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Original Article

Monthly Update: Anti-infectives: Recent advances in HIV-1 protease inhibitors

Pages 115-124 | Published online: 03 Mar 2008

References

  • VAN LEEUWEN R, KATLAMA C, KITCHEN V, BOUCHER CAB, TUBIANA R, MCBRIDE M et al.: Evaluation of safety and efficacy of 3TC (Lamivudine) in patients with a-symptomatic or mildly symptomatic human immuno- deficiency virus infection: A Phase I/11 study. JDis(1995) 171:1166–1171
  • DECLERCQ E: Non-nucleoside reverse transcriptase in-hibitors. Esp. Opin. Invest. Drugs (1994) 3:253–271.
  • DECLERCQ E: HIV resistance to reverse transcriptase Inhibitors. Biochem. Pharmacol. (1994) 47:155–169.
  • MERIGAN TC: Treatment of AIDS with combinations of antiretroviral agents. Am.j Med. (1991) 90:8S–17S.
  • JOHNSTON MI, HOTH DF: Present status and future prospects for HIV therapies. Science (1993) 260:1286–1293.
  • GOTTLINGER H, SODROSKI J, HASELTINE W: Role ofcapsid precursor processing and myristoylation in morphogenesis and infectivity of human immunodefi-ciency virus type 1. Proc. NatI Acad. Sci. USA (1989) 86:5781–5785.
  • KOHL NE, EMINI EA, SCHLEIF WA, DAVIS LJ, HEIMBACH JC, DIXON RAF et al.: Active human immunodeficiency virus protease is required for viral infectivity. Proc. Natl. Acad. Sci. USA (1988) 85:4686–4690.
  • WLODAWER A, ERICKSON JW: Structure-based inhibitors of HIV-1 protease. Ann. Rev. Biochem. (1993) 62:543–585.
  • DARKE PL, HUFF JR: HIV protease inhibitors target for the treatment of AIDS. In: Advances in Pharmacology. August TJ, Ander MW, Murad F (Eds.), Academic Press, San Diego (1994) 25:399–454.
  • THAISRIVONGS S: HIV protease inhibitors (Chapter 14). Ann. Rep. Med. Chem. (1994) 17:133–144.
  • KEMPF DJ: Progress in the discovery of orally bioavail-able inhibitors of HIV protease. Perspectives in Drug Discovery and Design (1994) 2:427–436.
  • WEST ML, FAIRLIE DP: Targeting HIV-1 protease: a test of drug-design methodologies. Trends Pharmacol. Sci. (1995) 16:67-75. MARTIN JA, REDSHAW S, THOMAS GJ: Inhibitors of HIV proteinase. Prog. Medi.Chein. (1995) 32:239. REDSHAW S: Inhibitors of HIV proteases. Exp. Opin. Invest. Drugs (1994) 3:273-286. DEBOUCK C: The HIV-I protease as a therapeutic target for AIDS. AIDS Res. Human Retroviruses (1992) 8:153-164. MARTIN JA: Recent advances in the design of HIV prote-inase inhibitors. Antiviral Res. (1992) 17:265-278. HO DD: Time to hit HIV, early and hard. New Engl.J. Med. (1995) 333:450-451. JOIINSON VA, MERRILL DP, CHOU T-C, HIRSCH MS: Hu-man immunodeficiency virus type 1 (HIV-1) inhibitory interactions between protease inhibitor Ro 31–8959 and zidovudine, 2',3'-dideoxycytosine or recombinant in-terferon aA against zidovudine-sensitive or -resistant 111V-1 in vitro. J. Infect. Dis. (1992) 166:1143–1146.
  • ROBERTS NA, MARTIN JA, KINCIIINGTON D, BROAD- HURST AV, CRAIG JC, DUNCAN IB et al.: Rational design of peptide-based HIV proteinase inhibitors. Science (1990) 248:358–361.
  • DANNER SA eta: Safety, pharmacokinetics and virologi- cal/immunological efficacy of ABT-538, an HIV-pro-tease inhibitor. A randomized, placebo-controlled Phase I/11 study. (1994) AIDS 8:9.
  • LEWIS K, MUSICK L, WU BW, ANDRADA D, SHERRY B, DAVIES J et al: Discovery of a series of non-peptidic HIV protease Inhibitors via structure-based iterative drug design. 207th Nail ACS. San Diego, CA (1994). Abstract Medi–20.
  • WEBBER S, KHALIL D, KOSA M, PATICK A, SHETTY B: Preclinical toxicokinetic studies with AG-1343, an orally bioavailable HIV-1 protease inhibitor. Second National Conference on Human Retorviruses. Washington DC (1995). Abstract 93.
  • MOYLE G, YOULE M, CHAPMAN S, PETERKIN J, MONA- GHAN, PARNELL A et al.: A Phase II dose escalation study of the agouron protease inhibitor AG-1343. 35th Inter-science Conference on Antimicrobial Agents and Chemother-apy. San Francisco (1995). Abstract LB–3.
  • MARKOWITZ M, CONANT M, HURLEY A, WAGGONER S, HO D, PETERKIN J et al.: Phase I/11 dose range-finding study of the HIV protease inhibitor AG-1343. 35th Inter-science Conference on Antimicrobial Agents and Chemother-apy. San Francisco (1995). Abstract LB–4.
  • PAINTER GR, STCLAIR MH, DEMIRANDA P, REYNOLDS D, CHING S, DORNSIFE R et al.: An overview of the preclini-cal development of the HIV protease inhibitor VX-478 (I41W94). Second National Conference on Human Re-torviruses. Washington DC (1995). Abstract LB5.
  • KIM EE, DWYER MD, THOMSON JA, BAKER CT, DEININGER DD, TUNG RD et al.: Structural analysis of the basis of viral resistance to VX-478. 35th Interscience Conference on Antimicrobial Agents and Chemotherapy. San Francisco, CA (1995). Abstract 1278.
  • LAM PY-S, JADHAV PK, EYERMANN CJ, HODGE CN, RU Y, BACHELER LT et al.: Cyclic, non-peptide HIV protease Inhibitors: de novo design and characterization of po-tent, orally bioavailable cyclic ureas. Science (1994) 363:380–384,
  • ERICKSON-VIITANEN S, HODGE CN, ALDRICH PE, BACHELER LT, CHANG C-H, EYERMANN CJ et al.: Cyclic urea inhibitors of lily protease. Second National Confer-ence on Human Retorviruses. Washington DC (1995). Ab-stract 96.
  • TITAISRIVONGS S, TOMICH PK, WATENPAUGH KD, CHONG K-T, HOWE WJ, YANG C-P: Structure-based de-sign of 1HV protease inhibitors: 4-hydroxycoumnrins and 4-hydroxy-2-pyrones as non-peptidic inhibitors. J. Med. Chem. (1994) 37:3200–3204.
  • CHONG KT, ZIPP GL, RUWART MJ, SCHWENDE FJ, PAD- BURY GE, TOMICH PK et al.: U-103017: An improved 4-hydroxy-2-pyrone inhibitor of HIV protease. 35th Interscience Conference on Antimicrobial Agents and Che-motherapy. San Francisco, CA (1995). Abstract 1121.
  • SKULNICK III, JOHNSON PD, HOWE vg, TOMICH PK, CHONG K-T, WATENTAUGH ND et al Structure-based design of sulfonamide substituted non-peptidic HIV protease inhibitors. Med Chem (1995) In press
  • KITCHEN VS, SKINNER C, ARIYOSHI K, LANE EA, DUNCANIB, BURCKHARDTJ et at: Safety and activity of saquinavir In HIV infection. The Lancet (1995) 345:952–955.
  • VELLA S: Update on a protease inhibitor. AIDS (1994)8:S25–S29.
  • COLLIER AC, COOMBS RW, SCHOENTELD DA, BASSETT R,BARUCH A, COREY L: Extended Treatment with Saqui-navir (SAQ), Zidovudine (ZDV), and Zalcitabine (ddC) vs. SAQ and ZDV vs. ddC and ZDV. 35th lnterscience Conference on Antimicrobial Agents and Chemotherapy. San Francisco (1995). Abstract 1173.
  • SCHAPIRO JM, WINTERS MA, KOZAI MJ, MERIGAN TC:Saquirtavir monotherapy trial: prolonged suppression of viral load and resistance mutations with higher dosage. 35th Interscience Conference on Antimicrobial Agents and Chemotherapy. San Francisco (1995). Abstract LB–5.
  • MELLORS J, STEIGBIGEL R, GULICK R, FRANK I, BERRY P,MCMAHON D et al.: Antiretroviral activity of the oral protease inhibitor, MK-639, in p24 antigenemic, HIV-1 infected patients with CD4/mm3. 35th Interscience Con-ference on Antimicrobial Agents and Chemotherapy, San Francisco (1995). Abstract 1172.
  • KORNEYEVA M, BOUCHER C, NIU P, SCHIPPER P, LYONSN, KEMPF DJ et al.: Phenotypic and genotypic evolution of HIV-1 in AIDS patients undergoing therapy with the protease inhibitor ABT-538. 35th Interscience Conference on Antimicrobial Agents and Chemotherapy. San Francisco (1995). Abstract 1175.
  • BRYANT M, GETMAN D, SMIDT M, MARK J, CLARE M, DILLARD R et al: SC-52151, a novel inhibitor of the human immunodeficiency virus protease. Antimicrob. Agents Chemother. (1995) 39:2229–2234.
  • ALTER' E, BOLD G, COZENS R, FAESSLER A, KLIMKAIT T, LANG M et al.: CGP-53437, an orally bioavailable inhibi-tor of human immunodeficiency virus type 1 protease with potent antiviral activity. Antimicrob. Agents Chemother. (1993) 37:2087–2092.
  • BORIN MT, BATTS DR PEEL BG, HANOVER CK, BREWERJE, FRANCOM SF, DIETZ AJ: U-103017, Phase I, single-dose, randomized, double-blind, safety, tolerance, and Pharmacolcinetics of several oral formulations in healthy volunteers. 35th Interscience Conference on An-timicrobial Agents and Chemotherapy. San Francisco (1995). Abstract A128.
  • CRAIG JC, WHTITAKER L, DUNCAN LB, ROBERTS NA: Invitro resistance to an inhibitor of HIV proteinase (Ro 31-8959) relative to inhibitors of reverse transcriptase (AZT and T1BO). Antivir. Chem. Chemother. (1993) 4:335–339.
  • DIANZANI F, ANTONELLI G, TURRIZIANI 0, RIVA E, DOUGG, BELLAROSA D. In vitro selection of human immu-nodeficiency virus type 1 resistant to Ro 31–8959 prote-inase inhibitor. Antivir. Chem. Chemother. (1993) 4:329–333.
  • EL-FARRASH MA, KURODA MJ, KITAZAKI T, MASLTDA T, KATO K, HATANAKA M, HARADA S: Generation and characterization of a human immunodeficiency virus type 1 (mV-1) mutant resistant to an HIV-1 protease inhibitor.]. Virol. (1994) 68:233–239.
  • EMINI E, SCI ILEIF WA, GRAHAM D, DEUTSCH P, MASSARI F, TEPPLER H et al.: Phenotypic and genotypic charac-terization of HIV-1 variants selected during treatment with the protease inhibitor L-735,524. Third Interna-tional Workshop on HIV Drug Resistance. Kauai, Hawaii, USA (1994) 3:16.
  • HO DD, TOYOSHIMA T, MO H, KEMPF DJ, NORBECK D,CHEM C-M vial.: Characterization of human immunode-ficiency virus type 1 variants with increased resistance to a C2-symmetric protease inhibitor. J. Virol. (1994) 68:2016–2020.
  • MARKOVITZ M, MO H, KEMPF DJ, NORBECK DW, BHATTN, ERICKSON JW et al: Selection and analysis of human Immunodeficiency virus type 1 variants with increased resistance to ABT-538, a novel protease inhibitor. J. Virol. (1995) 69:701–706.
  • TISDALE M, MYERS RE, MASCHERA B, PARRY NR, OLIVERNM, BLAIR ED: Cross-resistance analysis of human im-munodeficiency virus type 1 variants individually se-lected for resistance to five different protease Inhibitors. Antimicrob. Agents Chemother. (1995) 39:1704–1710.
  • KING RW, GARBER 5, WINSLOW DL, REID CD, BACHELERLT, ANTON E et at: Multiple mutations in the human immunodeficiency virus protease gene are responsible for decreased susceptibility to protease inhibitors. An-tiviral Chem. Chemother. (1995) 6. In press.
  • OTTO MJ, GABBER S, WINSLOW DL, REID CD, ALDRICH P,JADHAV PK et al.: In vitro isolation and identification of human immunodeficiency virus (HIV) variants with reduced sensitivity to C-2 symmetrical inhibitors of HIV type 1 protease. Proc. Natl. Acad. Sci. USA (1993) 90:7543–7547.
  • JACOBSEN H, BRUN-VEZINET F, DUNCAN I, HANGGI M,OTT M, VELLA S et al.: Genotypic characterization of 111V-1 from patients after prolonged treatment with proteinase inhibitor saquinivir. Third International Workshop on HIVD rug Resistance. Kauai, Hawaii, USA (1994) 3:16.
  • CONDRA JH, SCHLEIF WA, BLAHY OM, GABRYELSK1 IJ,GRAHAM DJ, QUINTERO JC: /n vivo emergence of HIV-1 variants resistant to multiple protease inhibitors. Na-ture (1995) 374:569–571.
  • ROBERTS NA, RACE E, TOMLINSON P, GILBERT S, DUNCANIB: Resistance and cross resistance issues: Studies with saquinavir. 35th Interscience Conference on Antimicrobial Agents and Chemotherapy. San Francisco (1995). Abstract 274.
  • VACCA JP, DORSEY BD, SCIILEIF WA, LEVIN RB,MCDANIEL SL, DARKE J et al.: L735,524: an orally b ioavail-able human immunodeficiency virus type 1 protease Inhibitor. Proc. Natl. Acad. Sci. USA (1994) 91:4096–4100.
  • GAO Q, STEWART K, PARK C, DAVE A, KEMPF DJ, LEONARD J et al: Specific mutations in HIV-1 protease that confer diminished susceptibility to ABT-538. 35th Interscience Conference on Antimicrobial Agents and Che-motherapy. San Francisco (1995). Abstract 1282.
  • KAGEYAMA S, WEISTEIN JN, SHIRASAKA T, KEMPF DJ,NORBECK DW, PLANTNER JJ et al.: /n vitro inhibition of human immunodeficiency virus HIV type 1 replication by C-2 symmetry-based HIV protease inhibitors as sin-gle agents or in combinations. Antimicrob, Agents Chemother. (1992) 36:926–933.
  • CRAIG JC, DUNCAN II3, WHITTAKER I, ROBERTS NA: Antiviral synergy between inhibitors of HIV proteinase and reverse transcriptase. Antiviral Chem. Chemother. (1990) 4:161–166.
  • PAGANO PJ, CHONG KT: In vitro inhibition of human immunodeficiency virus type 1 by a combination of delavirdine (U-90152) with protease inhibitor U-75875 or interferon-a. J. Inf. Dis. (1995) 171:61–67.
  • LAMBERT DM, BARTUS H, FERNANDEZ AV et al.: Syner-gistic drug interactions of an HIV-1 protease inhibitor with AZT in different in vitro models of HIV-1 infection. Antiviral Res. (1993) 21:327–342.
  • CRAIG JC, GRIEF C, MILLS JS, HOCKLEY D, GRIEF C, ROBERTS NA etal.: Antiviral properties of Ro 31–8959 an inhibitor of human immunodeficiency virus HIV pro-teinase. Antiviral Res. (1991) 2:181–186.
  • KEMPF DJ, MARSH KC, DENISSEN JF, MCDONALD E, VASA-VANONDA S, FLENTGE CA et al.: ABT-538 is a potent inhibitor of human immunodeficiency virus protease and has high oral bioavailability in humans. Proc. Natl. Acad. Sci. USA (1995) 92:2484–2488.
  • KEMPF DJ, MARSH KC, PAUL DA, KNIGGE MF, NORBECKDW, KOHLBRENNER WE et al.: Antiviral and pharmacok-inetic properties of C2 symmetric inhibitors of the human immunodeficiency virus type 1 protease. An-timicrob. Agents Chemother (1992) 35:2209–2214.
  • BRYANT M, CLARE M, DECRESCENZO G, DORN C, GET-MAN D, HEINTZ R et al.: SC-52151, A potent selective inhibitor of the HIV aspartyl protease. Antimicrob. Agents Chemother. (1992) 32:361.
  • KAGEYAMA S, MIMOTC, T, MURAKAWA Y, NOMIZU M,FORD JR H, SHIRASAKA T et al.: In vitro anti-human immunodeficiency virus (HIV) activities of transition state mimetic illy protease inhibitors containing allo-phenylnorstatine. Antimicrob. Agents Chemother. (1993) 37:810–817.
  • PAESSENS A, BUDT K-H, KLEIM J-P, KNOLLE J, MEICHSNER C, RLEB G et al.: HIV protease inhibitor HOE/BAY 793 Part 2: Virological characterization. IXtb International Conference on AIDS/IVth RD World Congress. Berlin (1993). Abstract A25–0611.
  • ALTERI E, BOLD G, COZENS RM, CAPRARO H-G, DOELKER E, FASSLER A et al.: Identification and biological profile of the orally bioavailable HIV-protease inhibitor. 35th Intetscience Conference on Antimicrobial Agents and Che-motherapy. San Francisco (1995). Abstract 1127.
  • BILLICH A, FRICKER G, MULLER I, DONATSCH P, ETIMAYER P, GSTACH H et al.: SDZ PRI 053, an orally bioavailable human immunodeficiency virus type 1 proteinase inhibitor containing the 2-aminobenzylstat-ine moiety. Antimicrob. Agents Chemother. (1995) 39:1406–1413.

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