Tedesco, Daniele et al.

Part of ChemBioChem, p. 1597-1608, 2021

• DOI for Discovery of an allosteric ligand binding site in SMYD3 lysine methyltransferase
• Download full text (pdf) of Discovery of an allosteric ligand binding site in SMYD3 lysine methyltransferase

Discovery of fragments inducing conformational effects in dynamic proteins using a second-harmonic generation biosensor

FitzGerald, Edward A.; Butko, Margaret T.; Boronat, Pierre; Cederfelt, Daniela et al.

Part of RSC Advances, p. 7527-7537, 2021

• DOI for Discovery of fragments inducing conformational effects in dynamic proteins using a second-harmonic generation biosensor
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A real-time cell-binding assay reveals dynamic features of STxB-Gb3 cointernalization and STxB-mediated cargo delivery into cancer cells

Encarnacao, Joao Crispim; Napolitano, Valeria; Opassi, Giulia; Danielson, U. Helena et al.

Part of FEBS Letters, p. 2406-2420, 2020

• DOI for A real-time cell-binding assay reveals dynamic features of STxB-Gb3 cointernalization and STxB-mediated cargo delivery into cancer cells
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Establishing Trypanosoma cruzi farnesyl pyrophosphatesynthase as a viable target for biosensor driven fragment-based lead discovery

Opassi, Giulia; Nordström, Helena; Lundin, Arne; Napolitano, Valeria et al.

Part of Protein Science, p. 991-1003, 2020

• DOI for Establishing Trypanosoma cruzi farnesyl pyrophosphatesynthase as a viable target for biosensor driven fragment-based lead discovery
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Macrocyclic Peptides Uncover a Novel Binding Mode for Reversible Inhibitors of LSD1

Yang, Jie; Talibov, Vladimir O; Peintner, Stefan; Rhee, Claire et al.

Part of ACS Omega, p. 3979-3995, 2020

• DOI for Macrocyclic Peptides Uncover a Novel Binding Mode for Reversible Inhibitors of LSD1
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Estimating Detection Limits of Potentiometric DNA sensors Using Surface Plasmon Resonance Analyses

Xu, Xingxing; Makaraviciute, Asta; Abdurakhmanov, Eldar; Werneling, Fredrik et al.

Part of ACS Sensors, p. 217-224, 2020

• DOI for Estimating Detection Limits of Potentiometric DNA sensors Using Surface Plasmon Resonance Analyses

Fibrin fragment E potentiates TGF-beta-induced myofibroblast activation and recruitment

Öhman Fuchs, Peder; Calitz, Carlemi; Pavlovic, Natasa; Binet, Francois et al.

Part of Cellular Signalling, 2020

• DOI for Fibrin fragment E potentiates TGF-beta-induced myofibroblast activation and recruitment
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Unveiling the Biochemistry of the Epigenetic Regulator SMYD3

Fabini, Edoardo; Talibov, Vladimir O; Mihalic, Filip; Naldi, Marina et al.

Part of Biochemistry, p. 3634-3645, 2019

• DOI for Unveiling the Biochemistry of the Epigenetic Regulator SMYD3

Structural Changes of Mercaptohexanol Self-assembled Monolayers on Gold and their Influence on Impedimetric Aptamer Sensors

Xu, Xingxing; Makaraviciute, Asta; Kumar, Shalen; Wen, Chenyu et al.

Part of Analytical Chemistry, p. 14697-14704, 2019

• DOI for Structural Changes of Mercaptohexanol Self-assembled Monolayers on Gold and their Influence on Impedimetric Aptamer Sensors

Noelin1 Affects Lateral Mobility of Synaptic AMPA Receptors

Pandya, Nikhil J; Seeger, Christian; Babai, Norbert; Gonzalez-Lozano, Miguel A et al.

Part of Cell Reports, p. 1218-1230, 2018

• DOI for Noelin1 Affects Lateral Mobility of Synaptic AMPA Receptors
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Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design

Linkuviene, Vaida; Talibov, Vladimir O; Danielson, U. Helena; Matulis, Daumantas

Part of Journal of Medicinal Chemistry, p. 2292-2302, 2018

• DOI for Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design

Pan-NS3 protease inhibitors of hepatitis C virus based on an R3-elongated pyrazinone scaffold

Belfrage, Anna Karin; Abdurakhmanov, Eldar; Åkerblom, Eva; Brandt, Peter et al.

Part of European Journal of Medicinal Chemistry, p. 453-464, 2018

• DOI for Pan-NS3 protease inhibitors of hepatitis C virus based on an R3-elongated pyrazinone scaffold

Intrinsic vs. observed thermodynamic and kinetic parameters of carbonic anhydrase-ligand interaction

Linkuviene, V.; Talibov, Vladimir O.; Danielson, U. Helena; Matulis, D.

Part of European Biophysics Journal, 2017

• DOI for Intrinsic vs. observed thermodynamic and kinetic parameters of carbonic anhydrase-ligand interaction

Intrinsic vs. observed thermodynamic and kinetic parameters of carbonic anhydrase-ligand interaction

Linkuviene, V.; Talibov, Vladimir O; Danielson, U. Helena; Matulis, D.

Part of European Biophysics Journal, 2017

• DOI for Intrinsic vs. observed thermodynamic and kinetic parameters of carbonic anhydrase-ligand interaction

Characterization of interactions between hepatitis C virus NS5B polymerase, annexin A2 and RNA - effects on NS5B catalysis and allosteric inhibition

Solbak, Sara M.Ø.; Abdurakhmanov, Eldar; Vedeler, Anni; Danielson, U. Helena

Part of Virology Journal, 2017

• DOI for Characterization of interactions between hepatitis C virus NS5B polymerase, annexin A2 and RNA - effects on NS5B catalysis and allosteric inhibition
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Insights from engineering the Affibody-Fc interaction with a computational-experimental method

Nosrati, Masoumeh; Solbak, Sara; Nordesjö, Olle; Nissbeck, Mikael et al.

Part of Protein Engineering Design & Selection, p. 593-601, 2017

• DOI for Insights from engineering the Affibody-Fc interaction with a computational-experimental method

Biophysical Mode-of-Action and Selectivity Analysis of Allosteric Inhibitors of Hepatitis C Virus (HCV) Polymerase

Abdurakhmanov, Eldar; Solbak, Sara Oie; Danielson, U. Helena

Part of Viruses, 2017

• DOI for Biophysical Mode-of-Action and Selectivity Analysis of Allosteric Inhibitors of Hepatitis C Virus (HCV) Polymerase
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Monitoring drug-serum protein interactions for early ADME prediction through Surface Plasmon Resonance technology

Fabini, Edoardo; Danielson, U. Helena

Part of Journal of Pharmaceutical and Biomedical Analysis, p. 188-194, 2017

• DOI for Monitoring drug-serum protein interactions for early ADME prediction through Surface Plasmon Resonance technology

Biophysical analysis of the dynamics of calmodulin interactions with neurogranin and Ca²⁺/calmodulin-dependent kinase II

Seeger, Christian; Talibov, Vladimir O; Danielson, U. Helena

Part of Journal of Molecular Recognition, p. 1-11, 2017

• DOI for Biophysical analysis of the dynamics of calmodulin interactions with neurogranin and Ca²⁺/calmodulin-dependent kinase II
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Development of a novel therapeutic vaccine carrier that sustains high antibody titers against several targets simultaneously

Saupe, Falk; Reichel, Matthias; Huijbers, Elisabeth J. M.; Femel, Julia et al.

Part of The FASEB Journal, p. 1204-1214, 2017

• DOI for Development of a novel therapeutic vaccine carrier that sustains high antibody titers against several targets simultaneously

Discovery of pyrazinone based compounds that potently inhibit the drug resistant enzyme variant R155K of the hepatitis C virus NS3 protease

Belfrage, Anna Karin; Abdurakhmanov, Eldar; Åkerblom, Eva; Brandt, Peter et al.

Part of Bioorganic & Medicinal Chemistry, p. 2603-2620, 2016

• DOI for Discovery of pyrazinone based compounds that potently inhibit the drug resistant enzyme variant R155K of the hepatitis C virus NS3 protease

Kinetically Selective Inhibitors of Human Carbonic Anhydrase Isozymes I, II, VII, IX, XII, and XIII

Talibov, Vladimir O; Linkuvienė, Vaida; Matulis, Daumantas; Danielson, Helena U.

Part of Journal of Medicinal Chemistry, p. 2083-2093, 2016

• DOI for Kinetically Selective Inhibitors of Human Carbonic Anhydrase Isozymes I, II, VII, IX, XII, and XIII

Analysis of the leakage of gene repression by an artificial TetR-regulated promoter in cyanobacteria

Danielson, U Helena; Huang, H H; Seeger, Christian; Lindblad, Peter

Part of BMC Research Notes, p. 459, 2015

Analysis of the leakage of gene repression by an artificial TetR-regulated promoter in cyanobacteria

Huang, Hsin-Ho; Seeger, Christian; Danielson, U. Helena; Lindblad, Peter

Part of BMC Research Notes, 2015

• DOI for Analysis of the leakage of gene repression by an artificial TetR-regulated promoter in cyanobacteria
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Identification and Characterization of an Irreversible Inhibitor of CDK2

Anscombe, Elizabeth; Meschini, Elisa; Mora-Vidal, Regina; Martin, Mathew P. et al.

Part of Chemistry and Biology, p. 1159-1164, 2015

• DOI for Identification and Characterization of an Irreversible Inhibitor of CDK2
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Proximity-dependent initiation of hybridization chain reaction

Koos, Björn; Cane, Gaëlle; Grannas, Karin; Löf, Liza et al.

Part of Nature Communications, 2015

• DOI for Proximity-dependent initiation of hybridization chain reaction
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Molecular blueprint of allosteric binding sites in a homologue of the agonist-binding domain of the alpha 7 nicotinic acetylcholine receptor

Spurny, Radovan; Debaveye, Sarah; Farinha, Ana; Veys, Ken et al.

Part of Proceedings of the National Academy of Sciences of the United States of America, 2015

• DOI for Molecular blueprint of allosteric binding sites in a homologue of the agonist-binding domain of the alpha 7 nicotinic acetylcholine receptor

Identification of weak points of hepatitis C virus NS3 protease inhibitors using surface plasmon resonance biosensor-based interaction kinetic analysis and genetic variants

Svahn Gustafsson, Sofia; Ehrenberg, Angelica; Schmuck, Benjamin; Anwar, Mohammed Ikram et al.

Part of Journal of Medicinal Chemistry, p. 1802-1811, 2014

Accounting for strain variations and resistance mutations in the characterization of hepatitis C NS3 protease inhibitors

Ehrenberg, Angelica; Schmuck, Benjamin; Anwar, Muhammad Ikram; Svahn Gustafsson, Sofia et al.

Part of Journal of enzyme inhibition and medicinal chemistry (Print), p. 868-876, 2014

• DOI for Accounting for strain variations and resistance mutations in the characterization of hepatitis C NS3 protease inhibitors

Vinylated linear P2 pyrimidinyloxyphenylglycine based inhibitors of the HCV NS3/4A protease and corresponding macrocycles

Lampa, Anna; Alogheli, Hiba; Ehrenberg, Angelica E.; Åkerblom, Eva et al.

Part of Bioorganic & Medicinal Chemistry, p. 6595-6615, 2014

• DOI for Vinylated linear P2 pyrimidinyloxyphenylglycine based inhibitors of the HCV NS3/4A protease and corresponding macrocycles

Novel Peptidomimetic Hepatitis C Virus NS3/4A Protease Inhibitors Spanning the P2–P1′ Region

Lampa, Anna; Bergman, Sara; Svahn Gustafsson, Sofia; Alogheli, Hiba et al.

Part of ACS Medicinal Chemistry Letters, p. 249-254, 2014

• DOI for Novel Peptidomimetic Hepatitis C Virus NS3/4A Protease Inhibitors Spanning the P2–P1′ Region

Identification of Weak Points of Hepatitis C Virus NS3 Protease Inhibitors Using Surface Plasmon Resonance Biosensor-Based Interaction Kinetic Analysis and Genetic Variants

Svahn Gustafsson, Sofia; Ehrenberg, Angelica; Schmuck, Benjamin; Anwar, Muhammad Ikram et al.

Part of Journal of Medicinal Chemistry, p. 1802-1811, 2014

• DOI for Identification of Weak Points of Hepatitis C Virus NS3 Protease Inhibitors Using Surface Plasmon Resonance Biosensor-Based Interaction Kinetic Analysis and Genetic Variants

Achiral Pyrazinone-Based Inhibitors of the Hepatitis C Virus NS3 Protease and Drug-Resistant Variants with Elongated Substituents Directed Toward the S2 Pocket

Gising, Johan; Belfrage, Anna Karin; Alogheli, Hiba; Ehrenberg, Angelica et al.

Part of Journal of Medicinal Chemistry, p. 1790-1801, 2014

• DOI for Achiral Pyrazinone-Based Inhibitors of the Hepatitis C Virus NS3 Protease and Drug-Resistant Variants with Elongated Substituents Directed Toward the S2 Pocket

The Versatile Nature of the 6-Aminoquinolone Scaffold: Identification of Submicromolar Hepatitis C Virus NS5B Inhibitors

Manfroni, Giuseppe; Cannalire, Rolando; Barreca, Maria Letizia; Kaushik-Basu, Neerja et al.

Part of Journal of Medicinal Chemistry, p. 1952-1963, 2014

• DOI for The Versatile Nature of the 6-Aminoquinolone Scaffold: Identification of Submicromolar Hepatitis C Virus NS5B Inhibitors

Identification and characterization of an irreversible inhibitor of CDK2

Martin, M.; Anscombe, E.; Meschini, E.; Staunton, D. et al.

Part of European Journal of Cancer, p. 106-106, 2014

• DOI for Identification and characterization of an irreversible inhibitor of CDK2

Resolution of the Interaction Mechanisms and Characteristics of Non-nucleoside Inhibitors of Hepatitis C Virus Polymerase - Laying the Foundation for Discovery of Allosteric HCV Drugs

Winquist, Johan; Abdurakhmanov, Eldar; Baraznenok, Vera; Henderson, Ian et al.

Part of Antiviral Research, p. 356-368, 2013

• DOI for Resolution of the Interaction Mechanisms and Characteristics of Non-nucleoside Inhibitors of Hepatitis C Virus Polymerase - Laying the Foundation for Discovery of Allosteric HCV Drugs

Efficient Screening of Marine Extracts for Protease Inhibitors by Combining FRET Based Activity Assays and Surface Plasmon Resonance Spectroscopy Based Binding Assays

Christopeit, Tony; Øverbø, Kersti; Danielson, Helena; Nilsen, Inge W.

Part of Marine Drugs, p. 4279-4293, 2013

• DOI for Efficient Screening of Marine Extracts for Protease Inhibitors by Combining FRET Based Activity Assays and Surface Plasmon Resonance Spectroscopy Based Binding Assays
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Identification of Structural-Kinetic and Structural-Thermodynamic Relationships for Thrombin Inhibitors

Winquist, Johan; Geschwindner, Stefan; Xue, Yafeng; Gustavsson, Lars et al.

Part of Biochemistry, p. 613-626, 2013

• DOI for Identification of Structural-Kinetic and Structural-Thermodynamic Relationships for Thrombin Inhibitors

The advantage of biosensor analysis over enzyme inhibition studies for slow dissociating inhibitors: characterization of hydroxamate-based matrix metalloproteinase-12 inhibitors

Gossas, Thomas; Nordström, Helena; Xu, Ming-Hua; Sun, Zhi-Hua et al.

Part of MedChemComm, p. 432-442, 2013

• DOI for The advantage of biosensor analysis over enzyme inhibition studies for slow dissociating inhibitors: characterization of hydroxamate-based matrix metalloproteinase-12 inhibitors

Structural basis of ligand recognition in 5-HT3 receptors

Kesters, D.; Thompson, A. J.; Brams, M.; Van Elk, R. et al.

Part of EMBO Reports, p. 49-56, 2013

• DOI for Structural basis of ligand recognition in 5-HT3 receptors

On the Active Site Protonation State in Aspartic Proteases: Implications for Drug Design

Sussman, Fredy; Carmen Villaverde, M.; Dominguez, Jose L.; Danielson, Helena

Part of Current pharmaceutical design, p. 4257-4275, 2013

• DOI for On the Active Site Protonation State in Aspartic Proteases: Implications for Drug Design

Structure-Based Discovery of Pyrazolobenzothiazine Derivatives As Inhibitors of Hepatitis C Virus Replication

Barreca, Maria Letizia; Manfroni, Giuseppe; Leyssen, Pieter; Winquist, Johan et al.

Part of Journal of Medicinal Chemistry, p. 2270-2282, 2013

• DOI for Structure-Based Discovery of Pyrazolobenzothiazine Derivatives As Inhibitors of Hepatitis C Virus Replication

Aliskiren displays long-lasting interactions with human renin

Gossas, Thomas; Vrang, Lotta; Henderson, Ian; Sedig, Susanne et al.

Part of Naunyn-Schmiedeberg's Archives of Pharmacology, p. 219-224, 2012

• DOI for Aliskiren displays long-lasting interactions with human renin

Histaminergic pharmacology of homo-oligomeric beta 3 gamma-aminobutyric acid type A receptors characterized by surface plasmon resonance biosensor technology

Seeger, Christian; Christopeit, Tony; Fuchs, Karoline; Grote, Katharina et al.

Part of Biochemical Pharmacology, p. 341-351, 2012

• DOI for Histaminergic pharmacology of homo-oligomeric beta 3 gamma-aminobutyric acid type A receptors characterized by surface plasmon resonance biosensor technology

Kinetic and mechanistic differences in the interactions between caldendrin and calmodulin with AKAP79 suggest different roles in synaptic function

Seeger, Christian; Gorny, Xenia; Reddy, Pasham Parameshwar; Seidenbecher, Constanze et al.

Part of Journal of Molecular Recognition, p. 495-503, 2012

• DOI for Kinetic and mechanistic differences in the interactions between caldendrin and calmodulin with AKAP79 suggest different roles in synaptic function

Experimental and 'in silico' analysis of the effect of pH on HIV-1 protease inhibitor affinity: Implications for the charge state of the protein ionogenic groups

Dominguez, Jose L.; Gossas, Thomas; Carmen Villaverde, M.; Danielson, U. Helena et al.

Part of Bioorganic & Medicinal Chemistry, p. 4838-4847, 2012

• DOI for Experimental and 'in silico' analysis of the effect of pH on HIV-1 protease inhibitor affinity: Implications for the charge state of the protein ionogenic groups

AKAP79/150 interacts with the neuronal calcium-binding protein caldendrin

Gorny, Xenia; Mikhaylova, Marina; Seeger, Christian; Reddy, Pasham Parameshwar et al.

Part of Journal of Neurochemistry, p. 714-726, 2012

• DOI for AKAP79/150 interacts with the neuronal calcium-binding protein caldendrin

Synthesis and SAR Around the R6 Position of 2(1H)-Pyrazinone Based HCV NS3 Protease Inhibitors

Belfrage, Anna-Karin; Gising, Johan; Örtqvist, Pernilla; Alogheli, Hiba et al.

Part of Biopolymers, p. 457-457, 2011

Quantification of interactions between drug leads and serum proteins by use of "binding efficiency"

Gustafsson, Sofia S.; Vrang, Lotta; Terelius, Ylva; Danielson, Helena

Part of Analytical Biochemistry, p. 163-175, 2011

• DOI for Quantification of interactions between drug leads and serum proteins by use of "binding efficiency"

Deconstruction of Non-Nucleoside Reverse Transcriptase Inhibitors of Human Immunodeficiency Virus Type 1 for Exploration of the Optimization Landscape of Fragments

Brandt, Peter; Geitmann, Matthis; Danielson, U Helena

Part of Journal of Medicinal Chemistry, 2011

• DOI for Deconstruction of Non-Nucleoside Reverse Transcriptase Inhibitors of Human Immunodeficiency Virus Type 1 for Exploration of the Optimization Landscape of Fragments

Powerful protein binders from designed polypeptides and small organic molecules: a general concept for protein recognition

Tegler, Lotta T.; Nonglaton, Guillaume; Büttner, Frank; Caldwell, Karin et al.

Part of Angewandte Chemie International Edition, p. 1823-1827, 2011

• DOI for Powerful protein binders from designed polypeptides and small organic molecules: a general concept for protein recognition

A surface plasmon resonance-based biosensor with full-length BACE1 in a reconstituted membrane

Christopeit, Tony; Stenberg, Gun; Gossas, Thomas; Nyström, Susanne et al.

Part of Analytical Biochemistry, p. 14-22, 2011

• DOI for A surface plasmon resonance-based biosensor with full-length BACE1 in a reconstituted membrane

Mechanistic and kinetic characterization of hepatitis C virus NS3 protein interactions with NS4A and protease inhibitors

Geitmann, Matthis; Dahl, Göran; Danielson, U. Helena

Part of Journal of Molecular Recognition, p. 60-70, 2011

• DOI for Mechanistic and kinetic characterization of hepatitis C virus NS3 protein interactions with NS4A and protease inhibitors

Identification of a Novel Scaffold for Allosteric Inhibition of Wild Type and Drug Resistant HIV-1 Reverse Transcriptase by Fragment Library Screening

Geitmann, Matthis; Elinder, Malin; Seeger, Christian; Brandt, Peter et al.

Part of Journal of Medicinal Chemistry, p. 699-708, 2011

• DOI for Identification of a Novel Scaffold for Allosteric Inhibition of Wild Type and Drug Resistant HIV-1 Reverse Transcriptase by Fragment Library Screening

Experimental Validation of a Fragment Library for Lead Discovery Using SPR Biosensor Technology

Elinder, Malin; Geitmann, Matthis; Gossas, Thomas; Källblad, Per et al.

Part of Journal of Biomolecular Screening, p. 15-25, 2011

• DOI for Experimental Validation of a Fragment Library for Lead Discovery Using SPR Biosensor Technology

P2-P1 ' macrocyclization of P2 phenylglycine based HCV NS3 protease inhibitors using ring-closing metathesis

Lampa, Anna; Ehrenberg, Angelica E.; Vema, Aparna; Åkerblom, Eva et al.

Part of Bioorganic & Medicinal Chemistry, p. 4917-4927, 2011

• DOI for P2-P1 ' macrocyclization of P2 phenylglycine based HCV NS3 protease inhibitors using ring-closing metathesis

Hepatitis C Virus NS3 Protease Inhibitors based on 2(1H)-Pyrazinones

Belfrage, Anna-Karin; Gising, Johan; Örtqvist, Pernilla; Danielson, U Helena et al.

Part of Journal of Peptide Science, p. 95-95, 2010

Discovery of Achiral Inhibitors of the Hepatitis C Virus NS3 Protease based on 2(1H)-pyrazinones

Örtqvist, Pernilla; Gising, Johan; Ehrenberg, Angelica; Vema, Aparna et al.

Part of Bioorganic & Medicinal Chemistry, p. 6512-6525, 2010

• DOI for Discovery of Achiral Inhibitors of the Hepatitis C Virus NS3 Protease based on 2(1H)-pyrazinones

Hepatitis C protease inhibitors based on 2(1H)-pyrazinones

Gising, Johan; Belfrage, Anna Karin; Örtqvist, Pernilla; Larhed, Mats et al.

Part of Abstracts of Papers of the American Chemical Society, 2010

Structure-activity relationships of HCV NS3 protease inhibitors evaluated on the drug-resistant variants A156T and D168V

Örtqvist, Pernilla; Vema, Aparna; Ehrenberg, Angelica E; Dahl, Göran et al.

Part of Antiviral Therapy, p. 841-852, 2010

• DOI for Structure-activity relationships of HCV NS3 protease inhibitors evaluated on the drug-resistant variants A156T and D168V

Improved P2 phenylglycine-based hepatitis C virus NS3 protease inhibitors with alkenylic prime-side substituents

Lampa, Anna; Ehrenberg, Angelica E.; Gustafsson, Sofia S.; Vema, Aparna et al.

Part of Bioorganic & Medicinal Chemistry, p. 5413-5424, 2010

• DOI for Improved P2 phenylglycine-based hepatitis C virus NS3 protease inhibitors with alkenylic prime-side substituents

Effect of the Protonation State of the Titratable Residues on the Inhibitor Affinity to BACE-1

Domínguez, José L; Christopeit, Tony; Villaverde, M Carmen; Gossas, Thomas et al.

Part of Biochemistry, p. 7255-7263, 2010

• DOI for Effect of the Protonation State of the Titratable Residues on the Inhibitor Affinity to BACE-1

Biotinylated lipid bilayer disks as model membranes for biosensor analyses

Lundquist, Anna; Hansen, Søren B; Nordström, Helena; Danielson, U Helena et al.

Part of Analytical Biochemistry, p. 153-159, 2010

• DOI for Biotinylated lipid bilayer disks as model membranes for biosensor analyses

Inhibition of HIV-1 by non-nucleoside reverse transcriptase inhibitors via an induced fit mechanism: Importance of slow dissociation and relaxation rates for antiviral efficacy

Elinder, Malin; Selhorst, Philippe; Vanham, Guido; Öberg, Bo et al.

Part of Biochemical Pharmacology, p. 1133-1140, 2010

• DOI for Inhibition of HIV-1 by non-nucleoside reverse transcriptase inhibitors via an induced fit mechanism: Importance of slow dissociation and relaxation rates for antiviral efficacy

Surface Plasmon Resonance Biosensor Based Fragment Screening Using Acetylcholine Binding Protein Identifies Ligand Efficiency Hot Spots (LE Hot Spots) by Deconstruction of Nicotinic Acetylcholine Receptor α7 Ligands

de Kloe, Gerdien E; Retra, Kim; Geitmann, Matthis; Källblad, Per et al.

Part of Journal of Medicinal Chemistry, p. 7192-7201, 2010

• DOI for Surface Plasmon Resonance Biosensor Based Fragment Screening Using Acetylcholine Binding Protein Identifies Ligand Efficiency Hot Spots (LE Hot Spots) by Deconstruction of Nicotinic Acetylcholine Receptor α7 Ligands

Development of surface plasmon resonance biosensor assays for primary and secondary screening of acetylcholine binding protein ligands

Retra, Kim; Geitmann, Matthis; Kool, Jeroen; Smit, August B et al.

Part of Analytical Biochemistry, p. 58-64, 2010

• DOI for Development of surface plasmon resonance biosensor assays for primary and secondary screening of acetylcholine binding protein ligands

Interaction kinetic and structural dynamic analysis of ligand binding to acetylcholine-binding protein

Geitmann, Matthis; Retra, Kim; de Kloe, Gerdien E; Homan, Evert et al.

Part of Biochemistry, p. 8143-8154, 2010

• DOI for Interaction kinetic and structural dynamic analysis of ligand binding to acetylcholine-binding protein

Integrating surface plasmon resonance biosensor-based interaction kinetic analyses into the lead discovery and optimization process

Danielson, U Helena

Part of Future Medicinal Chemistry, p. 1399-1414, 2009

Screening for NNRTIs with Slow Dissociation and High Affinity for a Panel of HIV-1 RT Variants

Elinder, Malin; Nordström, Helena; Geitmann, Matthis; Hämäläinen, Markku et al.

Part of Journal of Biomolecular Screening, p. 395-403, 2009

• DOI for Screening for NNRTIs with Slow Dissociation and High Affinity for a Panel of HIV-1 RT Variants

A protein interaction node at the neurotransmitter release site: domains of Aczonin/Piccolo, Bassoon, CAST, and rim converge on the N-terminal domain of Munc13-1

Wang, Xiaolu; Hu, Bin; Zieba, Agata; Neumann, Nicole G et al.

Part of Journal of Neuroscience, p. 12584-12596, 2009

• DOI for A protein interaction node at the neurotransmitter release site: domains of Aczonin/Piccolo, Bassoon, CAST, and rim converge on the N-terminal domain of Munc13-1

Integrating surface plasmon resonance biosensor-based interaction kinetic analyses into the lead discovery and optimization process

Danielson, U. Helena

Part of Future Medicinal Chemistry, p. 1399-1414, 2009

• DOI for Integrating surface plasmon resonance biosensor-based interaction kinetic analyses into the lead discovery and optimization process

Structural and Functional Analysis of Hepatitis C Virus Strain JFH1 Polymerase

Simister, Philip; Schmitt, Melanie; Geitmann, Matthis; Wicht, Oliver et al.

Part of Journal of Virology, p. 11926-11939, 2009

• DOI for Structural and Functional Analysis of Hepatitis C Virus Strain JFH1 Polymerase

Hepatitis C Virus NS3 Protease Is Activated by Low Concentrations of  Protease Inhibitors

Dahl, Göran; Gutiérrez Arenas, Omar; Danielson, Helena

Part of Biochemistry, p. 11592-11602, 2009

• DOI for Hepatitis C Virus NS3 Protease Is Activated by Low Concentrations of  Protease Inhibitors

Fragment library screening and lead characterization using SPR biosensors

Danielson, U Helena

Part of Current Topics in Medicinal Chemistry, p. 1725-1735, 2009

• DOI for Fragment library screening and lead characterization using SPR biosensors

HSA binding of HIV protease inhibitors: a high-performance affinity chromatography study

Bertucci, Carlo; Pistolozzi, Marco; Felix, Guy; Danielson, Helena

Part of Journal of Separation Science, p. 1625-1631, 2009

• DOI for HSA binding of HIV protease inhibitors: a high-performance affinity chromatography study

Characterization of Ca2+ and phosphocholine interactions with C-reactive protein using a surface plasmon resonance biosensor

Christopeit, Tony; Gossas, Thomas; Danielson, Helena

Part of Analytical Biochemistry, p. 39-44, 2009

• DOI for Characterization of Ca2+ and phosphocholine interactions with C-reactive protein using a surface plasmon resonance biosensor

MIV-170, a novel NNRTI exhibiting tight binding to HIV-1 reverse transcriptase (RT)

Elinder, Malin; Danielson, U Helena; Unge, Torsten; van Ham, Guido et al.

Part of Antiviral Research, 2008

Hepatitis C Virus NS3 Protease Inhibitors Comprising a Novel Aromatic P1 Moiety

Rönn, Robert; Lampa, Anna; Peterson, Shane D.; Gossas, Thomas et al.

Part of Bioorganic & Medicinal Chemistry, p. 2955-2967, 2008

• DOI for Hepatitis C Virus NS3 Protease Inhibitors Comprising a Novel Aromatic P1 Moiety

Identification of MMP-12 Inhibitors by Using Biosensor-Based Screening of a Fragment Library

Nordström, Helena; Gossas, Thomas; Hämäläinen, Markku; Källblad, Per et al.

Part of Journal of Medicinal Chemistry, p. 3449-3459, 2008

• DOI for Identification of MMP-12 Inhibitors by Using Biosensor-Based Screening of a Fragment Library

β-Amino acid substitutions and structure-based CoMFA modeling of hepatitis C virus NS3 protease inhibitors

Nurbo, Johanna; Peterson, Shane D.; Dahl, Göran; Danielson, U. Helena et al.

Part of Bioorganic & Medicinal Chemistry, p. 5590-5605, 2008

• DOI for β-Amino acid substitutions and structure-based CoMFA modeling of hepatitis C virus NS3 protease inhibitors

Evaluation of a diverse set of potential P-1 carboxylic acid bioisosteres in hepatitis C virus NS3 protease inhibitors

Rönn, Robert; Gossas, Thomas; Sabnis, Yogesh A; Daoud, H et al.

Part of Bioorganic & Medicinal Chemistry, p. 1448-1474, 2007

Investigation of beta-amino acids as building blocks in hepatitis c virus NS3 protease inhibitors

Nurbo, Johanna; Dahl, Göran; Danielson, U Helena; Sandström, Anja

Part of Biopolymers, p. 580-580, 2007

Phenylglycine as a Novel P2 Scaffold in Hepatitis C Virus NS3 Protease Inhibitors

Örtqvist, Pernilla; Peterson, Shane D.; Åkerblom, Eva; Gossas, Thomas et al.

Part of Bioorganic & Medicinal Chemistry, p. 1448-1474, 2007

• DOI for Phenylglycine as a Novel P2 Scaffold in Hepatitis C Virus NS3 Protease Inhibitors

Mechanistic studies of electrophilic protease inhibitors of full length hepatic C virus (HCV) NS3

Poliakov, Anton; Sandström, Anja; Åkerblom, Eva; Danielson, U. Helena

Part of Journal of enzyme inhibition and medicinal chemistry (Print), p. 191-199, 2007

• DOI for Mechanistic studies of electrophilic protease inhibitors of full length hepatic C virus (HCV) NS3

Evaluation of a diverse set of potential P1 carboxylic acid bioisosteres in hepatitis C virus NS3 protease inhibitors

Rönn, Robert; Gossas, Thomas; Sabnis, Yogesh A.; Daoud, Hanna et al.

Part of Bioorganic & Medicinal Chemistry, p. 4057-4068, 2007

• DOI for Evaluation of a diverse set of potential P1 carboxylic acid bioisosteres in hepatitis C virus NS3 protease inhibitors

Effects on protease inhibition by modifying of helicase residues in hepatitis C virus nonstructural protein 3

Dahl, Göran; Sandström, Anja; Åkerblom, Eva; Danielson, U. Helena

Part of The FEBS Journal, p. 5979-5986, 2007

• DOI for Effects on protease inhibition by modifying of helicase residues in hepatitis C virus nonstructural protein 3

Biomolecular Recognition of Glycosylated β3-Peptides by GalNAc Specific Lectins

Norgren, Anna S.; Geitmann, Matthis; Danielson, U. Helena; Arvidsson, Per I.

Part of Journal of Molecular Recognition, p. 132-138, 2007

• DOI for Biomolecular Recognition of Glycosylated β3-Peptides by GalNAc Specific Lectins

Additional level of information about complex interaction between non-nucleoside inhibitor and HIV-1 reverse transcriptase using biosensor-based thermodynamic analysis

Geitmann, Matthis; Danielson, U. Helena

Part of Bioorganic & Medicinal Chemistry, p. 7344-7354, 2007

• DOI for Additional level of information about complex interaction between non-nucleoside inhibitor and HIV-1 reverse transcriptase using biosensor-based thermodynamic analysis

Resistance profiling of hepatitis C virus protease inhibitors using full-length NS3

Dahl, Göran; Sandström, Anja; Åkerblom, Eva; Danielson, U. Helena

Part of Antiviral Therapy, p. 733-740, 2007

Detection of competitive enzyme inhibition with end point progress curve data

Gutierrez Arenas, Omar; Danielson, U. Helena

Part of Analytical Biochemistry, p. 11-19, 2006

• DOI for Detection of competitive enzyme inhibition with end point progress curve data

Biosensor-based screening and characterization of HIV-1 inhibitor interactions with Sap1, Sap2 and Sap3 from Candida albicans

Backman, Dan; Monod, Michel; Danielson, U. Helena

Part of Journal of Biomolecular Screening, p. 165-175, 2006

• DOI for Biosensor-based screening and characterization of HIV-1 inhibitor interactions with Sap1, Sap2 and Sap3 from Candida albicans

Interaction kinetic characterization of HIV-1 reverse transcriptase non-nucleoside inhibitor resistance

Geitmann, Matthis; Unge, Torsten; Danielson, U. Helena

Part of Journal of Medicinal Chemistry, p. 2375-87, 2006

• DOI for Interaction kinetic characterization of HIV-1 reverse transcriptase non-nucleoside inhibitor resistance

Characterization of Ca2+ interactions with matrix metallopeptidase-12: implications for matrix metallopeptidase regulation

Gossas, Thomas; Danielson, Helena

Part of Biochemical Journal, p. 393-398, 2006

• DOI for Characterization of Ca2+ interactions with matrix metallopeptidase-12: implications for matrix metallopeptidase regulation

Biosensor-based kinetic characterization of the interaction between HIV-1 reverse transcriptase and non-nucleoside inhibitors

Geitmann, Matthis; Unge, Torsten; Danielson, U. Helena

Part of Journal of Medicinal Chemistry, p. 2367-74, 2006

• DOI for Biosensor-based kinetic characterization of the interaction between HIV-1 reverse transcriptase and non-nucleoside inhibitors

Inhibition of viral proteases by Zingiberaceae extracts and flavones isolated from Kaempferia parviflora

Sookkongwaree, K; Geitmann, Matthis; Roengsumran, S; Petsom, A et al.

Part of Pharmazie, p. 717-721, 2006

Exploration of acyl sulfonamides as carboxylic acid replacements in protease inhibitors of the hepatitis C virus full-length NS3

Rönn, Robert; Sabnis, Yogesh A; Gossas, Thomas; Åkerblom, Eva et al.

Part of Bioorganic & Medicinal Chemistry, p. 544-559, 2006

• DOI for Exploration of acyl sulfonamides as carboxylic acid replacements in protease inhibitors of the hepatitis C virus full-length NS3

Sensitivity analysis and error structure of progress curves

Gutierrez Arenas, Omar; Danielson, U Helena

Part of Analytical Biochemistry, p. 1-10, 2006

• DOI for Sensitivity analysis and error structure of progress curves

Refolding of the full-length non-structural protein 3 of hepatitis C virus

Poliakov, Anton; Danielson, U. Helena

Part of Protein Expression and Purification, p. 298-305, 2005

• DOI for Refolding of the full-length non-structural protein 3 of hepatitis C virus

Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions

Cimitan, Samanta; Lindgren, Maria T.; Bertucci, Carlo; Danielson, U. Helena

Part of Journal of Medicinal Chemistry, p. 3536-46, 2005

• DOI for Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions

Studies of substrate-induced conformational changes in human cytomegalovirus protease using optical biosensor technology

Geitmann, Matthis; Danielson, U. Helena

Part of Analytical Biochemistry, p. 203-214, 2004

• DOI for Studies of substrate-induced conformational changes in human cytomegalovirus protease using optical biosensor technology

Optimisation of peptide-based inhibitors of full-length hepatitis C virus NS3 protease

Poliakov, Anton; Johansson, Anja; Åkerblom, Eva; Lindeberg, Gunnar et al.

Part of Antiviral Research, 2004

Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data

Shuman, Cynthia; Vrang, Lotta; Danielson, U. Helena

Part of Journal of Medicinal Chemistry, p. 5953-61, 2004

• DOI for Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data

Kinetic and thermodynamic characterization of HIV-1 protease inhibitors

Shuman, Cynthia F.; Hämäläinen, Markku; Danielson, U. Helena

Part of Journal of Molecular Recognition, p. 106-19, 2004

Structure-activity relationships for the selectivity of hepatitis C virus NS3 protease inhibitors

Poliakov, Anton; Johansson, Anja; Åkerblom, Eva; Oscarsson, Karin et al.

Part of Biochimica et Biophysica Acta, p. 51-59, 2004

• DOI for Structure-activity relationships for the selectivity of hepatitis C virus NS3 protease inhibitors

Refolding of a recombinant full-length non-structural (NS3) protein from hepatitis C virus by chromatographic procedures

Li, Ming; Poliakov, Anton; Danielson, U. Helena; Su, Zhiguo et al.

Part of Biotechnology letters, p. 1729-1734, 2003

• DOI for Refolding of a recombinant full-length non-structural (NS3) protein from hepatitis C virus by chromatographic procedures

Kinetic and mechanistic analysis of the association and dissociation of inhibitors interacting with secreted aspartic acid proteases 1 and 2 from Candida albicans

Backman, Dan; Danielson, U. Helena

Part of Biochimica et Biophysica Acta - Proteins and Proteomics, p. 184-195, 2003

• DOI for Kinetic and mechanistic analysis of the association and dissociation of inhibitors interacting with secreted aspartic acid proteases 1 and 2 from Candida albicans

Elucidation of HIV-1 protease resistance by characterization of interaction kinetics between inhibitors and enzyme variants

Shuman, Cynthia F.; Markgren, Per-Olof; Hämäläinen, Markku; Danielson, U. Helena

Part of Antiviral Research, p. 235-242, 2003

• DOI for Elucidation of HIV-1 protease resistance by characterization of interaction kinetics between inhibitors and enzyme variants

Optimization of P1-P3 groups in symmetric and asymmetric HIV-1 protease inhibitors

Andersson, Hans O.; Fridborg, Kerstin; Löwgren, Seved; Alterman, Mathias et al.

Part of European Journal of Biochemistry, p. 1746-1758, 2003

• DOI for Optimization of P1-P3 groups in symmetric and asymmetric HIV-1 protease inhibitors

Peptide-based inhibitors of hepatitis C virus full-length NS3 (protease-helicase/NTPase): model compounds towards small molecule inhibitors

Oscarsson, Karin; Poliakov, Anton; Oscarson, Stefan; Danielson, U. Helena et al.

Part of Bioorganic & Medicinal Chemistry, p. 2955-2963, 2003

• DOI for Peptide-based inhibitors of hepatitis C virus full-length NS3 (protease-helicase/NTPase): model compounds towards small molecule inhibitors

Acyl sulfonamides as potent protease inhibitors of the hepatitis C virus full-length NS3 (protease-helicase/NTPase): a comparative study of different C-terminals

Johansson, Anja; Poliakov, Anton; Åkerblom, Eva; Wiklund, Karin et al.

Part of Bioorganic & Medicinal Chemistry, p. 2551-2568, 2003

• DOI for Acyl sulfonamides as potent protease inhibitors of the hepatitis C virus full-length NS3 (protease-helicase/NTPase): a comparative study of different C-terminals

Analysis of the pH-dependencies of the association and dissociation kinetics of HIV-1 protease inhibitors

Gossas, Thomas; Danielson, U. Helena

Part of Journal of Molecular Recognition, p. 203-212, 2003

• DOI for Analysis of the pH-dependencies of the association and dissociation kinetics of HIV-1 protease inhibitors

Candida albicans secreted aspartic peptidase specificity: A chromogenic combinatorial approach

Beyer, B; Rubin, J; Johnson, J; Chung, A et al.

Part of Biopolymers, p. 310-P025, 2003

Peptide-based protease inhibitors of the hepatitis C virus full-length NS3 protein (protease-helicase/NTPase)

Johansson, Anja; Åkerblom, Eva; Poliakov, Anton; Lindeberg, Gunnar et al.

Part of Journal of Peptide Science, 2002

HIV-1 Vif-derived peptide inhibits drug-resistant HIV proteases

Blumenzweig, I; Baraz, L; Friedler, A; Danielson, U. Helena et al.

Part of Biochemical and Biophysical Research Communications - BBRC, p. 832-840, 2002

• DOI for HIV-1 Vif-derived peptide inhibits drug-resistant HIV proteases

Tetrapeptides as potent protease inhibitors of Hepatitis C Virus full-length NS3 (protease-helicase/NTPase)

Johansson, Anja; Poliakov, Anton; Åkerblom, Eva; Lindeberg, Gunnar et al.

Part of Bioorganic & Medicinal Chemistry, p. 3915-22, 2002

• DOI for Tetrapeptides as potent protease inhibitors of Hepatitis C Virus full-length NS3 (protease-helicase/NTPase)

Relationships between structure and interaction kinetics for HIV-1 protease inhibitors

Markgren, Per-Olof; Schaal, Wesley; Hämäläinen, Markku; Karlén, Anders et al.

Part of Journal of Medicinal Chemistry, p. 5430-5439, 2002

• DOI for Relationships between structure and interaction kinetics for HIV-1 protease inhibitors

Resistance profiles of cyclic and linear inhibitors of HIV-1 protease

Ahlsén, Göran; Hultén, Johan; Shuman, Cynthia; Poliakov, Anton et al.

Part of Antiviral Chemistry & Chemotherapy, p. 27-37, 2002

Expression and purification of recombinant full-length NS3 protease-helicase from a new variant of Hepatitis C virus

Poliakov, Anton; Hubatsch, Ina; Shuman, Cynthia F; Stenberg, Gun et al.

Part of Protein Expression and Purification, p. 363-371, 2002

• DOI for Expression and purification of recombinant full-length NS3 protease-helicase from a new variant of Hepatitis C virus

Inhibition of hepatitis C virus NS3 protease activity by product-based peptides is dependent on helicase domain

Johansson, Anja; Hubatsch, Ina; Åkerblom, Eva; Lindeberg, Gunnar et al.

Part of Bioorganic & Medicinal Chemistry Letters, p. 203-206, 2001

• DOI for Inhibition of hepatitis C virus NS3 protease activity by product-based peptides is dependent on helicase domain

Capture and analysis of low molecular weight ligands by surface plasmon resonance combined with mass spectrometry

Sönksen, C. P.; Roepstorff, P.; Markgren, Per-Olof; Danielson, U. Helena et al.

Part of European journal of mass spectrometry, p. 385-391, 2001

• DOI for Capture and analysis of low molecular weight ligands by surface plasmon resonance combined with mass spectrometry

Synthesis and comperative molecular field analysis (CoMFA) of symmetric and nonsymmetric cyclic sulfamide HIV-1 protease inhibitors

Schaal, Wesley; Karlsson, Anna; Ahlsén, Göran; Lindberg, Jimmy et al.

Part of Journal of Medicinal Chemistry, p. 155-169, 2001

• DOI for Synthesis and comperative molecular field analysis (CoMFA) of symmetric and nonsymmetric cyclic sulfamide HIV-1 protease inhibitors

P1/P1' modified HIV protease inhibitors as tools in two new sensitive surface plasmon resonance biosensor screening assays

Alterman, Mathias; Sjöbom, Hans; Säfsten, Pär; Markgren, Per-Olof et al.

Part of European Journal of Pharmaceutical Sciences, p. 203-212, 2001

• DOI for P1/P1' modified HIV protease inhibitors as tools in two new sensitive surface plasmon resonance biosensor screening assays

Determination of interaction kinetic constants for HIV-1 protease inhibitors using optical biosensor technology

Markgren, Per-Olof; Lindgren, Maria T.; Gertow, Karl; Karlsson, Robert et al.

Part of Analytical Biochemistry, p. 207-218, 2001

• DOI for Determination of interaction kinetic constants for HIV-1 protease inhibitors using optical biosensor technology

Characterization of a set of HIV-1 protease inhibitors using binding kinetics data from a biosensor-based screen

Hämäläinen, Markku D.; Markgren, Per-Olof; Schaal, Wesley; Karlén, Anders et al.

Part of Journal of Biomolecular Screening, p. 353-359, 2000

• DOI for Characterization of a set of HIV-1 protease inhibitors using binding kinetics data from a biosensor-based screen

Kinetic analysis of the interaction between HIV-1 protease and inhibitors using optical biosensor technology

Markgren, Per-Olof; Hämäläinen, Markku; Danielson, U. Helena

Part of Analytical Biochemistry, p. 71-78, 2000

• DOI for Kinetic analysis of the interaction between HIV-1 protease and inhibitors using optical biosensor technology

Probing the kinetic mechanism and coenzyme specificity of glutathione reductase from the cyanobacterium Anabaena PCC 7120 by redesign of the pyridine-nucleotide-binding site

Danielson, U. Helena; Jiang, Fanyi Y; Hansson, Lars O.; Mannervik, Bengt

Part of Biochemistry, p. 9254-9263, 1999

• DOI for Probing the kinetic mechanism and coenzyme specificity of glutathione reductase from the cyanobacterium Anabaena PCC 7120 by redesign of the pyridine-nucleotide-binding site

Inhibitors of the C(2)-symmetric HIV-1 protease: nonsymmetric binding of asymmetric cyclic sulfamide with ketoxime groups in the P2/P2' side chains

Hultén, Johan; Andersson, Hans O.; Schaal, Wesley; Danielson, U. Helena et al.

Part of Journal of Medicinal Chemistry, p. 4054-4061, 1999

• DOI for Inhibitors of the C(2)-symmetric HIV-1 protease: nonsymmetric binding of asymmetric cyclic sulfamide with ketoxime groups in the P2/P2' side chains

Design and fast synthesis of C-terminal duplicated potent C₂-symmetric P1/P1'-modified HIV-1 protease inhibitors

Alterman, Mathias; Andersson, Hans O.; Garg, Neeraj; Ahlsén, Göran et al.

Part of Journal of Medicinal Chemistry, p. 3835-3844, 1999

• DOI for Design and fast synthesis of C-terminal duplicated potent C₂-symmetric P1/P1'-modified HIV-1 protease inhibitors

Cyclic urea and sulfamide-based inhibitors of HIV-1 protease: Changes in binding mode upon modifications in the P1/P1 side chain

Bäckbro, Kristina; Andersson, Hans; Bonham, Nick M; Classon, Björn et al.

Part of Antiviral Research, 1998

Investigation of an allosteric site of HIV-1 proteinase involved in inhibition by Cu2+

Danielson, Helena; Lindgren, Maria T.; Markgren, Per-Olof; Nillroth, Ulrika

Part of Advances in Experimental Medicine and Biology, p. 99-103, 1998

Screening of compounds interacting with HIV-1 proteinase using optical biosensor technology

Markgren, Per-Olof; Hämäläinen, Markku; Danielson, U. Helena

Part of Analytical Biochemistry, p. 340-350, 1998

• DOI for Screening of compounds interacting with HIV-1 proteinase using optical biosensor technology

Cyclic 7-membered sulfamide HIV-1 protease inhibitors

Hultén, Johan; Schaal, Wesley; Unge, Torsten; Danielson, U Helena et al.

Part of Antiviral Research, 1998

HIV-1 protease inhibitors based on acyclic carbohydrates

Zuccarello, Guido; Bouzide, Abderrahim; Kvarnstrom, Ingemar; Niklasson, Gunilla et al.

Part of Journal of Organic Chemistry, p. 4898-4906, 1998

• DOI for HIV-1 protease inhibitors based on acyclic carbohydrates

Design and synthesis of new potent C2-symmetric HIV-1 protease inhibitors: Use of L-mannaric acid as a peptidomimetic scaffold

Alterman, Mathias; Björsne, Magnus; Mühlman, Anna; Classon, Björn et al.

Part of Journal of Medicinal Chemistry, p. 3782-3792, 1998

• DOI for Design and synthesis of new potent C2-symmetric HIV-1 protease inhibitors: Use of L-mannaric acid as a peptidomimetic scaffold

Development of a radiochemical cyclooxygenase-1 and 2 in vitro assay for identification of natural products as inhibitors of prostaglandin biosynthesis

Noreen, Ylva; Ringbom, Therese; Perera, Premila; Danielson, Helena et al.

Part of Journal of natural products (Print), p. 2-7, 1998

• DOI for Development of a radiochemical cyclooxygenase-1 and 2 in vitro assay for identification of natural products as inhibitors of prostaglandin biosynthesis

Synthesis of enantiomerically pure cis and trans 2-aminocyclopentanecarboxylic acids. Use of proline replacements in potential HIV-protease inhibitors

Nöteberg, Daniel; Brånalt, Jonas; Kvarnström, Ingemar; Classon, Björn et al.

Part of Tetrahedron, p. 7975-7984, 1997

• DOI for Synthesis of enantiomerically pure cis and trans 2-aminocyclopentanecarboxylic acids. Use of proline replacements in potential HIV-protease inhibitors

Cyclic HIV-1 protease inhibitors derived from mannitol: synthesis, inhibitory potencies, and computational predictions of binding affinities

Hultén, Johan; Bonham, Nicholas M; Nillroth, Ulrika; Hansson, Tomas et al.

Part of Journal of Medicinal Chemistry, p. 885-897, 1997

• DOI for Cyclic HIV-1 protease inhibitors derived from mannitol: synthesis, inhibitory potencies, and computational predictions of binding affinities

Human immunodeficiency virus type 1 proteinase resistance to symmetric cyclic urea inhibitor analogs

Nillroth, Ulrika; Vrang, Lotta; Markgren, Per-Olof; Hultén, Johan et al.

Part of Antimicrobial Agents and Chemotherapy, p. 2383-2388, 1997

A convenient synthesis of 1-(S)-[1'-(S)-(t-butyloxycarbonylamino)-2'-phenylethyl]oxirane: a useful building block in the synthesis of HIV protease inhibitors

Brånalt, J; Kvarnstrom, I; Classon, B; Samuelsson, B et al.

Part of Tetrahedron Letters, p. 3483-3486, 1997

• DOI for A convenient synthesis of 1-(S)-[1'-(S)-(t-butyloxycarbonylamino)-2'-phenylethyl]oxirane: a useful building block in the synthesis of HIV protease inhibitors

Synthesis of C-2 symmetric potential inhibitors of HIV-1 protease from D-mannitol

Niklasson, Gunilla; Kvarnström, Ingemar; Classon, Björn; Samuelsson, Bertil et al.

Part of Journal of carbohydrate chemistry, p. 555-569, 1996

• DOI for Synthesis of C-2 symmetric potential inhibitors of HIV-1 protease from D-mannitol

The use of 5'-phosphate derivatives of nucleoside analogs as inhibitors of HIV-1 replication

Nillroth, Ulrika; Vrang, Lotta; Ahlsén, Göran; Besidsky, Y et al.

Part of Antiviral Chemistry & Chemotherapy, p. 50-64, 1995

Specific interaction between HIV-1 proteinase and 5'-phosphate peptidomimetic derivatives of nucleoside analogues

Nillroth, Ulrika; Besidsky, Yosef; Classon, Björn; Chattopahyaya, Jyoti et al.

Part of Drug design and discovery, p. 43-54, 1995

Isothiocyanates as substrates for human glutathione transferases: structure-activity studies

Kolm, Rüdiger H.; Danielson, U Helena; Zhang, Y.uesheng; Talalay, Paul et al.

Part of Biochemical Journal, p. 453-459, 1995

Engineering of a metal coordinating site into human glutathione transferase M1-1 based on immobilized metal ion affinity chromatography of homologous rat enzymes

Chaga, Grigoriy; Widersten, Mikael; Andersson, Lennart; Porath, Jerker et al.

Part of Protein Engineering, p. 1115-1119, 1994

• DOI for Engineering of a metal coordinating site into human glutathione transferase M1-1 based on immobilized metal ion affinity chromatography of homologous rat enzymes

High-yield purification of HIV-1 proteinase expressed by a synthetic gene in Escherichia coli

Goobar, Laura; Danielson, U Helena; Brodin, Peter; Grundström, Thomas et al.

Part of Protein Expression and Purification, p. 15-23, 1991

Cooperative effect of fructose bisphosphate and glyceraldehyde-3-phosphate dehydrogenase on aldolase action

Neuzil, Jiri; Danielson, Helena; Welch, G Rickey; Ovádi, Judit

Part of Biochimica et Biophysica Acta, p. 307-312, 1990

• DOI for Cooperative effect of fructose bisphosphate and glyceraldehyde-3-phosphate dehydrogenase on aldolase action

Proteolytic cleavage of microtubule-associated proteins by retroviral proteinases

Wallin, Margareta; Deinum, Johanna; Goobar, Laura; Danielson, U Helena

Part of Journal of General Virology, p. 1985-1991, 1990

• DOI for Proteolytic cleavage of microtubule-associated proteins by retroviral proteinases

Relaxed thiol substrate specificity of glutathione transferase effected by a non-substrate glutathione derivative

Principato, Giovanni B; Danielson, U Helena; Mannervik, Bengt

Part of FEBS Letters, p. 155-158, 1988

• DOI for Relaxed thiol substrate specificity of glutathione transferase effected by a non-substrate glutathione derivative

Paradoxical inhibition of rat glutathione transferase 4-4 by indomethacin explained by substrate-inhibitor-enzyme complexes in a random-order sequential mechanism

Danielson, U Helena; Mannervik, Bengt

Part of Biochemical Journal, p. 705-711, 1988

Glutathione transferases - structure and catalytic activity

Mannervik, Bengt; Danielson, U Helena

Part of Crc Critical Reviews in Biochemistry, p. 283-337, 1988

Expression of class-pi glutathione transferase in drug-resistant human-melanoma cells

Mannervik, Bengt; Castro, Victor M; Danielson, U Helena; Platz, A et al.

Part of Proceedings of the American Association of Cancer Research, p. 5-5, 1987

Structure-activity relationships of 4-hydroxyalkenals in the conjugation catalysed by mammalian glutathione transferases

Danielson, U Helena; Esterbauer, Hermann; Mannervik, Bengt

Part of Biochemical Journal, p. 707-713, 1987

Purification of major basic glutathione transferase isoenzymes from rat liver by use of affinity chromatography and fast protein liquid chromatofocusing

Ålin, Per; Jensson, Helgi; Guthenberg, Claes; Danielson, U Helena et al.

Part of Analytical Biochemistry, p. 313-320, 1985

• DOI for Purification of major basic glutathione transferase isoenzymes from rat liver by use of affinity chromatography and fast protein liquid chromatofocusing

4-Hydroxyalk-2-enals are substrates for glutathione transferase

Ålin, Per; Danielson, U. Helena; Mannervik, Bengt

Part of FEBS Letters, p. 267-270, 1985

• DOI for 4-Hydroxyalk-2-enals are substrates for glutathione transferase

Kinetic independence of the subunits of cytosolic glutathione transferase from the rat

Danielson, U Helena; Mannervik, Bengt

Part of Biochemical Journal, p. 263-267, 1985

STRUCTURAL DATA AND ENZYMATIC-PROPERTIES DEFINING 3 CLASSES OF MAMMALIAN CYTOSOLIC GLUTATHIONE TRANSFERASE

Mannervik, Bengt; Ålin, P; Danielson, U Helena; Guthenberg, C et al.

Part of Federation proceedings, p. 471-471, 1985

Inhibition of HIV-1 protease by Cu2+ occurs by a reversible allosteric mechanism involving His-69

Lindgren, Maria T.; Markgren, Per-Olof; Nillroth, Ulrika; Danielson, U. Helena

Thermodynamic analysis of non-nucleoside inhibitor binding to HIV-1 reverse transcriptase

Geitmann, Matthis; Danielson, U. Helena

The high affinity of hydroxamate-based MMP-12 inhibitors is due to an inherently slow dissociation rate of the enzyme-inhibitor complex

Gossas, Thomas; Nordström, Helena; Wallberg, Hans; Danielson, Helena

Let There Be Light!

Raykova, Doroteya; Koos, Bjoern; Asplund, Anna; Gelleri, Marton et al.

Part of Proteomes, 2016

• DOI for Let There Be Light!
• Download full text (pdf) of Let There Be Light!

Biophysics in drug discovery: impact, challenges and opportunities

Renaud, Jean-Paul; Chung, Chun-wa; Danielson, U. Helena; Egner, Ursula et al.

Part of Nature reviews. Drug discovery, p. 679-698, 2016

• DOI for Biophysics in drug discovery: impact, challenges and opportunities

Molecular Interaction Analysis for Discovery of Drugs Targeting Enzymes and for Resolving Biological Function

Danielson, U. Helena

Part of Multifaceted Roles Of Crystallography In Modern Drug Discovery, p. 223-240, 2015

• DOI for Molecular Interaction Analysis for Discovery of Drugs Targeting Enzymes and for Resolving Biological Function

MIV-170: A novel NNRTI exhibiting tight binding to HIV-1 reverse transcriptase (RT)

Elinder, Malin; Danielson, Helena; Unge, Torsten; VanHam, Guido et al.

2008

• DOI for MIV-170: A novel NNRTI exhibiting tight binding to HIV-1 reverse transcriptase (RT)

Investigation of beta-amino acids as building blocks in hepatitis c virus NS3 protease inhibitors

Nurbo, Johanna; Dahl, G; Danielson, U Helena; Sandström, Anja

2007

Novel C-terminal functionalities in hepatitis C virus NS3 protease inhibitors

Rönn, Robert; Gossas, T; Sabnis, Y A; Åkerblom, E et al.

2005

Optimisation of peptide-based inhibitors of full-length hepatitis C virus NS3 protease

Poliakov, Anton; Johansson, A; Åkerblom, E; Lindeberg, G et al.

2004

Identification of complexities in HIV-1 protease - ligand interactions using biosensor technology

Lindgren, Maria T.; Shuman, Cynthia F.; Hämäläinen, Markku; Karlsson, R. et al.

Discovery of the subsite specificity of Candida albicans Sap1 and Sap2 and the design of potent peptidomimetic inhibitors

Rubin, Jamie E.; Beyer, Bret B.; Chung, Alfred Y.; Johnson, Jodie V. et al.

Substrate specificity and pH dependence of secreted aspartic proteases Sap1, Sap2 and Sap3 from Candida albicans

Backman, Dan; Danielson, U. Helena

Initial evaluation of biotinylated bilayer disks as model membranes for biosensor analyses

Lundquist, Anna; Hansen, Soren B.; Nordström, Helena; Danielson, Helena et al.

Kinetic, mechanistic and chemodynamic characterisation of non-nucleoside hepatitis C virus NS5B polymerase inhibitors using SPR biosensor technology

Geitmann, Matthis; Dahl, Göran; Lohmann, Volker; Paeshuyse, Jan et al.

Kinetic characterization of HCV NS3 inhibitors using an SPR biosensor

Geitmann, Matthis; Dahl, Göran; Danielson, Helena

Efficient protein binders for the C-reactive protein from a designed chemically modified peptide library

T. Tegler, Lotta; Nonglaton, Guillaume; Büttner, Frank; Karin, Caldwell et al.

Target Engagement-Mediated Amplification for Monitoring Drug-Target Interactions in Situ

Al-Amin, Rasel A.; Johansson, Lars; Landegren, Nils; Löf, Liza et al.

Multiplexed biosensor-based screening and structural assessment of fragments targeting KLHL12 and KLHL20

Myers, Nadine; Koehler, Konrad; Diallo, Marcel; Xiong, Ruisheng et al.

Design of a Stapled Peptide Targeting KLHL20^Kelch: A Computational and Biosensor-based Approach

Myers, Nadine; Cadot, Marie Elodie Helene; Varga, Julia; Diallo, Marcel et al.

Deciphering the RNA recognition by Musashi-1 to design protein and RNA mutants for in vitro and in vivo applications

Pérez-Ràfols, Anna; Pérez-Ropero, Guillermo; Cerofolini, Linda; Sperotto, Luca et al.

• DOI for Deciphering the RNA recognition by Musashi-1 to design protein and RNA mutants for in vitro and in vivo applications

Exploring real-time interaction analysis to monitor CD44 expression modulation in cancer cells by inhibiting Musashi-1 interactions with RNA

Pérez-Ropero, Guillermo; Ortstad, Nathalie; Nestor, Marika; Danielson, Helena et al.