Abstract
Mutant HIV-1 that expresses a Glu138-->Lys substitution in its RT [(E138K)RT] is resistant to the HIV-1-specific RT inhibitor 2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro-5"-(4"-amino-1",2"- oxathiole-2",2"-dioxide)pyrimidine (TSAO). However, cell cultures infected with this mutant were completely protected against virus-mediated destruction by micromolar concentrations of the HIV-1-specific RT inhibitors tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione (TIBO), nevirapine, and bis(heteroaryl)piperazine (BHAP). In contrast, cells infected with a virus mutant that expresses a Tyr181-->Cys substitution in its RT [(Y181C)RT] were not protected by nevirapine and TIBO and were only temporarily protected by BHAP. HIV-1 mutant that emerged under the latter conditions contained a Cys181-->Ile substitution in their RT [(LC181I)RT]. This mutant proved highly resistant to all HIV-1-specific RT inhibitors tested, except for several 1-(2-hydroxyethoxymethyl)-6-(phenylthio)thymine (HEPT) derivatives. When recombinant (C181I)RT was evaluated for susceptibility to the HIV-1-specific RT inhibitors, it was resistant to all inhibitors except the HEPT compounds. Since a (Y181F)RT HIV mutant strain was isolated from cells infect...Continue Reading
References
Jun 1, 1992·Virology·K de VreeseJ Anné
Jul 1, 1992·Antimicrobial Agents and Chemotherapy·J H CondraV V Sardana
Sep 1, 1992·Virology·M B VasudevachariN P Salzman
Jul 20, 1991·Lancet·G PialouxP A Janssen
Nov 1, 1991·Proceedings of the National Academy of Sciences of the United States of America·C K ShihJ A Griffin
Dec 15, 1991·Proceedings of the National Academy of Sciences of the United States of America·D RichmanJ Griffin
Aug 1, 1988·Proceedings of the National Academy of Sciences of the United States of America·R J ColonnoM A Murcko
May 15, 1993·Proceedings of the National Academy of Sciences of the United States of America·T J DuewekeW G Tarpley
Jan 1, 1993·Virology·J BalzariniE De Clercq
May 1, 1993·Antimicrobial Agents and Chemotherapy·T J DuewekeL Resnick
Oct 7, 1993·The New England Journal of Medicine·M S SaagJ C Kappes
Oct 1, 1993·Virology·J BalzariniE De Clercq
Aug 1, 1993·Antimicrobial Agents and Chemotherapy·J P KleimA Paessens
Citations
Jun 1, 1996·Reviews in Medical Virology· De Clercq E
Jun 1, 1995·Antiviral Research·J BalzariniA Karlsson
Jun 1, 1996·Antiviral Research·W KeulenB Berkhout
Jan 1, 1996·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·E De Clercq
May 14, 2003·Antiviral Research·F NotkaR Wagner
Mar 1, 1997·Antiviral Research·K T Chong, P J Pagano
Jun 1, 1997·International Journal of Antimicrobial Agents·E De Clercq
Jan 13, 2001·Journal of Molecular Graphics & Modelling·P Pungpo, S Hannongbua
Jul 5, 2005·The Journal of Infectious Diseases·Soo-Yon RheeRobert W Shafer
Oct 6, 2000·AIDS Research and Human Retroviruses·P B GilbertR T D'Aquila
Apr 25, 2013·Antimicrobial Agents and Chemotherapy·Hong-Tao XuMark A Wainberg
Jan 19, 2012·Antimicrobial Agents and Chemotherapy·Karen A KirbyStefan G Sarafianos
Apr 1, 1995·Antimicrobial Agents and Chemotherapy·J BalzariniE De Clercq
Apr 5, 2002·Clinical Microbiology Reviews·Robert W Shafer
Dec 28, 2002·Journal of Virology·Wei HuangJeannette M Whitcomb
Jun 29, 2004·Journal of Virology·Joeri AuwerxJan Balzarini
Sep 29, 2005·Journal of Virology·Johan VingerhoetsMarie-Pierre de Béthune
Jun 9, 2001·Antiviral Research·C ChamorroM J Camarasa
Jul 2, 2005·Expert Opinion on Emerging Drugs·M L AndreolaM Legraverend
Sep 8, 2011·Antiviral Research·Luis Menéndez-AriasTania Matamoros
Sep 29, 2009·Antiviral Research·Marie-Pierre de Béthune
Aug 14, 1995·FEBS Letters·N FanS K Sharma
Apr 1, 1995·Nature Structural Biology·J RenD Stuart
Nov 10, 2011·Journal of Acquired Immune Deficiency Syndromes : JAIDS·Laurence RimskyGaston Picchio
Jan 12, 1995·Nature·X WeiB H Hahn
Feb 18, 2010·AIDS·Hiroyuki GatanagaShinichi Oka
Jun 4, 2011·Journal of Acquired Immune Deficiency Syndromes : JAIDS·Lotke TambuyzerJohan Vingerhoets
Feb 9, 2007·The Biochemical Journal·Dwight V NissleyNicolas Sluis-Cremer
Aug 18, 2020·Computational Biology and Chemistry·Pooja Balasaheb ShindeMd Ataul Islam
Oct 23, 1997·Clinical Microbiology Reviews·E De Clercq
Dec 1, 1994·Journal of Virology·J BalzariniJ P Kleim
Jul 1, 1996·Antimicrobial Agents and Chemotherapy·Y KewV R Prasad
Feb 15, 2001·Journal of Medicinal Chemistry·R C RizzoW L Jorgensen