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Tomas Cihlar

Research Profile

Chemicals & Drugs

Physiology

Viral Drug Resistance

Anatomy

Genes & Molecular Sequences

Molecular Structure

Living Beings

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Publications

TOP 3
Christian R Frey; Wanchi Fung; Romas Geleziunas; Bin Han; Magdeleine Hung; Xiaohong Liu; Ghislain Opdenakker; Robert Snoeck; Ivan Votruba; Graciela Andrei; Carina Cannizzaro; Pierre Fiten; Tomas Cihlar
Mutations in Adenosine Deaminase-like (ADAL) Protein Confer Resistance to the Antiproliferative Agents N6-Cyclopropyl-PMEDAP and GS-9219.
Kirsten M Stray; Luong Tsai; Lianhong Xu; Christian Callebaut; Bärbel Glass; Hans-Georg Kräusslich; Barbara Müller; Tomas Cihlar
Mutations in multiple domains of Gag drive the emergence of in vitro resistance to the phosphonate-containing HIV-1 protease inhibitor GS-8374.
Aurelie Bourderioux; Tomas Cihlar; Petr Dzubák; Joy Y Feng; Marián Hajdúch; Gabriel Birkus; Petr Konecný; Petr Naus; Pavla Perlíková; Iva Pichová; Radek Pohl; Adrian S Ray; Kirsten M Stray; Ivan Votruba; Ting Wang; Michal Hocek
Synthesis and significant cytostatic activity of 7-hetaryl-7-deazaadenosines.

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All Publications

2013: Christian R Frey; Wanchi Fung; Romas Geleziunas; Bin Han; Magdeleine Hung; Xiaohong Liu; Ghislain Opdenakker; Robert Snoeck; Ivan Votruba; Graciela Andrei; Carina Cannizzaro; Pierre Fiten; Tomas Cihlar
Mutations in Adenosine Deaminase-like (ADAL) Protein Confer Resistance to the Antiproliferative Agents N6-Cyclopropyl-PMEDAP and GS-9219.
Anticancer research 2013;33(5):1899-912.
2013: Kirsten M Stray; Luong Tsai; Lianhong Xu; Christian Callebaut; Bärbel Glass; Hans-Georg Kräusslich; Barbara Müller; Tomas Cihlar
Mutations in multiple domains of Gag drive the emergence of in vitro resistance to the phosphonate-containing HIV-1 protease inhibitor GS-8374.
Journal of virology 2013;87(1):454-63.
2011: Aurelie Bourderioux; Tomas Cihlar; Petr Dzubák; Joy Y Feng; Marián Hajdúch; Gabriel Birkus; Petr Konecný; Petr Naus; Pavla Perlíková; Iva Pichová; Radek Pohl; Adrian S Ray; Kirsten M Stray; Ivan Votruba; Ting Wang; Michal Hocek
Synthesis and significant cytostatic activity of 7-hetaryl-7-deazaadenosines.
Journal of medicinal chemistry 2011;54(15):5498-507.
2011: Gabriel Birkus; Nilima Kutty; Christian R Frey; Riri Shribata; Tsuifen Chou; Carston Wagner; Martin McDermott; Tomas Cihlar
Role of cathepsin A and lysosomes in the intracellular activation of novel antipapillomavirus agent GS-9191.
Antimicrobial agents and chemotherapy 2011;55(5):2166-73.
2011: Christian Callebaut; Kirsten Stray; Luong Tsai; Matt Williams; Zheng-Yu Yang; Carina Cannizzaro; Stephanie A Leavitt; Xiaohong Liu; Kelly Wang; Bernard P Murray; Andrew Mulato; Marcos Hatada; Tina Priskich; Neil Parkin; Swami Swaminathan; William Lee; Gong-Xin He; Lianhong Xu; Tomas Cihlar
In vitro characterization of GS-8374, a novel phosphonate-containing inhibitor of HIV-1 protease with a favorable resistance profile.
Antimicrobial agents and chemotherapy 2011;55(4):1366-76.
2010: Richard L Mackman; Adrian S Ray; Hon C Hui; Lijun Zhang; Gabriel Birkus; Constantine G Boojamra; Manoj C Desai; Janet L Douglas; Ying Gao; Deborah Grant; Genevieve Laflamme; Kuei-Ying Lin; David Y Markevitch; Ruchika Mishra; Martin McDermott; Rowchanak Pakdaman; Oleg V Petrakovsky; Jennifer E Vela; Tomas Cihlar
Discovery of GS-9131: Design, synthesis and optimization of amidate prodrugs of the novel nucleoside phosphonate HIV reverse transcriptase (RT) inhibitor GS-9148.
Bioorganic & medicinal chemistry 2010;18(10):3606-17.
2010: Eric B Lansdon; Dharmaraj Samuel; Leanna Lagpacan; Katherine M Brendza; Kirsten L White; Magdeleine Hung; Xiaohong Liu; Constantine G Boojamra; Richard L Mackman; Tomas Cihlar; Adrian S Ray; Mary E McGrath; Swami Swaminathan
Visualizing the molecular interactions of a nucleotide analog, GS-9148, with HIV-1 reverse transcriptase-DNA complex.
Journal of molecular biology 2010;397(4):967-78.
2009: Constantine G Boojamra; Jay P Parrish; David Sperandio; Ying Gao; Oleg V Petrakovsky; Sharon K Lee; David Y Markevitch; Jennifer E Vela; Genevieve Laflamme; James M Chen; Adrian S Ray; Abraham C Barron; Mark L Sparacino; Manoj C Desai; Choung U Kim; Tomas Cihlar; Richard L Mackman
Design, synthesis, and anti-HIV activity of 4'-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors.
Bioorganic & medicinal chemistry 2009;17(4):1739-46.
2008: Warner Greene; zeger debyser; Yasuhiro Ikeda; Eric O Freed; Edward Stephens; Wes Yonemoto; Robert W Buckheit; José A Esté; Tomas Cihlar
Novel targets for HIV therapy.
Antiviral research 2008;80(3):251-65.
2008: Koen K A Van Rompay; Lucie Durand-Gasselin; Laurie L Brignolo; Adrian S Ray; Kristina Abel; Tomas Cihlar; Abigail Spinner; Christopher Jerome; Joseph Moore; Brian P Kearney; Marta L Marthas; Hans Reiser; Norbert Bischofberger
Chronic administration of tenofovir to rhesus macaques from infancy through adulthood and pregnancy: summary of pharmacokinetics and biological and virological effects.
Antimicrobial agents and chemotherapy 2008;52(9):3144-60.
2008: Gabriel Birkus; Nilima Kutty; Gong-Xin He; Andrew Mulato; William Lee; Martin McDermott; Tomas Cihlar
Activation of 9-[(R)-2-[[(S)-[[(S)-1-(Isopropoxycarbonyl)ethyl]amino] phenoxyphosphinyl]-methoxy]propyl]adenine (GS-7340) and other tenofovir phosphonoamidate prodrugs by human proteases.
Molecular pharmacology 2008;74(1):92-100.
2008: Hans Reiser; Jianying Wang; Lee Chong; William J Watkins; Adrian S Ray; Riri Shibata; Gabriel Birkus; Tomas Cihlar; Sylvia Wu; Bei Li; Xiaohong Liu; Ilana N Henne; Grushenka H I Wolfgang; Manoj Desai; Gerald R Rhodes; Arnold Fridland; William A Lee; William Plunkett; David Vail; Douglas Thamm; Robert Jeraj; Daniel B Tumas
GS-9219--a novel acyclic nucleotide analogue with potent antineoplastic activity in dogs with spontaneous non-Hodgkin's lymphoma.
Clinical cancer research : an official journal of the American Association for Cancer Research 2008;14(9):2824-32.
2008: Constantine G Boojamra; Richard L Mackman; David Y Markevitch; Vidya Prasad; Adrian S Ray; Janet Douglas; Deborah Grant; Choung U Kim; Tomas Cihlar
Synthesis and anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor.
Bioorganic & medicinal chemistry letters 2008;18(3):1120-3.
2008: Richard L Mackman; Kuei-Ying Lin; Constantine G Boojamra; Hon C Hui; Janet Douglas; Deborah Grant; Oleg Petrakovsky; Vidya Prasad; Adrian S Ray; Tomas Cihlar
Synthesis and anti-HIV activity of 2'-fluorine modified nucleoside phosphonates: analogs of GS-9148.
Bioorganic & medicinal chemistry letters 2008;18(3):1116-9.
2008: Tomas Cihlar; Adrian S Ray; Constantine G Boojamra; Lijun Zhang; Hon C Hui; Genevieve Laflamme; Jennifer E Vela; Deborah Grant; James Chen; Florence Myrick; Kirsten L White; Ying Gao; Kuei-Ying Lin; Janet L Douglas; Neil T Parkin; Anne Carey; Rowchanak Pakdaman; Richard L Mackman
Design and profiling of GS-9148, a novel nucleotide analog active against nucleoside-resistant variants of human immunodeficiency virus type 1, and its orally bioavailable phosphonoamidate prodrug, GS-9131.
Antimicrobial agents and chemotherapy 2008;52(2):655-65.
2008: Adrian S Ray; Jennifer E Vela; Constantine G Boojamra; Lijun Zhang; Hon C Hui; Christian Callebaut; Kirsten Stray; Kuei-Ying Lin; Ying Gao; Richard L Mackman; Tomas Cihlar
Intracellular metabolism of the nucleotide prodrug GS-9131, a potent anti-human immunodeficiency virus agent.
Antimicrobial agents and chemotherapy 2008;52(2):648-54.
2007: Richard L Mackman; Constantine G Boojamra; Vidya Prasad; Lijun Zhang; Kuei-Ying Lin; Oleg Petrakovsky; Darius Babusis; James Chen; Janet Douglas; Deborah Grant; Hon C Hui; Choung U Kim; David Y Markevitch; Jennifer E Vela; Adrian Ray; Tomas Cihlar
Synthesis, anti-HIV activity, and resistance profiles of ribose modified nucleoside phosphonates.
Bioorganic & medicinal chemistry letters 2007;17(24):6785-9.
2007: Richard L Mackman; Lijun Zhang; Vidya Prasad; Constantine G Boojamra; Janet Douglas; Deborah Grant; Hon Hui; Choung U Kim; Genevieve Laflamme; Jay Parrish; Antitsa D Stoycheva; Swami Swaminathan; Keyu Wang; Tomas Cihlar
Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs.
Bioorganic & medicinal chemistry 2007;15(16):5519-28.
2007: Adrian S Ray; Tomas Cihlar
Unlikely association of multidrug-resistance protein 2 single-nucleotide polymorphisms with tenofovir-induced renal adverse events.
The Journal of infectious diseases 2007;195(9):1389-90; author reply 1390-1.
2007: Gabriel Birkus; Ruth Wang; Xiaohong Liu; Nilima Kutty; Holly MacArthur; Tomas Cihlar; Craig Gibbs; Swami Swaminathan; William Lee; Martin McDermott
Cathepsin A is the major hydrolase catalyzing the intracellular hydrolysis of the antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and GS-9131.
Antimicrobial agents and chemotherapy 2007;51(2):543-50.
2007: Richard L Mackman; Lijun Zhang; Vidya Prasad; Constantine G Boojamra; James Chen; Janet Douglas; Deborah Grant; Genevieve Laflamme; Hon Hui; Choung U Kim; Jay Parrish; Antitsa D Stoycheva; Swami Swaminathan; KeYu Wang; Tomas Cihlar
Synthesis and anti-HIV activity of cyclic pyrimidine phosphonomethoxy nucleosides and their prodrugs: a comparison of phosphonates and corresponding nucleosides.
Nucleosides, nucleotides & nucleic acids 2007;26(6-7):573-7.
2007: Tomas Cihlar; Adrian S Ray; Genevieve Laflamme; Jennifer E Vela; Leah Tong; Michael D Fuller; Anupma Roy; Gerald R Rhodes
Molecular assessment of the potential for renal drug interactions between tenofovir and HIV protease inhibitors.
Antiviral therapy 2007;12(2):267-72.
2006: Francesc Vidal; Joan Carles Domingo; Jordi P Guallar; Maria Saumoy; Begoña Cordobilla; Rainel Sánchez-de la Rosa; Marta Giralt; Maria Luisa Alvarez; Miguel López-Dupla; Ferran Torres; Francesc Villarroya; Tomas Cihlar; Pere Domingo
In vitro cytotoxicity and mitochondrial toxicity of tenofovir alone and in combination with other antiretrovirals in human renal proximal tubule cells.
Antimicrobial agents and chemotherapy 2006;50(11):3824-32.
2006: Tomas Cihlar; Gong-Xin He; Xiaohong Liu; James M Chen; Marcos Hatada; Swami Swaminathan; Martin J McDermott; Zheng-Yu Yang; Andrew S Mulato; Xiaowu Chen; Stephanie A Leavitt; Kirsten M Stray; William A Lee
Suppression of HIV-1 protease inhibitor resistance by phosphonate-mediated solvent anchoring.
Journal of molecular biology 2006;363(3):635-47.
2006: Adrian S Ray; Tomas Cihlar; Kelly L Robinson; Leah Tong; Jennifer E Vela; Michael D Fuller; Lani M Wieman; Eugene J Eisenberg; Gerald R Rhodes
Mechanism of active renal tubular efflux of tenofovir.
Antimicrobial agents and chemotherapy 2006;50(10):3297-304.
2006: Tomas Cihlar
Nucleotide HIV reverse transcriptase inhibitors: tenofovir and beyond.
Current opinion in HIV and AIDS 2006;1(5):373-9.
2005: Janet L Douglas; Marites L Panis; Edmund Ho; Kuei-Ying Lin; Steve H Krawczyk; Deborah M Grant; Ruby Cai; Swami Swaminathan; Xiaowu Chen; Tomas Cihlar
Small molecules VP-14637 and JNJ-2408068 inhibit respiratory syncytial virus fusion by similar mechanisms.
Antimicrobial agents and chemotherapy 2005;49(6):2460-6.
2005: William A Lee; Gong-Xin He; Eugene Eisenberg; Tomas Cihlar; Swami Swaminathan; Andrew S Mulato; Kenneth C Cundy
Selective intracellular activation of a novel prodrug of the human immunodeficiency virus reverse transcriptase inhibitor tenofovir leads to preferential distribution and accumulation in lymphatic tissue.
Antimicrobial agents and chemotherapy 2005;49(5):1898-906.
2004: Jens Rengelshausen; Heike Lindenmaier; Tomas Cihlar; Ingeborg Walter-Sack; Walter E Haefeli; Johanna Weiss
Inhibition of the human organic anion transporter 1 by the caffeine metabolite 1-methylxanthine.
Biochemical and biophysical research communications 2004;320(1):90-4.
2003: Janet L Douglas; Marites L Panis; Edmund Ho; Kuei-Ying Lin; Steve H Krawczyk; Deborah M Grant; Ruby Cai; Swami Swaminathan; Tomas Cihlar
Inhibition of respiratory syncytial virus fusion by the small molecule VP-14637 via specific interactions with F protein.
Journal of virology 2003;77(9):5054-64.
2003: Gabriel Birkus; C S Gibbs; Tomas Cihlar
Comparative effects of adefovir and selected nucleoside inhibitors of hepatitis B virus DNA polymerase on mitochondrial DNA in liver and skeletal muscle cells.
Journal of viral hepatitis 2003;10(1):50-4.
2002: Tomas Cihlar; Gabriel Birkus; Dale E Greenwalt; Michael J M Hitchcock
Tenofovir exhibits low cytotoxicity in various human cell types: comparison with other nucleoside reverse transcriptase inhibitors.
Antiviral research 2002;54(1):37-45.
2002: Gabriel Birkus; Michael J M Hitchcock; Tomas Cihlar
Assessment of mitochondrial toxicity in human cells treated with tenofovir: comparison with other nucleoside reverse transcriptase inhibitors.
Antimicrobial agents and chemotherapy 2002;46(3):716-23.
2002: George Hill; Tomas Cihlar; Charles Oo; Edmund S Ho; Ken Prior; Hugh Wiltshire; Jo Barrett; Baulian Liu; Penny Ward
The anti-influenza drug oseltamivir exhibits low potential to induce pharmacokinetic drug interactions via renal secretion-correlation of in vivo and in vitro studies.
Drug metabolism and disposition: the biological fate of chemicals 2002;30(1):13-9.
2001: Susan K Seo; A Regan; Tomas Cihlar; DC Lin; Farid Boulad; Diane George; VK Prasad; Timothy E Kiehn; B Polsky
Cytomegalovirus ventriculoencephalitis in a bone marrow transplant recipient receiving antiviral maintenance: clinical and molecular evidence of drug resistance.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America 2001;33(9):e105-8.
2001: Z M Wang; L L Tong; D Grant; Tomas Cihlar
Expression and characterization of soluble human parainfluenza virus type 1 hemagglutinin-neuraminidase glycoprotein.
Journal of virological methods 2001;98(1):53-61.
2001: Tomas Cihlar; Edmund S Ho; DC Lin; Andrew S Mulato
Human renal organic anion transporter 1 (hOAT1) and its role in the nephrotoxicity of antiviral nucleotide analogs.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):641-8.
2000: Andrew S Mulato; Edmund S Ho; Tomas Cihlar
Nonsteroidal anti-inflammatory drugs efficiently reduce the transport and cytotoxicity of adefovir mediated by the human renal organic anion transporter 1.
The Journal of pharmacology and experimental therapeutics 2000;295(1):10-5.
2000: Tomas Cihlar; Edmund S Ho
Fluorescence-based assay for the interaction of small molecules with the human renal organic anion transporter 1.
Analytical biochemistry 2000;283(1):49-55.
2000: Edmund S Ho; DC Lin; Dirk B Mendel; Tomas Cihlar
Cytotoxicity of antiviral nucleotides adefovir and cidofovir is induced by the expression of human renal organic anion transporter 1.
Journal of the American Society of Nephrology : JASN 2000;11(3):383-93.
1999: Tomas Cihlar; DC Lin; John B Pritchard; Michael D Fuller; Dirk B Mendel; Douglas H Sweet
The antiviral nucleotide analogs cidofovir and adefovir are novel substrates for human and rat renal organic anion transporter 1.
Molecular pharmacology 1999;56(3):570-80.
1998: Tomas Cihlar; Michael D Fuller; Andrew S Mulato; Julie M Cherrington
A point mutation in the human cytomegalovirus DNA polymerase gene selected in vitro by cidofovir confers a slow replication phenotype in cell culture.
Virology 1998;248(2):382-93.
1998: Michael D Miller; PD Lamy; Michael D Fuller; Andrew S Mulato; Nicolas A Margot; Tomas Cihlar; Julie M Cherrington
Human immunodeficiency virus type 1 reverse transcriptase expressing the K70E mutation exhibits a decrease in specific activity and processivity.
Molecular pharmacology 1998;54(2):291-7.
1998: Tomas Cihlar; Michael D Fuller; Julie M Cherrington
Characterization of drug resistance-associated mutations in the human cytomegalovirus DNA polymerase gene by using recombinant mutant viruses generated from overlapping DNA fragments.
Journal of virology 1998;72(7):5927-36.
1997: Tomas Cihlar; Michael D Fuller; Julie M Cherrington
Expression of the catalytic subunit (UL54) and the accessory protein (UL44) of human cytomegalovirus DNA polymerase in a coupled in vitro transcription/translation system.
Protein expression and purification 1997;11(2):209-18.
1997: Dirk B Mendel; Tomas Cihlar; K Moon; MS Chen
Conversion of 1-[((S)-2-hydroxy-2-oxo-1,4,2-dioxaphosphorinan-5-yl)methyl]cytosine to cidofovir by an intracellular cyclic CMP phosphodiesterase.
Antimicrobial agents and chemotherapy 1997;41(3):641-6.