Section Reviews; Anti-infectives: Section Review Anti-infectives: HIV protease inhibitors in early development

References to Primary Literature

• AGGLETON P, O'REILLY K, SLUTKIN G, DAVIES P: Risking everything? Risk behaviour change and AIDS. Science (1994) 265:341–345.
   PubMedGoogle Scholar
• WEI X, GHOSH SK, TAYLOR ME et al.: Viral dynamics inhuman immunodeficiency virus type 1 infection. Nature (1995) 373:117–122.
   PubMed Web of Science ®Google Scholar
• HO DD, NEUMANN AU, CHEN W et al.: Rapid turnover ofplasma virions and CD4 lymphocytes in HIV-1 infec-tion. Nature (1995) 373:123–126.
   PubMed Web of Science ®Google Scholar
• O'BRIEN WA, HARTIGAN PM, MARTIN D et al.: Changes inplasma HIV-1 RNA and CD4 lymphocyte counts and risk of progression to AIDS. New Engl. J. Med. (1996) 334:426–431.
   Google Scholar
• HIRSCH MS, D'AQUILA RT: Therapy for human immuno-deficiency virus infection. New Engl. J. Med. (1992) 328:1686–1695.
   Web of Science ®Google Scholar
• COHEN J: Results on the new AIDS drugs bring cautious optimism. Science (1996) 271:755–756.
   PubMed Web of Science ®Google Scholar
• KIM EE, BAKER CT, DWYER MD et al.: Crystal structure of HIV-1 protease in the complex with VX-478, a potent and orally bioavailable inhibitor of the enzyme. J. Am. Chem. Soc. (1995) 117:1181–1182.
   Web of Science ®Google Scholar
• VERTEX: Company News Letter (1995).
   Google Scholar
• STONE D: HIV protease inhibitors head to market. Bio/Technology (1995) 13(91:940–942.
   PubMedGoogle Scholar
• HAMBRECHT & QUIET: Harnbrecht & Quist health care conference. San Francisco, (January 7–10, 1996).
   Google Scholar
• BORMAN S: Clinical trials to begin on designed AIDS drug. Chem. Eng. News (Februaiy 13, 1995):39–40.
   Google Scholar
• LIVINGSTON DJ, PAZHANISAMY S, PORTER DJ et al.: Weak binding of VX-478 to human plasma proteins and im-plications for anti-human immunodeficiency virus therapy. J. Infect. Dis. (1995) 172:1238–1245.
   Google Scholar
• PARTALEDIS JA, YAMAGUCHI K, TISDALE M et al.: In vitroselection and characterisation of human immunodefi-ciency virus type 1 (HIV-1) isolates with reduced sensi-tivity to hydroxyethylamino sulfonamide inhibitors of HIV-1 aspartyl protease. J. Virology (1995) 69(9):5228–5235.
   Google Scholar
• CLAW MU, ST MILLARD J, ROONEY J: In vitro antiviralactivity of 141W94 (VX-478) in combination with other antiretroviral agents. Antiviral Res. (1996) 29:53–56.
   PubMed Web of Science ®Google Scholar
• VERTEX PHARMACEUTICALS INC.: Glaxo Wellcome be-gins Phase 1/II clinical trials with Vertex Pharmaceuti-cals' protease inhibitor for WV. Press Release (December 14, 1995),
   Google Scholar
• KALISH V3, KALDOR 5, SHETTY B et al.: Iterative protein structure-based drug design and synthesis of HIV pro-tease inhibitors. Int. Symp. Med. Chem. (1994). ML8.
   Google Scholar
• 'CALDER SW, KALISH VJ, DRESSMAN BA et al.: Design and synthesis of potent, orally bioavailable 111V-1 protease Inhibitors. Am. Chem. Soc. (1994) MEDI 17.
   Google Scholar
• TATLOCK JH, KALISH VJ, DAVIES J et al.: Protein struc-ture-based drug design and synthesis of nonpeptide HIV protease inhibitors. 209th Meeting Am. Chem. Soc. Anaheim, (April 1995). Abstract 120.
   Google Scholar
• PATRICK AK, MO H, MARKOWITZ M et al.: Antiviral andresistance studies of AG-1343, an orally bioavailable Inhibitor of human immunodeficiency virus protease. Antimicrob. Agents Chemother. (1996) 40:292–297.
   PubMed Web of Science ®Google Scholar
• YOULE M, MOYLE G, CHAPMAN S et al.: Phasestudyof AG-1343 a novel HIV protease inhibitor. Can.J. Infect. Dis. (1996) 6(Suppl. C). Abstract 2160.
   Google Scholar
• AGOURON PHARMACUTICALS, INC.: Pilot Phase II resultsreported for anti-HIV drug AG-1343 at the 35th Inter-science Conference On Antimicrobial Agents And Che-motherapy. Press Release (September 18, 1995).
   Google Scholar
• AGOURON PHARMACEUTICALS, INC.: Agouron's anti-WV drug AG-1343 shown to be active and well tolerated in British pilot Phase II study. Press Release (July 18, 1995).
   Google Scholar
• UBS BIOTECH ANALYSTS MEETING: UBS securities life science conference. New York, (October 17–18, 1995).
   Google Scholar
• AGOURON PHARMACEUTICALS, INC.: Agouron initiates pivotal Phase WHI clinical trials of anti-HIV drug Vira-ceptTm. Press Release (January 30, 1996).
   Google Scholar
• ABRAHAM A, ANDERSON PC, BEAULIU PL et al.: Prepara-tion of (2S, 4R)-4-hydroxypipecolic acid and deriva-tives: high affinity P[11-P[21 ligands for HIV protease Inhibitors. 210th Meeting Am. Chem. Soc. Chicago (August 20–24, 1995). MEDI 29.
   Google Scholar
• LAMARRE D: BELA 2011: an HIV protease inhibitor opti-mized for potent antiviral activity and good oral bioavailability. Can. J. Infect. Dis. (1995) 6(Suppl. C). Abstract 0496.
   Google Scholar
• ABRAHAM A, ANDERSON PC, BEAULIU PL et al.: Synthesisof palinavir, a new HIV protease inhibitor. 211th Meeting Am. Chem. Soc. New Orleans, (March 24–28, 1996). MEDI 13.
   Google Scholar
• MIMOTO T, IMAI J, KISANUKI S: Kynostatin KNI-227 and-272, highly potent anti-HIV agents: conformationally constrained tripepticle inhibitors of WV protease con-taining allophenylnorstatine. Chem. Pharm. Bull. (1992) 40:2251–2253.
   PubMed Web of Science ®Google Scholar
• KAGEYAMA S, MIMOTO T, MURAKAWA Y: In vitro anti-human immunodeficiency virus (HIV) activities of tran-sition state mimetic HIV protease inhibitors containing allophenylnorstatine. Antimicrob. Agents Chemother. (1993) 37:810–817.
   PubMed Web of Science ®Google Scholar
• KAGEYAMA S, ANDERSON BD, HOESTEREY BL et al.: Protein binding of human immunodeficiency virus protease inhibitor KNI-272 and alteration of its in vitro anti-retroviral activity in the presence of high concen-trations of proteins. Antimicrob. Agents Chemother. (1994) 38(5):1107–1111.
   PubMed Web of Science ®Google Scholar
• UENO T, MITSUYA H: Current status of the developmentof HIV protease inhibitors and their clinical potential Clin. Immunother. (1995) 4(6):451–461.
   Google Scholar
• GULNIK SV, SUVOROV LI, LIU B et al,: Kinetic charac-terization and cross resistance patterns of IHV-1 pro-tease mutants selected under drug pressure. Biochemistry (1995) 34:9282–9287.
   PubMed Web of Science ®Google Scholar
• Japan Energy's AIDS drug undergoes clinical trials in Britain. Pharma.Jpn. (December 18, 1995) 19: 1480.
   Google Scholar
• LAM PY, JADHAV PK, EYERMANN g et al.: Rational design of potent bioavailable non-peptide cyclic ureas as IHV protease inhibitors. Science (1994) 263:380–384.
   Google Scholar
• WINSLOW DL, REID CD, GARBER S et al.: DMP-450, anewcyclic urea inhibitor of HIV protease with potent in vitro antiviral activity. Antiviral Res. (1995) 26(3):22.
   Google Scholar
• ERICKSON-VITANEN S, HODGE CN, ALDRICH PE et al.:Cyclic urea inhibitors of HIV protease. Second National Conference On Human Retroviruses And Related Infections, Am. Soc. Microbiology Meeting. Washington DC, (January 29-February 2, 1995). Abstract 96.
   Google Scholar
• WHITE SJ, ROBINSON CA, SHUM L et al.: Pharmacokinet-ics, safety and tolerance of DMP-450 single oral doses In healthy male subjects. J. Clin. Pharmacol. (1995) 35\(Suppl. 9). Abstract 51.
   Google Scholar
• THAISRIVONGS S, TOMICH PK, WATENPAUGH ICD et al.: Structure-based design of IIW protease inhibitors: 4-hy-droxycoumarines and 4-hydroxy-2-pyrones as non-peptidic inhibitors. J. Med. Chem. (1994) 37:3200–3204.
   PubMed Web of Science ®Google Scholar
• THAISRIVONGS S, WATENPUAGH ICD, HOWE WJ et al.: Structure-based design of novel HIV protease inhibi-tors: carboxamide-containing 4-hydroxycoumarines and 4-hydroxy-2-pyrones as potent nonpeptidic inhibi-tors. J. Med. Chem. (1995) 38:3624–3637.
   PubMed Web of Science ®Google Scholar
• ROMINES KR, WATENPAUGH ICD, HOWE WJ et al.: Struc-ture-based design of nonpeptidic HIV protease inhibi-tors from cyclooctylpyrone lead structure. J. Med. Chem. (1995) 38:4463–4473.
   PubMed Web of Science ®Google Scholar
• SKULNICK HI, JOHNSON PD, HOWE WJ et al.: Structure-based design of sulfonamide-substituted non-peptidic HIV protease inhibitors J. Med. Chem. (1995) 38:4968–4971.
   Web of Science ®Google Scholar
• ROMINES KR, CHRUSCIEL RA: 4-Hydroxypyrones and related templates as nonpeptidic HIV protease inhibi-tors. CUM Med. Chem. (1995) 2:825–838.
   Web of Science ®Google Scholar
• SKULNICK HI, JOHNSON PD, ARISTOFF PA et al.: Design, synthesis and SAR of novel HIV protease inhibitors for the treatment of AIDS. 210th Meeting Am. Chem. Soc. Chicago, (August 20–24, 1995). Abstract 009.
   Google Scholar
• BORIN MT, BATTS DH, PEEL BG et al.: U-103017, Phase I, single-dose, randomized, double-blind, safety tolerance and pharmacokinetics of several oral formulation in healthy volunteers. ICAAC (September 17–20, 1995). Ab-stract 128.
   Google Scholar
• CAPRARO HG, BOLD G, FASSLER A et al.: CGP 61755:synthesis and biological profile. 211th Meeting Am . Chem Soc. New Orleans, (March 24–28, 1996). MEDI 160.
   Google Scholar
• MOLLA A, KEMPF DJ, KORNEYEVA M et al.: Ordered accumulation of mutations in HIV protease confers resistance to ritonavir. Nature Medicine (1996). In Press.
   Google Scholar