Per Artursson
Professor i läkemedelsformulering 92 vid Institutionen för farmaci; Läkemedelsformulering
- Telefon:
- 018-471 44 71
- E-post:
- per.artursson@uu.se
- Besöksadress:
- Biomedicinskt Centrum BMC, Husargatan 3
- Postadress:
- Box 580
751 23 UPPSALA
Ladda ned kontaktuppgifter för Per Artursson vid Institutionen för farmaci; Läkemedelsformulering
- Akademiska meriter:
- FarmD, docent i galenisk farmaci
- ORCID:
- 0000-0002-3708-7395
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Biografi
Per Artursson is a professor in Dosage Form Design at the Department of Pharmacy, Uppsala University, Sweden, where he heads the Drug Delivery research team. He is also Director of the Uppsala University drug optimization and pharmaceutical profiling platform within Science for Life Laboratories. His research aims at understanding drug absorption, distribution, metabolism and elimination (ADME) at the molecular and cellular level in order to deliver drugs more effectively via the oral route. He also investigates the influence of drug transporting proteins, drug metabolizing enzymes and cellular and sub-cellular drug uptake, distribution and elimination. For this purpose, both 2D and 3D cell cultures are used in combination with state-of-the-art omics and bioinformatics. Both traditional small drug molecules and biopharmaceuticals such as peptide and antisense oligonucleotides are investigated. He has published more than 200 research articles and 50 reviews and book chapters, is highly cited and has received several international awards for his research.
Website: https://www.farmaci.uu.se/research/drugdelivery/research/artursson/
Forskning
Current research is focused on mechanisms of drug transport, pharmaceutical profiling and the prediction of ADMET properties. Most cited papers deals with absorption prediction. Per currently leads a group, including a collaborative profiling platform (UDOPP) of 20+ staff. UDOPP is a platform for drug optimization and pharmaceutical profiling at the Dep. of Pharmacy, Uppsala University and participates in two national infrastructures within SciLifeLab (CBCS and DDD-Platform).
Publikationer
Urval av publikationer
- Improved predictions of time-dependent drug-drug interactions by determination of cytosolic drug concentrations (2019)
- A simple approach for restoration of differentiation and function in cryopreserved human hepatocytes (2019)
- Intracellular Drug Bioavailability (2018)
- Prediction of intracellular exposure bridges the gap between target- and cell-based drug discovery (2017)
- Intracellular drug bioavailability (2017)
- Variability in Mass Spectrometry-based Quantification of Clinically Relevant Drug Transporters and Drug Metabolizing Enzymes (2017)
- CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil (2016)
- Oral absorption of peptides and nanoparticles across the human intestine (2016)
- Structural and conformational determinants of macrocycle cell permeability (2016)
- Complete Knockout of Endogenous Mdr1 (Abcb1) in MDCK Cells by CRISPR-Cas9 (2016)
Senaste publikationer
- Expression of intestinal drug transporter proteins and metabolic enzymes in neonatal and pediatric patients (2024)
- Global 13C tracing and metabolic flux analysis of intact human liver tissue ex vivo (2024)
- Digoxin Pharmacokinetics in Patients with Obesity Before and After a Gastric Bypass or a Strict Diet Compared with Normal Weight Individuals (2024)
- In silico and biological analyses of missense variants of the human biliary efflux transporter ABCC2 (2024)
- OCT1 (SLC22A1) transporter kinetics and regulation in primary human hepatocyte 3D spheroids (2024)
Alla publikationer
Artiklar
- Expression of intestinal drug transporter proteins and metabolic enzymes in neonatal and pediatric patients (2024)
- Global 13C tracing and metabolic flux analysis of intact human liver tissue ex vivo (2024)
- Digoxin Pharmacokinetics in Patients with Obesity Before and After a Gastric Bypass or a Strict Diet Compared with Normal Weight Individuals (2024)
- In silico and biological analyses of missense variants of the human biliary efflux transporter ABCC2 (2024)
- OCT1 (SLC22A1) transporter kinetics and regulation in primary human hepatocyte 3D spheroids (2024)
- The choice of ultra-low attachment plates impacts primary human and primary canine hepatocyte spheroid formation, phenotypes, and function (2024)
- Illuminating the function of the orphan transporter, SLC22A10, in humans and other primates (2024)
- Loss of heterozygosity of CYP2D6 enhances the sensitivity of hepatocellular carcinomas to talazoparib (2024)
- Epithelial and microbial determinants of colonic drug distribution (2023)
- Proteome deconvolution of liver biopsies reveals hepatic cell composition as an important marker of fibrosis (2023)
- Neither Gastric Bypass Surgery Nor Diet-Induced Weight-Loss Affect OATP1B1 Activity as Measured by Rosuvastatin Oral Clearance (2023)
- Monitoring drug–target interactions through target engagement-mediated amplification on arrays and in situ (2022)
- High Throughput Screening of a Prescription Drug Library for Inhibitors of Organic Cation Transporter 3, OCT3 (2022)
- The impact of inflammation on the expression of drug transporters and metabolic enzymes in colonic tissue from ulcerative colitis patients (2022)
- Inhibition of prolyl oligopeptidase (2022)
- Impact of type 2 diabetes on in vivo activities and protein expressions of cytochrome P450 in patients with obesity (2022)
- Correlations between 4 beta-hydroxycholesterol and hepatic and intestinal CYP3A4 (2022)
- Short- and long-term effects of body weight, calorie restriction and gastric bypass on CYP1A2, CYP2C19 and CYP2C9 activity (2022)
- Short- and long-term effects of body weight loss following calorie restriction and gastric bypass on CYP3A-activity (2022)
- Professor Margareta Hammarlund-Udenaes - Humbled Scientist Shaping Modern Neuropharmacokinetics (2022)
- Barriers to the Intestinal Absorption of Four Insulin-Loaded Arginine-Rich Nanoparticles in Human and Rat (2022)
- Hepatic Expression of the Na+-Taurocholate Cotransporting Polypeptide Is Independent from Genetic Variation (2022)
- Drug Disposition Protein Quantification in Matched Human Jejunum and Liver From Donors With Obesity (2022)
- Proteomics-Informed Identification of Luminal Targets For In Situ Diagnosis of Inflammatory Bowel Disease (2021)
- Newly developed dual topoisomerase inhibitor P8-D6 is highly active in ovarian cancer (2021)
- Conditions for maintenance of hepatocyte differentiation and function in 3D cultures (2021)
- Common and mutation specific phenotypes of KRAS and BRAF mutations in colorectal cancer cells revealed by integrative -omics analysis (2021)
- Getting a grip with kirigami (2021)
- Current challenges and future perspectives in oral absorption research (2021)
- Expanding the Efflux In Vitro Assay Toolbox (2021)
- Influence of Proteome Profiles and Intracellular Drug Exposure on Differences in CYP Activity in Donor-Matched Human Liver Microsomes and Hepatocytes (2021)
- Proteomics‐Informed Prediction of Rosuvastatin Plasma Profiles in Patients with a Wide Range of Body Weight (2021)
- Hepatocyte size fractionation allows dissection of human liver zonation (2021)
- Acamprosate Is a Substrate of the Human Organic Anion Transporter (OAT) 1 without OAT3 Inhibitory Properties (2020)
- A new opening for orally taken peptide drugs (2020)
- The Critical Role of Passive Permeability in Designing Successful Drugs (2020)
- A Comparative Analysis of Cytochrome P450 Activities in Paired Liver and Small Intestinal Samples from Patients with Obesity (2020)
- Exploiting loss of heterozygosity for allele-selective colorectal cancer chemotherapy (2020)
- Global variability analysis of mRNA and protein concentrations across and within human tissues (2020)
- Cell-type-resolved proteomic analysis of the human liver (2020)
- Experimental approaches to understand intracellular based drug bioavailability (2019)
- Improved predictions of time-dependent drug-drug interactions by determination of cytosolic drug concentrations (2019)
- Comprehensive drug uptake transporter proteomics and metabolomic profiling of human liver (2019)
- Toward a Consensus on Applying Quantitative Liquid Chromatography-Tandem Mass Spectrometry Proteomics in Translational Pharmacology Research (2019)
- Impact of Intracellular Concentrations on Metabolic Drug-Drug Interaction Studies (2019)
- A Cell-Free Approach Based on Phospholipid Characterization for Determination of the Cell Specific Unbound Drug Fraction (f(u,cell)) (2019)
- Multiple-Enzyme-Digestion Strategy Improves Accuracy and Sensitivity of Label- and Standard-Free Absolute Quantification to a Level That Is Achievable by Analysis with Stable Isotope-Labeled Standard Spiking (2019)
- Image-based quantification of cell debris as a measure of apoptosis (2019)
- A simple approach for restoration of differentiation and function in cryopreserved human hepatocytes (2019)
- Anti-Rift Valley fever virus activity in vitro, pre-clinical pharmacokinetics and oral bioavailability of benzavir-2, a broad-acting antiviral compound (2018)
- CRISPR-Cas9 (2018)
- Linking FOXO3, NCOA3, and TCF7L2 to Ras pathway phenotypes through a genome-wide forward genetic screen in human colorectal cancer cells (2018)
- The stimulation of GLP-1 secretion and delivery of GLP-1 agonists &ITvia&IT nanostructured lipid carriers (2018)
- Intracellular Drug Bioavailability (2018)
- Small-molecule inhibitor of OGG1 suppresses proinflammatory gene expression and inflammation (2018)
- Direct Quantification of Cytochromes P450 and Drug Transporters-A Rapid, Targeted Mass Spectrometry-Based Immunoassay Panel for Tissues and Cell Culture Lysates (2018)
- A human intestinal M-cell-like model for investigating particle, antigen and microorganism translocation (2017)
- A CRISPR-Cas9 Generated MDCK Cell Line Expressing Human MDR1 Without Endogenous Canine MDR1 (cABCB1) (2017)
- Structure-metabolism-relationships in the microsomal clearance of piperazin-1-ylpyridazines (2017)
- Piperazin-1-ylpyridazine Derivatives Are a Novel Class of Human dCTP Pyrophosphatase 1 Inhibitors (2017)
- Identification of Triazolothiadiazoles as Potent Inhibitors of the dCTP Pyrophosphatase 1 (2017)
- Prediction of intracellular exposure bridges the gap between target- and cell-based drug discovery (2017)
- Intracellular drug bioavailability (2017)
- Substrate and method dependent inhibition of three ABC-transporters (MDR1, BCRP, and MRP2) (2017)
- Variability in Mass Spectrometry-based Quantification of Clinically Relevant Drug Transporters and Drug Metabolizing Enzymes (2017)
- CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil (2016)
- New cell-based approaches for better predictions of drug transport and cellular drug exposure (2016)
- Validation and development of MTH1 inhibitors for treatment of cancer (2016)
- Aryl Sulfonamide Inhibitors of Insulin-Regulated Aminopeptidase Enhance Spine Density in Primary Hippocampal Neuron Cultures (2016)
- Thiazolino 2-Pyridone Amide Inhibitors of Chlamydia trachomatis Infectivity (2016)
- Direct Measurement of Intracellular Compound Concentration by RapidFire Mass Spectrometry Offers Insights into Cell Permeability (2016)
- Development of MS- based immunoassays for Cytochrome P450 and transporter quantification (2016)
- Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1 (2016)
- Oral absorption of peptides and nanoparticles across the human intestine (2016)
- Impact of drug transporters on intracellular unbound drug concentrations (2016)
- The Need for Speed-Kinetic Limits of Drug Transporters (2016)
- The Pro-inflammatory Cytokine Interleukin-6 Regulates Nanoparticle Transport Across Model Follicle-Associated Epithelium Cells (2016)
- Structural and conformational determinants of macrocycle cell permeability (2016)
- A Tribute to Ronald T. Borchardt-Teacher, Mentor, Scientist, Colleague, Leader, Friend, and Family Man (2016)
- Complete Knockout of Endogenous Mdr1 (Abcb1) in MDCK Cells by CRISPR-Cas9 (2016)
- Global proteome changes in liver tissue 6 weeks after FOLFOX treatment of colorectal cancer liver metastases (2016)
- Mechanistic Modeling of Pitavastatin Disposition in Sandwich-Cultured Human Hepatocytes (2016)
- Mechanistic modeling of hepatic pitavastatin disposition (2016)
- Comparative proteome analysis of human liver tissue and isolated hepatocytes (2016)
- Protein quantification of human hepatic drug transporters and metabolizing enzymes (2016)
- In-depth quantitative analysis and comparison of the human hepatocyte and hepatoma cell line HepG2 proteomes (2016)
- Subcellular fractionation of human liver reveals limits in global proteomic quantification from isolated fractions (2016)
- To attach or not to attach (2016)
- The Proteome of Filter-Grown Caco-2 Cells With a Focus on Proteins Involved in Drug Disposition (2016)
- Breaking the intestinal barrier to deliver drugs (2015)
- Preclinical Characterization of Acyl Sulfonimidamides (2015)
- Structure-activity relationships for lipoprotein lipase agonists that lower plasma triglycerides in vivo (2015)
- Global Membrane Protein Analysis Of The Human Liver (2015)
- Addendum to 'Quantifying the impact of transporters on cellular drug permeability' (2015)
- Quantifying the impact of transporters on cellular drug permeability. (2015)
- Comparative Proteomic Analysis of Human Liver Tissue and Isolated Hepatocytes with a Focus on Proteins Determining Drug Exposure (2015)
- Early pharmaceutical profiling to predict oral drug absorption (2014)
- Exploration and pharmacokinetic profiling of phenylalanine based carbamates as novel substance p 1-7 analogues (2014)
- MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool (2014)
- Achiral Pyrazinone-Based Inhibitors of the Hepatitis C Virus NS3 Protease and Drug-Resistant Variants with Elongated Substituents Directed Toward the S2 Pocket (2014)
- Vulnerability of Glioblastoma Cells to Catastrophic Vacuolization and Death Induced by a Small Molecule (2014)
- Vinylated linear P2 pyrimidinyloxyphenylglycine based inhibitors of the HCV NS3/4A protease and corresponding macrocycles (2014)
- Novel Peptidomimetic Hepatitis C Virus NS3/4A Protease Inhibitors Spanning the P2–P1′ Region (2014)
- A High-Throughput Cell-Based Method to Predict the Unbound Drug Fraction in the Brain (2014)
- Impact of Stereospecific Intramolecular Hydrogen Bonding on Cell Permeability and Physicochemical Properties (2014)
- Passive Lipoidal Diffusion and Carrier-Mediated Cell Uptake Are Both Important Mechanisms of Membrane Permeation in Drug Disposition (2014)
- Hepatic Uptake of Atorvastatin (2014)
- Constrained H-Phe-Phe-NH2 Analogues With High Affinity to the Substance P 1-7 Binding Site and With Improved Metabolic Stability and Cell Permeability (2013)
- Population pharmacokinetic modeling and deconvolution of enantioselective absorption of eflornithine in the rat (2013)
- Rapid Measurement of Intracellular Unbound Drug Concentrations (2013)
- Combined in Vitro-in Vivo Approach To Assess the Hepatobiliary Disposition of a Novel Oral Thrombin Inhibitor (2013)
- Computational Prospecting for Drug-Transporter Interactions (2013)
- An Integrated in Vitro Model for Simultaneous Assessment of Drug Uptake, Metabolism, and Efflux (2013)
- Cadmium Transport in a Model of Neonatal Intestinal Cells Correlates to MRP1 and Not DMT1 or FPN1 (2013)
- Early Identification of Clinically Relevant Drug Interactions with the Human Bile Salt Export Pump (BSEP; ABCB11) (2013)
- The value of selected in vitro and in silico methods to predict acute oral toxicity in a regulatory context (2013)
- Optimizing Solubility and Permeability of a Biopharmaceutics Classification System (BCS) Class 4 Antibiotic Drug Using Lipophilic Fragments Disturbing the Crystal Lattice (2013)
- Caco-2 monolayers in experimental and theoretical predictions of drug transport (2012)
- Evidence-based approach to assess passive diffusion and carrier-mediated drug transport (2012)
- mRNA expression of drug-transporting proteins along the human intestine and comparison with expression in Caco-2 cells (2012)
- In Vitro and In Silico Strategies to Identify OATP1B1 Inhibitors and Predict Clinical Drug-Drug Interactions (2012)
- Classification of Inhibitors of Hepatic Organic Anion Transporting Polypeptides (OATPs) (2012)
- Genotype-dependent effects of inhibitors of the organic cation transporter, OCT1: (2011)
- Structural Features Determining the Intestinal Epithelial Permeability and Efflux of Novel HIV-1 Protease Inhibitors (2011)
- In vitro ADMET and physicochemical investigations of poly-N-methylated peptides designed to inhibit Aβ aggregation (2010)
- Uptake mechanism of ochratoxin A and citrinin through human liver (2010)
- Interaction of 140 orally administered drugs with the liver-specific organic anion transporter OATP1B1 (SLCO1B1) (2010)
- Specific and general inhibitors of the three hepatic organic anion transporters OATP1B1 (SLCO1B1), OATP1B3 (SLCO1B3) and OATP2B1 (SLCO2B1) (2010)
- Integrated cell models for prediction of drug transport and drug metabolism in the human hepatocyte (2010)
- Paracellular porosity and pore size of the human intestinal epithelium in tissue and cell culture models (2010)
- Molecular design of chitosan gene delivery systems with an optimized balance between polyplex stability and polyplex unpacking (2010)
- Coexistence of passive and carrier-mediated processes in drug transport (2010)
- A Modified Physiological BCS for Prediction of Intestinal Absorption in Drug Discovery (2010)
- Endogenous Gene and Protein Expression of Drug Transporting Proteins in Cell Lines Routinely used in Drug Discovery Programs (2009)
- Hepatitis C virus NS3 protease inhibitors (2009)
- Identification of novel specific and general inhibitors of the three major human ATP-binding cassette transporters P-gp, BCRP and MRP2 among registered drugs (2009)
- Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1 (2008)
- Comparison of drug transporter gene expression and functionality in Caco-2 cells from 10 different laboratories (2008)
- Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2) (2008)
- Yersinia pseudotuberculosis induces transcytosis of nanoparticles across human intestinal villus epithelium via invasin-dependent macropinocytosis (2008)
- Tailoring of chitosans for gene delivery (2008)
- Molecular characteristics for solid-state limited solubility (2008)
- Efflux transporters in ulcerative colitis (2007)
- Expression of thirty-six drug transporter genes in human intestine, liver, kidney, and organotypic cell lines (2007)
- Beta- and gamma-di- and tripeptides as potential substrates for the oligopeptide transporter hPepT1 (2007)
- Determination of drug permeability and prediction of drug absorption in Caco-2 monolayers (2007)
- A Global Drug Inhibition Pattern for the Human ATP-Binding Cassette Transporter Breast Cancer Resistance Protein (ABCG2) (2007)
- Advantages and disadvantages of using bovine serum albumin and/or Cremophor EL as extracellular additives during transport studies of lipophilic compounds across Caco-2 monolayers (2007)
- Regional levels of drug transporters along the human intestinal tract (2006)
- Identification of Cell Adhesion Molecules in the Human Follicle-Associated Epithelium That Improve Nanoparticle Uptake into the Peyer's Patches (2006)
- Targeted gene delivery with trisaccharide-substituted chitosan oligomers in vitro and after lung administration in vivo (2006)
- Characterization of antigen and bacterial transport in the follicle-associated epithelium of human ileum. (2006)
- Impact of extracellular protein binding on passive and active drug transport across Caco-2 cells. (2006)
- Gene expression profiles in mouse lung tissue after administration of two cationic polymers used for nonviral gene delivery (2006)
- Predominant contribution of organic anion transporting polypeptide OATP-B (OATP2B1) to apical uptake of estrone-3-sulfate by human intestinal Caco-2 cells. (2006)
- Contribution of solid-state properties to the aqueous solubility of drugs. (2006)
- Characterization of Surface-Modified Nanoparticles for in Vivo Biointeraction. A Sedimentation Field Flow Fractionation Study (2005)
- Caco-2 permeability of weakly basic drugs predicted with the Double-Sink PAMPA pK flux a method. (2005)
- Transport of nanoparticles across an in vitro model of the human intestinal follicle associated epithelium. (2005)
- Improvement of absorption enhancing effects of n-dodecyl-beta-D-maltopyranoside by its colon-specific delivery using chitosan microspheres. (2005)
- Orally active antiviral tripeptide glycyl-prolyl-glycinamide is activated by CD26 (dipeptidyl peptidase IV) before transport across the intestinal epithelium. (2005)
- A miniaturized nebulization catheter for improved gene delivery to the mouse lung. (2005)
- Exploring the role of different drug transport routes in permeability screening. (2005)
- X-ray yield and selectively excited X-ray emission spectra of atenolol and nadolol. (2005)
- Ketobemidone is a substrate for cytochrome P4502C9 and 3A4, but not for P-glycoprotein. (2005)
- Accuracy of calculated pH-dependent aqueous drug solubility. (2004)
- Global and local computational models for aqueous solubility prediction of drug-like molecules. (2004)
- Association between the number of coadministered P-glycoprotein inhibitors and serum digoxin levels in patients on therapeutic drug monitoring (2004)
- Improved chitosan-mediated gene delivery based on easily dissociated chitosan polyplexes of highly defined chitosan oligomers. (2004)
- Contribution of the paracellular route to the pH-dependent epithelial permeability to cationic drugs. (2004)
- Exploring the quantitative relationship between the level of MDR1 transcript, protein and function using digoxin as a marker ofMDR1-dependent drug efflux activity. (2004)
- Theoretical predictions of drug absorption in drug discovery and development (2002)
- Target Engagement-Mediated Amplification for Monitoring Drug-Target Interactions in Situ
- A Naked Host Cell Membrane is the Optimal Surface for Targeting by Salmonella
- Transporter kinetics of the organic cation transporter OCT1 in 3D cultured primary human hepatocytes
- Proteomics-informed deconvolution of different cell types in human liver tissue
- Non-genetic and epigenetic factors contribute to inter-individualvariability of the hepatic bile acid and drug transporter NTCP
- Effects of obesity and weight loss on global protein expression in human liver and jejunum
- Global expression variability of proteins across and within human tissues
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