Jyoti Chattopadhyaya
Professor emeritus at Department of Cell and Molecular Biology; Molecular Biology
- Mobile phone:
- +46 70 425 02 43
- E-mail:
- jyoti.chattopadhyaya@icm.uu.se
- Visiting address:
- Husargatan 3
752 37 Uppsala - Postal address:
- Box 596
751 24 Uppsala
Professor emeritus at Department of Cell and Molecular Biology; Uppsala RNA Research Centre - URRC
- Mobile phone:
- +46 70 425 02 43
- Visiting address:
- Husargatan 3
752 37 Uppsala - Postal address:
- Box 596
751 24 Uppsala
More information is available to staff who log in.
Short presentation
Research focuses on (a) design of gene (RNA)-directed therapeutics based on Antisense, Small interfering RNA (siRNA) and micro-RNA, in which the translation of the RNA specific to a gene is selectively inhibited, (b) Physical and structural chemistry of DNA and RNA foldings,(c) design and synthesis of drug against resistant bacteria. Synthetic organic chemistry of heterocycles and carbohydrates is utilized to design mimics to model biological functions and/or transition state of RNA and DNA.
Keywords
- antisense technology
- bioorganic chemistry
- chemical biology
- dna
- dnazyme
- nucleic acids analogs
- rna
- rna interference
- rnase h
- sirna
Biography
Prof Jyoti Chattopadhyaya is a Senior Professor at the Department of Cell & Molecular Biology, University of Uppsala. During his career at Uppsala University he has been working as a Chair of Bioorganic Chemistry as well as Program Director of the Chemical Biology Program at the Department of Cell & Molecular Biology at the University of Uppsala, Sweden. The first program of Bioorganic Chemistry has been established by him in Sweden back in 1980, and since than he has supervised research of 30 Ph.D students, promoted 4 Docents [Dr. Neil Balgobin (1985), Dr. Marek Kwiatkowski (1996), Dr. András Földesi (2004), Dr. Oleksandr Plashkevych (2018)] and has reported high level Bioorganic chemistry research, resulting in over 420 publications in various peer-reviewed Journals (for details see http://www.boc.uu.se). Prof. Chattopadhyaya acknowledges significant contributions to this ground breaking research by his students,co-workers and postdocs whos list (possibly incomplete) is shown below:
Dr. Christelle Dupouy (France, 2007-)
Dr. Liu Yi (China, 2007-)
Dr. Jianfeng Xu (China, 2007-)
Dr. Badgujar Naresh (India, 2007-)
Dr. Andaloussi Mounir (Morocco, 2007)
Dr. Mariappan Mirumari (India, 2005-2006)
Dr. Isaksson Johan (Sweden, 2005)
Dr. Naus Petr (Chez Republic, 2004-2006)
Dr. Bogucka Malgorzata (Poland, 2004-2006)
Dr. Plashkevych Oleksandr (Ukraina, 2000)
Dr. Acharaya Parag (India, 2004)
Dr. Amirkhanov Nariman (Russia, 2003)
Dr. Kumar Pradeep (India, 2005)
Dr. Földesi Andras (Hungary, 2003)
Dr. Ossipov Dimitri ( Russia, 2002)
Dr. Zamaratski Edouard (Russia, 2000)
Dr. Maltseva Tatiana (Russia, 2000)
Dr. Nitin Puri (India, 1999)
Dr. Thibaudeau Christophe (France, 1999)
Dr. Agback Peter (Sweden, 1998)
Dr. Dr. Wen Pei (China, 1998)
Dr. Densov Alexei (Russia, 1998)
Dr. Maini Mitu (India, 1998)
Dr. Guibin Ma (China, 1997)
Dr. Dubey Krishna (India, 1997)
Dr. Hossain Nafizal (India, 1997)
Dr. Kumar Anil (India, 1997)
Dr. Luyten Ingrid (Sweden, 1996)
Dr. Yamakag Schunichi (Japan, 1996)
Dr. Forgó Péter (Hungary, 1995)
Dr. Kolupaev Sergei (Russia, 1995)
Dr. Plavec Janez (Slovenia, 1995)
Dr. Sandström Corine (France, 1995)
Dr. Vasiliev Andrei (Russia, 1995)
Dr. Zhen Xi (China, 1994)
Dr. Nilson Frans Peder (Sweden 1994)
Dr. Paptchikhine Alexander (Russia, 1994)
Dr. Rong Jianhui (China, 1994)
Dr. Rousse Bertrand (France, 1993)
Dr. Sandström Anders (Sweden, 1993)
Dr. Sund Christian (Finland, 1993)
Dr. Tong Weimin (China, 1993)
Dr. Garg Neeraj (India, 1993)
Dr. Poselt Peter (Australia, 1993)
Dr. Viswanadham Garimella (India, 1992)
Dr. Hovinen Jari (Finland, 1992)
Dr. Koole Leo (The Netherlands, 1991)
Dr. Nyilas Agnes (Hungary, 1991)
Dr. Besidsky Yevgeny (Russia, 1991)
Dr. Fedorov Ivan (Russia, 1991)
Dr. Forfar Isabelle (Sweden, 1991)
Dr. Gebru Tesfai (Ethiopia, 1991)
Dr. Wu Jinchang (China, 1990)
Dr. Jaseja Mahesh (India, 1989)
Dr. Katjiteo Ehry (South Africa, 1989)
Dr. Vial Jean-Marc (France, 1989)
Dr. Xiaoguang Luo (China, 1988)
Dr. Zhou Xiaoxiong (China, 1988)
Dr. Bazin Hervé, (France, 1988)
Dr. Pathak Tanmaya (India, 1988)
Dr. Bekiroglu Somer (Turkey, 1987)
Dr. Welch Christopher (UK, 1986)
Dr. Heikkilä Jarmo (Finland, 1985)
Dr. Juntunen Seppo (Finland, 1985)
Dr. Remauld Gerald (France, 1985)
Dr. Gioelli Carlo (Italy, 1984)
Dr. Grouiller Annie (France, 1984)
Dr. Kwiatkowski Marek (Hungary, 1984)
Dr. Sundström Birgitta (Sweden, 1982)
Dr. Balgobin Neil (UK, 1982)
Dr. Bhattacharya Birenda (India, 1982)
Dr. Björkman Sven (Sweden, 1982)
Dr Staffan Josephsson (Sweden) 1979-1982
Dr. Catherine Petit (France, 2002-2004)
Dr. Mrinal Kundu (India, 1998-9)
Former Ph.D. students:
2012
Conformationally Constrained Oligonucleotides for RNA Targeting . Li Qing ISSN 1651-6214; 948 http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-179069 ISBN: 978-91-554-8414-9
2010
Conformationally Constrained Nucleic Acids as Potential RNA Targeting Therapeutics. Zhou Chuanzheng. ISSN 1651-6214; ISBN 978-91-554-7728-8; urn:nbn:se:uu:diva-114136
2008
Conformationally Constrained Nucleosides, Nucleotides, and Oligonucleotides. Design, Synthesis and Properties. Dmytro Honcharenko. ISSN 1651-6214; ISBN 978-91-554-7219-1
2006
Some Aspects of Physicochemical Properties of DNA and RNA. Sandipta Acharya. ISSN 1651-6214; ISBN 91-554-6518-8.
2005
Studies on Nucleic Acids - Structure and Dynamics Johan Isaksson. ISSN 1651-6214, ISBN 91-554-6293-6
2004
Chemically Modified Oligonucleotides: Synthesis, Physicochemical and Biochemical Properties of their Duplexes with DNA and RNA P.I. Pradeepkumar. ISSN 1104-232X, ISBN 91-554-5957-9
2003
Studies on the Non-covalent Interactions (Stereoelectronics, Stacking and Hydrogen Bonding) in the Self-assembly of DNA and RNA . Parag Acharya. ISSN 1104-232X, ISBN 91-554-5821-1
2002
Aspects of Antisense and Antigene of Oligonucleotides Tethered to Intercallators. Dimitri Ossipov. ISBN 91-554-5365-1
2000
Some Aspects of Nucleic Acid Chemistry. Edouard Zamaratski. ISSN 1104-232X, ISBN 91-554-4868-2
1999
Stereoelectronic Effects in Nucleosides and Nucleotides. Christophe Thibaudeau. ISBN 91-554-4365-6
1999
Studies on Nucleic Acids Chemistry. Nitin Puri. ISBN 91-554-4348-6
1996
Synthetic and Structural (NMR) Studies on DNA and RNA. Shun-Ichi Yamakage. ISBN 91-554-3821-0
1995
Studies on Stereoelectronic Effects in Nucleosides and Nucleotides. Janez Plavec. ISBN 91-554-3553-X
1994
Some Recent Developments in Nucleoside Chemistry. Nafizal Hossain. ISBN 91-554-3346-4
1994
Some New Aspects of Nucleoside Chemistry. Zhen Xi. ISBN 91-554-3292-1
1993
Conformational Analysis of Ribonucleic acids (RNA) by NMR Spectroscopy. Peter Agback. ISBN 91-554-3127-5
1993
Studies on Nucleic Acid Chemistry. Andras Földesi. ISBN 91-554-3075-9
1993
Studies on Nucleoside Chemistry. Weimin Tong. ISBN 91-554-3048-1
1992
Studies on Ribonucleic Acid (RNA) Chemistry. Christian Sund. ISBN 91-554-2984-X
1991
Structural Studies on Nucleosides and Nucleotides by Nuclear Magnetic Resonance (NMR) Spectroscopy. Corine Glemarec. ISBN 91-554-2803-7
1990
Studies on Nucleoside Chemistry. Jin-Chang Wu. ISBN 91-554 -2655-7
1989
Synthesis, Separation, and Structure of Ribonucleic Acids and a Toxic Cyclic Peptide. Anders Sandström. ISBN 91-554-2476-7
1989
Studies on Nucleoside and Nucleotide Chemistry. Jean-Marc Vial. ISBN 91-554-2450-3
1988
Studies on Nucleic Acid Chemistry. Xiao-Xiong Zhou. ISBN 91-554-2291-8
1988
Studies on Nucleoside and Nucleotide Chemistry. Tanmaya Pathak. ISBN 91-554-2288-8
1988
Studies on Nucleoside and Nucleotide Chemistry. Agnes Nyilas. ISBN 91-554-2263-2
1988
Studies on Nucleoside Chemistry. Herve Bazin. ISBN 91-554-2073-7
1986
Studies on Nucleoside and Nucleotide Chemistry. Christopher John Welch. ISBN 91-554-1902-X
1985
Studies on the Chemistry of Nucleosides and Nucleotides. Jarmo Heikkilä. ISBN 91-554-1736-1
1984
Studies on Oligoribonucleotide (RNA) Chemistry. Marek Kwiatkowski. ISBN 91-554-1499-0
1982
Studies on Oligodeoxyribonucleotide (DNA) Chemistry. Neil Balgobin. ISBN 91-7146-230-9
Research
Prof. Chattopadhyaya is leading multidisciplinary research at the interface of the frontiers of Chemistry/Structure/Enzymology. His research focuses on (a) design of gene (RNA)-directed therapeutics based on Antisense, Small interfering RNA (siRNA) and micro-RNA, in which the translation of the RNA specific to a gene is selectively inhibited, (b) Physical and structural chemistry of DNA and RNA foldings, (c) design and synthesis of drug against resistant bacteria including hospital infections – MDR and XDR Tuberculosis, Staphylococcus aureus (both methicillin and penicillin resistant), vancomycin resitant Enterococcus and pseudomonas. In these research he employs synthetic organic chemistry of heterocycles and carbohydrates to design mimics to model biological functions and/or the transition state. The major achievements include (a) successful design of new conformationally locked chemically modified nucleo(s)tides, to self-organize oligo-DNA and –RNA molecules to minimize the contribution of entropic energy penalty to the free-energy, (b) to improve the stability and cellular delivery of siRNAs and antisense oligonucleotides; (c) development of new synthetic methodologies for RNA, DNA, and their modified analogs as potential DNA/RNA-directed therapeutics (siRNAs, antisense, triplexing agent, aptamers, etc), including synthetic and physico-chemical aspects of monosaccharide, heterocyclic, and phospholipid, phosphorylating and protecting group chemistry. (d) development of novel active antibiotic lead compounds against multiple drug resistant and extensive drug resistant strains of tuberculosis and hospital pathogens; (e) determination of NMR solution structures of RNA to understand RNA folding-dependent function of non-coding RNAs with emphasis on the role of microRNA, siRNAs and RNA catalyst; (e) elucidation of bioorganic chemical mechanisms using synthetic physical and structural (NMR) chemistry to model transition state or the intermediate of biochemical reactions, such as splicing, RNA catalysis, and RNA-RNA-ligand or RNA-DNA-ligand interactions; (f) development of new chemical tools for RNA, carbohydrate and peptide synthesis to understand molecular details of how structure of molecules dictate function.
Some key references to his work (for details see www.boc.uu.se):
S. Dutta, N. Bhaduri, N. Rastogi, S. G. Chandel, J. Vandavasi, R. S. Upadhayaya, and J. Chattopadhyaya. The carba-LNA modified siRNAs targeting HIV-1 TAR region downregulates HIV-1 replication successfully with Enhanced Potency. MedChemComm, Hot article, 2, 206-216 (2011) http://blogs.rsc.org/md/
C. Zhou, O. Plashkevych, J. Chattopadhyaya. Double Sugar and Phosphate Backbone-constrained Nucleotides: Synthesis, Structure, Stability and Their Incorporation into Oligodeoxynucleotides. Journal of Organic Chemistry, Featured article; 74 (9), 3248–3265 (2009); http://pubs.acs.org/galleyproof/AP-ufiZFcydQcUwd8JbtJ5w
P. Srivastava, J. Barman, W. Pathmasiri, O. Plashkevych, M. Wenska and J. Chattopadhyaya The Five- and Six-Membered Conformationally Locked 2',4'-Carbocyclic ribo-Thymidine: Synthesis, Structure and Biochemical Studies. Journal of the American Chemical Society, 129 (26), 8362 – 8379 (2007).
O. P. Varghese, J. Barman, W. Pathmasiri, O. Plashkevych, D. Honcharenko, and J. Chattopadhyaya Conformationally Constrained 2'-N,4'-C-Ethylene-Bridged Thymidine (Aza-ENA-T): Synthesis, Structure, Physical, and Biochemical Studies of Aza-ENA-T-Modified Oligonucleotides. Journal of the American Chemical Society, 128 (47), 15173–15187 (2006).
Currently active particularly successful research areas and groups/networks, in a national or international perspective led by Prof. Chattopadhyaya
● Strong and fruitful collaboration with the infectious diseases, chemical biology and systems biology groups involved in Linnéa sponsored RNA research Consortium concentrating on “Design and Synthesis of Site-specific Bifunctional Ligands Targeted to RNA hairpin loops depending upon their Stem-Loop-size and Sequence-context” funded by the Swedish Research Council (Natural and Technical Research), “Strategic Funding of Uppsala RNA Research Center (URRC) (VR diary No 349-2006-267). Within this project we design and synthesis unique specific Ruthenium based organometalic compounds as well as metallopeptides that are aimed to bind to the sequence-specific stem-loop motif of pre-micro-RNA structure with a far reaching aim to modulate the biosynthesis, and consequently regulating the cellular function of micro-RNA.
● RNA research which is holding very high international level as recognized by the referees of 2010 VR application (VR diary No 2010-4991). This research is focused on three main goals: 1) specific RNA- and chemically modified RNA- synthesis, 2) structure and conformational determination of RNA and 3) studies of RNA function.
● Prof. Chattopadhyaya has been nominated as a Research Professor by the Dept of Science & Technology, India Gov since 2009. In that capacity, he helps to organize strategic research on biotechnology of CSIR/India in an international perspective.
● Prof. Chattopadhyaya is an honorary professor at Jilin University in China, and nominated honorary professor at Nankai University in China.
● Prof.Chattopadhyaya collaborates and actively helped to organize research with 26 scientists at the Institute of Molecular Medicine at Pune/India to devise therapeutics against resistant infectious diseases.
● He has conceived and demonstrated the concept of Stereoelectronic effects in DNA and RNA and their structural and functional implications, which has found wide applications and acceptance internationally (http://www.boc.uu.se/boc14www/publications/Stereoelectronic_effect.pdf ).
● He has conceived and demonstrated the concept of The Uppsala NMR-window concept to simplify the NMR spectra of large DNA/RNA, which is used worldwide.
● He has conceived and demonstrated the design principles for the synthesis of new conformationally-constrained nucleic acids and their enzymology to develop effective antisense oligos and siRNAs to enhance blood serum stability and facilitate delivery.
● He has conceived and demonstrated the design principles for the Synthesis and modifications of aza-modified conformationally restricted nucleotides as fluorescent DNA probes.
● He has conceived and demonstrated that the single-strand DNA and RNA conformation in the purine-rich single-strand oligo-DNA and –RNA are well pre-organized to helical form - not random coils as it was originally thought. The structure of the self-assembled single-strand oligo-DNA and -RNA is very much reminiscent of their double-stranded counterparts. The set of papers published from Uppsala on self-assembled single-strand oligo-DNA and -RNA has brought about a paradigm shift after Watson-Crick basepaired double helix as the origin of helical structure of DNA duplex
● He and his coworkers have shown that all internucleotidic phosphodiester bonds in RNA are not chemically equivalent, and their reactivity depends upon the sequence-context governed by specific intrinsic electrostatic interactions.
● He and his coworkers have developed solid-phase oligo-RNA synthesis utilizing our new 2'-O-TEM protecting group.
● He and his cowrkers have designed, synthesized, performed biological evaluation and molecular modeling studies of novel quinoline, triazole, urea and thiourea derivatives against drug resistant Mycobacterium tuberculosis.
List of present grants (exchange rate €1 = 9.41725 SEK)
- EU FP 6th, “RIGHT, RNA Interference Technology as Human Therapeutic Tool” 2005, 2006, 2007, 2008 : 200,000 €/year UU project number: 15250900, EU RIGHT contract number: 005276
- Swedish Research Council (Medical Research), “New Nucleolitically Stable Antisense Oligonucleotides Which Recruits RNase H and cleave target RNA” 2008, 2009, 2010. 85,000 €/year (ID number: 521-2007-2400) UU project number: 15250806, VR Contract ID K2008-66X-14224-07-3
- Swedish Research Council (Natural and Technical Research VR) ”Synthesis, Structure and Function of RNA” 2008, 2009, 2010. 117,000 €/year (ID number: 621-2007-4466), UU project number: 15250807, VR Contract ID 70446601
- Swedish Research Council (Natural and Technical Research VR) ” Synthesis, Structure and Function of RNA” 2008 53,000 € /year (ID number: 621-2007-4466) UU project number: 15250808, VR Contract ID: 70446602
- Swedish Research Council (Natural and Technical Research VR “Strategic Funding of Uppsala RNA Research Center (Urrc) 70,000 €/year 2006-07-01, 2008, 2009,2010 (ID number 349-2006-267) UU project number 15250805, VR contract ID: 60026701
- EU FP7, “NATT” (New Approaches to target Tuberculosis) 2008, 2009, 2010 ( tot €402000) 117,000 €/year
- Swedish Research Council (Natural and Technical Research VR) ”Synthesis, Structure and Function of RNA” 2011, 2012, 2013: 117,000 €/year (ID number: 621-2011-4466)
- Swedish Research Council (Medical Research), “New Nucleolitically Stable Antisense Oligonucleotides Which Recruits RNase H and cleave target RNA” 2011, 2012, 2013, 2014: 85,000 €/year (ID number: 521-2011-2400)
- Swedish Research Council (Natural and Technical Research VR “Strategic Funding of Uppsala RNA Research Center (Urrc) 70,000 €/year 2011, 2012 (ID number 349-2006-267)
- Swedish Research Council, Grant for organizing conference “Development of drugs against resistant forms of tuberculosis and other infectious diseases" at the Biomedical Center, Uppsala University. 9600 €, 2011
The complete list of 420 publications can be found following the link:
http://www.boc.uu.se/boc14www/res_proj/List_of_publications.pdf
ISI Web of knowledge Citation Report: Results found: 350; Sum of the Times Cited: 6111; Sum of Times Cited without self-citations: 4243; Average Citations per item: 17.46; H-index: 36
Highlights of 30-Years of Bioogranic Chemistry research at Uppsala University can be found following the link: http://www.boc.uu.se/boc14www/publications/survey_isbn.pdf
Publications
Selection of publications
- C2 '-F Stereoconfiguration As a Puckering Switch for Base Stacking at the Dinucleotide Level (2018)
- Synthetic siRNA targeting human papillomavirus 16 E6 (2018)
- How RNase HI (Escherichia coli) promoted site-selective hydrolysis works on RNA in duplex with carba-LNA and LNA substituted antisense strands in an antisense strategy context? (2017)
- A Minute Amount of S-Puckered Sugars Is Sufficient for (6-4) Photoproduct Formation at the Dinucleotide Level (2015)
- Distal Two-Bond versus Three-Bond Electronegative Oxo-Substituent Effect Controls the Kinetics and Thermodynamics of the Conversion of a C-Nitroso Function to the Corresponding Oxime in the Conformationally Locked Pentofuranose (Bicyclo[2.2.1]heptane) System (2014)
- New antiprotozoal agents (2013)
- New parasite inhibitors encompassing novel conformationally-locked 5 '-acyl sulfamoyl adenosines (2012)
- Steric Effects in the Tuning of the Diastereoselectivity of the Intramolecular Free-Radical Cyclization to an Olefin As Exemplified through the Synthesis of a Carba-Pentofuranose Scaffold (2012)
- Unusual strain-releasing nucleophilic rearrangement of a bicyclo[2.2.1]heptane system to a cyclohexenyl derivative (2012)
- Intramolecular Free-Radical Cyclization Reactions on Pentose Sugars for the Synthesis of Carba-LNA and Carba-ENA and the Application of Their Modified Oligonucleotides as Potential RNA Targeted Therapeutics (2012)
- Carba-LNA modified siRNAs targeting HIV-1 TAR region downregulate HIV-1 replication successfully with enhanced potency (2011)
- The R-diastereomer of 6 '-O-toluoyl-carba-LNA modification in the core region of siRNA leads to 24-times improved RNA silencing potency against the HIV-1 compared to its S-counterpart (2011)
- Allele-selective inhibition of ataxin-3 (ATX3) expression by antisense oligomers and duplex RNAs (2011)
- Molecular Structure of the Core-Modified siRNA Duplexes Containing Diastereomeric Pair of [C6′(R)-OH]- versus [C6′(S)-OH]-carba-LNAs Suggests a Model for RNAi Action (2011)
- Carba-LNA-5MeC/A/G/T Modified Oligos Show Nucleobase-Specific Modulation of 3′-Exonuclease Activity, Thermodynamic Stability, RNA Selectivity, and RNase H Elicitation (2011)
- A large-scale chemical modification screen identifies design rules to generate siRNAs with high activity, high stability and low toxicity (2009)
- High-quality oligo-RNA synthesis using the new 2′-O-TEM protecting group by selectively quenching the addition of p-tolyl vinyl sulphone to exocyclic amino functions (2007)
- Non-identical electronic characters of the internucleotidic phosphates in RNA modulate the chemical reactivity of the phosphodiester bonds. (2006)
- Interactions of drugs and an oligonucleotide with charged membranes analyzed by immobilized liposome chromatography (2006)
- Electrostatic Cross-modulation of the Pseudoaromatic Character in Single Stranded RNA by Nearest-neighbor interactions (2005)
- 2'/3'-O-peptidyl Adenosine as a General Base Catalyst of its Own External Peptidyl Transfer: Implications for the Ribosome Catalytic Mechanism. (2005)
- A uniform mechanism correlating dangling-end stabilization and stacking geometry. (2005)
- Oxetane locked thymidine in the Dickerson-Drew dodecamer causes local base pairing distortions (2005)
- Measurement of nucleobase pKa values in model mononucleotides shows RNA-RNA duplexes to be more stable than DNA-DNA duplexes. (2004)
- Significant pKa perturbation of nucleobases is an intrinsic property of the sequence context in DNA and RNA. (2004)
- Book Review on "Highlights in Bioorganic Chemistry" (2004)
- Modified Nucleosides and Nucleotides and Their Use Thereof. (2004)
- Synthesis of 2'-2H1-Ribonucleosides (2004)
- Single-stranded adenine-rich DNA and RNA retain structural characteristics of their respective double-stranded conformations and show directional differences in stacking pattern. (2004)
- Oxetane modified, conformationally constrained, antisense oligodeoxyribonucleotides function efficiently as gene silencing molecules. (2004)
- Synthesis, physicochemical and biochemical studies of 1',2'-oxetane constrained adenosine and guanosine modified oligonucleotides, and their comparison with those of the corresponding cytidine and thymidine analogues. (2004)
- Human deoxycytidine kinase as a deoxyribonucleoside phosphorylase. (2004)
- Tandem electrostatic effect from the first to the third aglycon in the trimeric RNA owing to the nearest-neighbor interaction. (2003)
- A repertoire of pyridinium-phenyl-methyl cross-talk through a cascade of intramolecular electrostatic interactions. (2003)
- The pK(a) of the internucleotidic 2'-hydroxyl group in diribonucleoside (3'-->5') monophosphates. (2003)
- Studies towards the large scale chemical synthesis of the precursors of ribonucleosides-3',4',5',5''-2H4 and -2',3',4',5',5''-2H5. (2003)
- Studies on the Stereoselective Synthesis of Deuterated- Ribose Derivatives (2003)
- Antisense oligonuclotides with oxetane-constrained cytidine enhance heteroduplex stability, and elicit satisfactory RNase H response as well as showing improved resistance to both exo and endonucleases. (2003)
- The Hydrogen Bonding and Hydration of 2'-OH in Adenosine and Adenosine 3'-ethylphosphate. (2002)
- Experimental Evidences Unequivocally Prove the Role of Stereoelectronics as One of the Major Forces Responsible for the Self-assembly of DNA and RNA. (2002)
- Cross-modulation of physicochemical character of aglycones in dinucleoside (3'-->5') monophosphates by the nearest neighbor interaction in the stacked state. (2002)
- The RNase H Affinity and Cleavage of the target RNA in the Antisense-RNA Hybrid Duplexes Containing various 3’-Tethered Substituents in the Antisense Strand. (2002)
- Kinetic Analysis of the RNA Cleavage of the oxetane modified Antisense-RNA Hybrid Duplex by RNase H. (2002)
- An electrochemical probe of DNA stacking in an antisense oligonucleotide containing a C3'-endo-locked sugar. (2002)
- Synthesis of the DNA-[Ru(tpy)(dppz)(CH(3)CN)](2+) conjugates and their photo cross-linking studies with the complementary DNA strand. (2002)
- Do we understand the molecular nature of antisense oligo/RNA hybrid duplex recognition by RNase H? (2001)
- Synthesis of [Ru(phen)(2)dppz](2+)-tethered oligo-DNA and studies on the metallointercalation mode into the DNA duplex (2001)
- The strength of the 3 '-gauche effect dictates the structure of 3 '-O-anthraniloyladenosine and its 5 '-phosphate, two analogues of the 3 '-end of aminoacyl-tRNA (1999)
- MCR .3. Multicomponent reactions and their libraries, a new type of organic chemistry of the isocyanides and phosphorus derivatives. (1997)
- 2',3'-DIDEOXY-3'-C,2'-N-[(3R,5R)-5-ETHOXYCARBONYL-2-METHYL-1,2-ISOXAZOLIDINE]-RIBOTHYMIDINE (1995)
- The use of 5'-phosphate derivatives of nucleoside analogs as inhibitors of HIV-1 replication (1995)
Recent publications
- C2 '-F Stereoconfiguration As a Puckering Switch for Base Stacking at the Dinucleotide Level (2018)
- Synthetic siRNA targeting human papillomavirus 16 E6 (2018)
- How RNase HI (Escherichia coli) promoted site-selective hydrolysis works on RNA in duplex with carba-LNA and LNA substituted antisense strands in an antisense strategy context? (2017)
- A Minute Amount of S-Puckered Sugars Is Sufficient for (6-4) Photoproduct Formation at the Dinucleotide Level (2015)
- Distal Two-Bond versus Three-Bond Electronegative Oxo-Substituent Effect Controls the Kinetics and Thermodynamics of the Conversion of a C-Nitroso Function to the Corresponding Oxime in the Conformationally Locked Pentofuranose (Bicyclo[2.2.1]heptane) System (2014)
All publications
Articles
- C2 '-F Stereoconfiguration As a Puckering Switch for Base Stacking at the Dinucleotide Level (2018)
- Synthetic siRNA targeting human papillomavirus 16 E6 (2018)
- How RNase HI (Escherichia coli) promoted site-selective hydrolysis works on RNA in duplex with carba-LNA and LNA substituted antisense strands in an antisense strategy context? (2017)
- A Minute Amount of S-Puckered Sugars Is Sufficient for (6-4) Photoproduct Formation at the Dinucleotide Level (2015)
- Distal Two-Bond versus Three-Bond Electronegative Oxo-Substituent Effect Controls the Kinetics and Thermodynamics of the Conversion of a C-Nitroso Function to the Corresponding Oxime in the Conformationally Locked Pentofuranose (Bicyclo[2.2.1]heptane) System (2014)
- New antiprotozoal agents (2013)
- New parasite inhibitors encompassing novel conformationally-locked 5 '-acyl sulfamoyl adenosines (2012)
- Steric Effects in the Tuning of the Diastereoselectivity of the Intramolecular Free-Radical Cyclization to an Olefin As Exemplified through the Synthesis of a Carba-Pentofuranose Scaffold (2012)
- Unusual strain-releasing nucleophilic rearrangement of a bicyclo[2.2.1]heptane system to a cyclohexenyl derivative (2012)
- Design and Divergent Synthesis of Aza Nucleosides from a Chiral Imino Sugar (2012)
- Intramolecular Free-Radical Cyclization Reactions on Pentose Sugars for the Synthesis of Carba-LNA and Carba-ENA and the Application of Their Modified Oligonucleotides as Potential RNA Targeted Therapeutics (2012)
- Carba-LNA modified siRNAs targeting HIV-1 TAR region downregulate HIV-1 replication successfully with enhanced potency (2011)
- The R-diastereomer of 6 '-O-toluoyl-carba-LNA modification in the core region of siRNA leads to 24-times improved RNA silencing potency against the HIV-1 compared to its S-counterpart (2011)
- Allele-selective inhibition of ataxin-3 (ATX3) expression by antisense oligomers and duplex RNAs (2011)
- Molecular Structure of the Core-Modified siRNA Duplexes Containing Diastereomeric Pair of [C6′(R)-OH]- versus [C6′(S)-OH]-carba-LNAs Suggests a Model for RNAi Action (2011)
- Synthesis and antimycobacterial activity of prodrugs of indeno[2,1-c]quinoline derivatives (2011)
- Carba-LNA-5MeC/A/G/T Modified Oligos Show Nucleobase-Specific Modulation of 3′-Exonuclease Activity, Thermodynamic Stability, RNA Selectivity, and RNase H Elicitation (2011)
- Free-Radical Ring Closure to Conformationally Locked alpha-L-Carba-LNAs and Synthesis of Their Oligos (2010)
- Synthesis and structure of azole-fused indeno[2,1-c]quinolines and their anti-mycobacterial properties (2010)
- Why Carba-LNA-Modified Oligonucleotides Show Considerably Improved 3 '-Exonuclease Stability Compared to That of the LNA Modified or the Native Counterparts (2010)
- A large-scale chemical modification screen identifies design rules to generate siRNAs with high activity, high stability and low toxicity (2009)
- Design, synthesis and biological evaluation of novel triazole, urea and thiourea derivatives of quinoline against Mycobacterium tuberculosis (2009)
- Comparison of the RNase H Cleavage Kinetics and Blood Serum Stability of the North-Conformationally Constrained and 2‘-Alkoxy Modified Oligonucleotides (2007)
- Chemical and Structural Implications of 1‘,2‘- versus 2‘,4‘- Conformational Constraints in the Sugar Moiety of Modified Thymine Nucleosides (2007)
- Five- and Six-Membered Conformationally Locked 2‘,4‘-Carbocyclic ribo-Thymidines (2007)
- 2-(4-Tolylsulfonyl)ethoxymethyl (TEM)-a new 2'-OH protecting group for solid-supported RNA synthesis (2007)
- High-quality oligo-RNA synthesis using the new 2′-O-TEM protecting group by selectively quenching the addition of p-tolyl vinyl sulphone to exocyclic amino functions (2007)
- Non-identical electronic characters of the internucleotidic phosphates in RNA modulate the chemical reactivity of the phosphodiester bonds. (2006)
- Interactions of drugs and an oligonucleotide with charged membranes analyzed by immobilized liposome chromatography (2006)
- Electrostatic Cross-modulation of the Pseudoaromatic Character in Single Stranded RNA by Nearest-neighbor interactions (2005)
- 2'/3'-O-peptidyl Adenosine as a General Base Catalyst of its Own External Peptidyl Transfer: Implications for the Ribosome Catalytic Mechanism. (2005)
- A uniform mechanism correlating dangling-end stabilization and stacking geometry. (2005)
- Oxetane locked thymidine in the Dickerson-Drew dodecamer causes local base pairing distortions (2005)
- Measurement of nucleobase pKa values in model mononucleotides shows RNA-RNA duplexes to be more stable than DNA-DNA duplexes. (2004)
- Significant pKa perturbation of nucleobases is an intrinsic property of the sequence context in DNA and RNA. (2004)
- Book Review on "Highlights in Bioorganic Chemistry" (2004)
- Synthesis of 2'-2H1-Ribonucleosides (2004)
- Single-stranded adenine-rich DNA and RNA retain structural characteristics of their respective double-stranded conformations and show directional differences in stacking pattern. (2004)
- Oxetane modified, conformationally constrained, antisense oligodeoxyribonucleotides function efficiently as gene silencing molecules. (2004)
- Synthesis, physicochemical and biochemical studies of 1',2'-oxetane constrained adenosine and guanosine modified oligonucleotides, and their comparison with those of the corresponding cytidine and thymidine analogues. (2004)
- Human deoxycytidine kinase as a deoxyribonucleoside phosphorylase. (2004)
- Tandem electrostatic effect from the first to the third aglycon in the trimeric RNA owing to the nearest-neighbor interaction. (2003)
- A repertoire of pyridinium-phenyl-methyl cross-talk through a cascade of intramolecular electrostatic interactions. (2003)
- The pK(a) of the internucleotidic 2'-hydroxyl group in diribonucleoside (3'-->5') monophosphates. (2003)
- Studies towards the large scale chemical synthesis of the precursors of ribonucleosides-3',4',5',5''-2H4 and -2',3',4',5',5''-2H5. (2003)
- Studies on the Stereoselective Synthesis of Deuterated- Ribose Derivatives (2003)
- Antisense oligonuclotides with oxetane-constrained cytidine enhance heteroduplex stability, and elicit satisfactory RNase H response as well as showing improved resistance to both exo and endonucleases. (2003)
- The Hydrogen Bonding and Hydration of 2'-OH in Adenosine and Adenosine 3'-ethylphosphate. (2002)
- Experimental Evidences Unequivocally Prove the Role of Stereoelectronics as One of the Major Forces Responsible for the Self-assembly of DNA and RNA. (2002)
- Cross-modulation of physicochemical character of aglycones in dinucleoside (3'-->5') monophosphates by the nearest neighbor interaction in the stacked state. (2002)
- The RNase H Affinity and Cleavage of the target RNA in the Antisense-RNA Hybrid Duplexes Containing various 3’-Tethered Substituents in the Antisense Strand. (2002)
- Kinetic Analysis of the RNA Cleavage of the oxetane modified Antisense-RNA Hybrid Duplex by RNase H. (2002)
- An electrochemical probe of DNA stacking in an antisense oligonucleotide containing a C3'-endo-locked sugar. (2002)
- Synthesis of the DNA-[Ru(tpy)(dppz)(CH(3)CN)](2+) conjugates and their photo cross-linking studies with the complementary DNA strand. (2002)
- Do we understand the molecular nature of antisense oligo/RNA hybrid duplex recognition by RNase H? (2001)
- Synthesis of [Ru(phen)(2)dppz](2+)-tethered oligo-DNA and studies on the metallointercalation mode into the DNA duplex (2001)
- The strength of the 3 '-gauche effect dictates the structure of 3 '-O-anthraniloyladenosine and its 5 '-phosphate, two analogues of the 3 '-end of aminoacyl-tRNA (1999)
- MCR .3. Multicomponent reactions and their libraries, a new type of organic chemistry of the isocyanides and phosphorus derivatives. (1997)
- 2',3'-DIDEOXY-3'-C,2'-N-[(3R,5R)-5-ETHOXYCARBONYL-2-METHYL-1,2-ISOXAZOLIDINE]-RIBOTHYMIDINE (1995)
- The use of 5'-phosphate derivatives of nucleoside analogs as inhibitors of HIV-1 replication (1995)