HIV-1 reverse transcriptase and antiviral drug resistance. Part 1

Current Opinion in Virology

Volumn 3, Issue 2, 2013, Pages 111-118

  Das, Kalyan ^a   Arnold, Eddy ^a  

^a RUTGERS UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DELAVIRDINE; DIDANOSINE; EFAVIRENZ; ETRAVIRINE; LAMIVUDINE; NEVIRAPINE; NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR; RILPIVIRINE; RNA DIRECTED DNA POLYMERASE; RNA DIRECTED DNA POLYMERASE INHIBITOR; STAVUDINE; ZALCITABINE; ZIDOVUDINE;

ANTIVIRAL RESISTANCE; ANTIVIRAL THERAPY; ARTICLE; DRUG APPROVAL; DRUG CONFORMATION; HUMAN IMMUNODEFICIENCY VIRUS 1 INFECTION; NONHUMAN; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION;

EID: 84880054656     PISSN: 18796257     EISSN: 18796265     Source Type: Journal    
DOI: 10.1016/j.coviro.2013.03.012     Document Type: Review

References (31)

1. Barre-Sinoussi F, Chermann JC, Rey F, Nugeyre MT, Chamaret S, Gruest J, Dauguet C, Axler-Blin C, Vezinet-Brun F, Rouzioux C et al.: Isolation of a T-lymphotropic retrovirus from a patient at risk for acquired immune deficiency syndrome (AIDS). Science 1983, 220:868-871.
2. Gallo RC, Salahuddin SZ, Popovic M, Shearer GM, Kaplan M, Haynes BF, Palker TJ, Redfield R, Oleske J, Safai B et al.: Frequent detection and isolation of cytopathic retroviruses (HTLV-III) from patients with AIDS and at risk for AIDS. Science 1984, 224:500-503.
3. Mitsuya H, Weinhold KJ, Furman PA, St Clair MH, Lehrman SN, Gallo RC, Bolognesi D, Barry DW, Broder S: 30-Azido-30-deoxythymidine (BW A509U): an antiviral agent that inhibits the infectivity and cytopathic effect of human T-lymphotropic virus type III/lymphadenopathy-associated virus in vitro. Proc Natl Acad Sci U S A 1985, 82:7096-7100.
4. Fischl MA, Richman DD, Grieco MH, Gottlieb MS, Volberding PA, Laskin OL, Leedom JM, Groopman JE, Mildvan D, Schooley RT et al.: The efficacy of azidothymidine (AZT) in the treatment of patients with AIDS and AIDS-related complex. A double-blind, placebo-controlled trial. N Engl J Med 1987, 317:185-191.
5. Grobler JA, Stillmock K, Hu B, Witmer M, Felock P, Espeseth AS, Wolfe A, Egbertson M, Bourgeois M, Melamed J et al.: Diketo acid inhibitor mechanism and HIV-1 integrase: implications for metal binding in the active site of phosphotransferase enzymes. Proc Natl Acad Sci U S A 2002, 99:6661-6666.
6. Hare S, Vos AM, Clayton RF, Thuring JW, Cummings MD, Cherepanov P: Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance. Proc Natl Acad Sci U S A 2010, 107:20057-20062.
7. Keele BF, Giorgi EE, Salazar-Gonzalez JF, Decker JM, Pham KT, Salazar MG, Sun C, Grayson T, Wang S, Li H et al.: Identification and characterization of transmitted and early founder virus envelopes in primary HIV-1 infection. Proc Natl Acad Sci U S A 2008, 105:7552-7557.
8. Coffin JM: HIV population dynamics in vivo: implications for genetic variation, pathogenesis, and therapy. Science 1995, 267:483-489.
9. Ho DD, Neumann AU, Perelson AS, Chen W, Leonard JM, Markowitz M: Rapid turnover of plasma virions and CD4 lymphocytes in HIV-1 infection. Nature 1995, 373:123-126.
10. Ratner L, Haseltine W, Patarca R, Livak KJ, Starcich B, Josephs SF, Doran ER, Rafalski JA, Whitehorn EA, Baumeister K et al.: Complete nucleotide sequence of the AIDS virus, HTLVIII. Nature 1985, 313:277-284.
11. Wain-Hobson S, Sonigo P, Danos O, Cole S, Alizon M: Nucleotide sequence of the AIDS virus, LAV. Cell 1985, 40:9-17.
12. Mansky LM, Temin HM: Lower in vivo mutation rate of human immunodeficiency virus type 1 than that predicted from the fidelity of purified reverse transcriptase. J Virol 1995, 69:5087-5094.
13. Kohlstaedt LA, Wang J, Friedman JM, Rice PA, Steitz TA: Crystal structure at 3.5 A ° resolution of HIV-1 reverse transcriptase complexed with an inhibitor. Science 1992, 256:1783-1790.
14. Jacobo-Molina A, Ding J, Nanni RG, Clark AD Jr, Lu X, Tantillo C, Williams RL, Kamer G, Ferris AL, Clark P et al.: Crystal structure of human immunodeficiency virus type 1 reverse transcriptase complexed with double-stranded DNA at 3.0 A ° resolution shows bent DNA. Proc Natl Acad Sci U S A 1993, 90:6320-6324.
15. Nikolenko GN, Palmer S, Maldarelli F, Mellors JW, Coffin JM, Pathak VK: Mechanism for nucleoside analog-mediated abrogation of HIV-1 replication: balance between RNase H activity and nucleotide excision. Proc Natl Acad Sci U S A 2005, 102:2093-2098.
16. Yap SH, Sheen CW, Fahey J, Zanin M, Tyssen D, Lima VD, Wynhoven B, Kuiper M, Sluis-Cremer N, Harrigan PR et al.: N348I in the connection domain of HIV-1 reverse transcriptase confers zidovudine and nevirapine resistance. PLoS Med 2007, 4:e335.
17. Meyer PR, Matsuura SE, So AG, Scott WA: Unblocking of chainterminated primer by HIV-1 reverse transcriptase through a nucleotide-dependent mechanism. Proc Natl Acad Sci U S A 1998, 95:13471-13476.
18. Arion D, Kaushik N, McCormick S, Borkow G, Parniak MA: Phenotypic mechanism of HIV-1 resistance to 30-azido-30-deoxythymidine (AZT): increased polymerization processivity and enhanced sensitivity to pyrophosphate of the mutant viral reverse transcriptase. Biochemistry 1998, 37:15908-15917.
19. Ding J, Das K, Moereels H, Koymans L, Andries K, Janssen PA, Hughes SH, Arnold E: Structure of HIV-1 RT/TIBO R 86183 complex reveals similarity in the binding of diverse nonnucleoside inhibitors. Nat Struct Biol 1995, 2:407-415.
20. Das K, Clark JAD, Lewi PJ, Heeres J, de Jonge MR, Koymans LMH, Vinkers HM, Daeyaert F, Ludovici DW, Kukla MJ et al.: Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (Etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drugresistant HIV-1 variants. J Med Chem 2004, 47:2550-2560.
21. Janssen PA, Lewi PJ, Arnold E, Daeyaert F, de Jonge M, Heeres J, Koymans L, Vinkers M, Guillemont J, Pasquier E et al.: In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2- cyanoethenyl]-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). J Med Chem 2005, 48:1901-1909.
22. de Bethune MP: Non-nucleoside reverse transcriptase inhibitors (NNRTIs), their discovery, development, and use in the treatment of HIV-1 infection: a review of the last 20 years (1989-2009). Antiviral Res 2010, 85:75-90.
23. Das K, Bauman JD, Clark AD Jr, Frenkel YV, Lewi PJ, Shatkin AJ, Hughes SH, Arnold E: High-resolution structures of HIV-1 reverse transcriptase/TMC278 complexes: strategic flexibility explains potency against resistance mutations. Proc Natl Acad Sci U S A 2008, 105:1466-1471.
24. Chong P, Sebahar P, Youngman M, Garrido D, Zhang H, Stewart EL, Nolte RT, Wang L, Ferris RG, Edelstein M et al.: Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. J Med Chem 2012, 55:10601-10609.
25. Kuroda D, Bauman JD, Challa JR, Patel D, Troxler T, Das K, Arnold E, Hochstrasser RM: Snapshot of the equilibrium dynamics of a drug bound to human immunodeficiency virus 1 reverse transcriptase. Nat Chem 2013, 5:174-181.
26. Frenkel YV, Clark AD Jr, Das K, Wang YH, Lewi PJ, Janssen PA, Arnold E: Concentration and pH dependent aggregation of hydrophobic drug molecules and relevance to oral bioavailability. J Med Chem 2005, 48:1974-1983.
27. Jilek BL, Zarr M, Sampah ME, Rabi SA, Bullen CK, Lai J, Shen L, Siliciano RF: A quantitative basis for antiretroviral therapy for HIV-1 infection. Nat Med 2012, 18:446-451.
28. Shen L, Peterson S, Sedaghat AR, McMahon MA, Callender M, Zhang H, Zhou Y, Pitt E, Anderson KS, Acosta EP et al.: Doseresponse curve slope sets class-specific limits on inhibitory potential of anti-HIV drugs. Nat Med 2008, 14:762-766.
29. Hsiou Y, Ding J, Das K, Clark AD Jr, Hughes SH, Arnold E: Structure of unliganded HIV-1 reverse transcriptase at 2.7 A resolution: implications of conformational changes for polymerization and inhibition mechanisms. Structure 1996, 4:853-860.
30. Huang H, Chopra R, Verdine GL, Harrison SC: Structure of a covalently trapped catalytic complex of HIV-1 reverse transcriptase: implications for drug resistance. Science 1998, 282:1669-1675.
31. Das K, Martinez SE, Bauman JD, Arnold E: HIV-1 reverse transcriptase complex with DNA and nevirapine reveals non-nucleoside inhibition mechanism. Nat Struct Mol Biol 2012, 19:253-259.