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Review

Inhibitors of HIV-1 protease: 10 years after

, , &
Pages 1067-1091 | Published online: 26 Jul 2006

Bibliography

  • DE CLERCQ E: New approaches toward anti-HIV chemotherapy. J. Med. Chem. (2005) 48:1297-1313.
  • DE CLERCQ E: Antivirals and antiviral strategies. Nature Drug Discov. (2002) 1:13-25.
  • RICHMAN DD: HIV chemotherapy. Nature (2001) 410:995-1001.
  • BARBARO G, SCOZZAFAVA A, MASTROLORENZO A, SUPURAN CT: Highly active antiretroviral therapy: current state of the art, new agents and their pharmacological interactions useful for improving therapeutic outcome. Curr. Pharm. Des. (2005) 11:1805-1843.
  • DE CLERCQ E: New developments in anti-HIV chemotherapy. Curr. Med. Chem. (2001) 8:1543-1572.
  • SCOZZAFAVA A, OWA T, MASTROLORENZO A, SUPURAN CT: Anticancer and antiviral sulfonamides. Curr. Med. Chem. (2003) 10:925-953.
  • GREENE WC, PETERLIN M: Charting HIV's remarkable voyage through the cell: basic science as a passport to future therapy. Nature Med. (2002) 8:673-680.
  • SHEEHY AM, GADDIS NC, MALIM MH: The antiretroviral enzyme APOBEC3G is degraded by the proteasome in response to HIV-1 Vif. Nature Med. (2003) 9:1404-1407.
  • MARIN M, ROSE KM, KOZAK SL, KABAT D: HIV-1 Vif protein binds the editing enzyme APOBEC3G and induces its degradation. Nature Med. (2003) 9:1398-1403.
  • ZHANG H, YANG B, POMERANTZ RJ, ZHANG C, ARUNACHALAM SC, GAO L: The cytidine deaminase CEM15 induces hypermutation in newly synthesized HIV-1 DNA. Nature (2003) 424:94-98.
  • OGDEN RC, FLEXNER CW: Protease Inhibitors in AIDS Therapy. (Eds) Marcel Dekker, New York, Basel, USA (2001).
  • ERICKSON JW: HIV-1 protease as a target for AIDS therapy. In: Protease inhibitors in AIDS therapy. Ogden RC, Flexner CW (Eds) Marcel Dekker, New York, USA (2001):1-25.
  • SCOZZAFAVA A, MASTROLORENZO A, SUPURAN CT: Non-peptidic chemokine receptors antagonists as emerging anti-HIV agents. J. Enzyme Inhib. Med. Chem. (2002) 17:69-76.
  • SCHECHTER I, BERGER A: On the size of the active site in proteases. Biochem. Biophys. Res. Commun. (1967) 27:157-162.
  • CASINI A, SCOZZAFAVA A, SUPURAN CT: Sulfonamide derivatives with protease inhibitory action as anticancer, antiinflammatory and antiviral agents. Expert Opin. Ther. Pat. (2002) 12:1307-1327.
  • SUPURAN CT, CASINI A, SCOZZAFAVA A: Protease inhibitors of the sulfonamide type: anticancer, anti-inflammatory and antiviral agents. Med. Res. Rev. (2003) 23:535-558.
  • WLODAWER A, GUSTCHINA A: Structural and biochemical studies of retroviral proteases. Biochim. Biophys. Acta. (2000) 1477:16-34.
  • TOMASSELLI AG, HEINRIKSON RL: Targeting the HIV-protease in AIDS therapy: a current clinical perspective. Biochim. Biophys. Acta (2000) 1477:189-214.
  • DUNCAN IB, REDSHAW S: Discovery and early development of saquinavir. In: Protease inhibitors in AIDS therapy. Ogden RC, Flexner CW (Eds) Marcel Dekker, New York, USA (2001):27-47.
  • KEMPF DJ: Discovery and early development of ritonavir and ABT-378. In: Protease inhibitors in AIDS therapy. Ogden RC, Flexner CW (Eds) Marcel Dekker, New York, USA (2001):49-64.
  • DORSEY BD, VACCA JP: Discovery and early development of indinavir. In: Protease inhibitors in AIDS therapy. Ogden RC, Flexner CW (Eds) Marcel Dekker, New York, USA (2001):65-83.
  • REICH SH: Discovery and early development of nelfinavir (Viracept). In: Protease inhibitors in AIDS therapy. Ogden RC, Flexner CW (Eds) Marcel Dekker, New York, USA (2001):85-99.
  • TUNG RD, LIVINGSTON DJ, RAO BG et al.: Design and synthesis of amprenavir, a novel HIV protease inhibitor. In: Protease inhibitors in AIDS therapy. Ogden RC, Flexner CW (Eds) Marcel Dekker, New York, USA (2001):101-118.
  • CHRUSCIEL RA, THAISRIVONGS S, NICHOLAS JA: HIV protease inhibitors in early development. In: Protease inhibitors in AIDS therapy. Ogden RC, Flexner CW (Eds), Marcel Dekker, New York, USA (2001):119-137.
  • QAZI NA, MORLESE JF, POZNIAK AL: Lopinavir/ritonavir (ABT-378/r). Exp. Opin. Pharmacother. (2002) 3:315-327.
  • RUSCONI S, LA SETA CATAMANCIO S: HIV-1 protease inhibitors in development. Expert Opin. Investig. Drugs (2002) 11:387-395.
  • WITHERELL G: BMS-232632 (Novartis/Bristol-Myers Squibb). Curr. Opin. Invest. Drugs (2001) 2:340-347.
  • PILIERO PJ: Atazanavir: a novel HIV-1 protease inhibitor. Expert Opin. Investig. Drugs (2002) 11:1295-1301.
  • GATELL JM: From amprenavir to GW433908. J. HIV Ther. (2001) 6:95-99.
  • QUERCIA R, GARNIER E, FERRE V et al.: Salvage therapy with ritonavir- boosted amprenavir/fosamprenavir: virological and immunological response in 2 years follow-up. HIV Clin. Trials (2005) 6:73-80.
  • ARVIEUX C, TRIBUT O: Amprenavir or fosamprenavir plus ritonavir in HIV infection: pharmacology, efficacy and tolerability profile. Drugs (2005) 65:633-659.
  • BECKER S, THORNTON L: Fosamprenavir: advancing HIV protease inhibitor treatment options. Expert Opin. Pharmacother. (2004) 5:1995-2005.
  • FLEXNER CW: Pharmacology and drug interactions of HIV protease inhibitors. In: Protease inhibitors in AIDS therapy. Ogden RC, Flexner CW (Eds) Marcel Dekker, New York, USA (2001):139-159.
  • FLEXNER CW: Beneficial pharmacokinetic interactions: are two protease inhibitors better than one ? In: Protease inhibitors in AIDS therapy. Ogden RC, Flexner CW (Eds) Marcel Dekker, New York, USA (2001):161-177.
  • KAPLAN SS, HICKS CB: Safety and antiviral activity of lopinavir/ritonavir-based therapy in human immunodeficiency virus type 1 (HIV-1) infection. J. Antimicrob. Chemother. (2005) 56:273-276.
  • BONFANTI P, MARTINELLI C, RICCI E et al.; CISAI GROUP (ITALIAN COORDINATORS FOR THE STUDY OF ALLERGIES HIV INFECTION): An Italian approach to postmarketing monitoring: preliminary results from the SCOLTA (Surveillance Cohort Long-Term Toxicity Antiretrovirals) project on the safety of lopinavir/ritonavir. J. Acquir. Immune Defic. Syndr. (2005) 39:317-20.
  • ARRIBAS JR, PULIDO F, DELGADO R et al.: Lopinavir/ritonavir as single-drug therapy for maintenance of HIV-1 viral suppression: 48-week results of a randomized, controlled, open-label, proof-of-concept pilot clinical trial (OK Study). J. Acquir. Immune Defic. Syndr. (2005) 40:280-287
  • ANANWORANICH J, KOSALARAKSA P, HILL A et al.; HIV-NAT 017 STUDY TEAM: Pharmacokinetics and 24-week efficacy/safety of dual boosted saquinavir/lopinavir/ritonavir in nucleoside-pretreated children. Pediatr. Infect. Dis. J. (2005) 24:874-879.
  • FUSTER D, CLOTET B: Review of atazanavir: a novel HIV protease inhibitor. Expert Opin. Pharmacother. (2005) 6:1565-1572
  • FELDT T, OETTE M, KROIDL A et al.: Atazanavir for treatment of HIV infection in clinical routine: efficacy, pharmacokinetics and safety. Eur. J. Med. Res. (2005) 10:7-10.
  • PILIERO PJ: Atazanavir: a novel once-daily protease inhibitor. Drugs Today. (2004) 40:901-912.
  • LE TIEC C, BARRAIL A, GOUJARD C, TABURET AM: Clinical pharmacokinetics and summary of efficacy and tolerability of atazanavir. Clin. Pharmacokinet. (2005) 44:1035-1050.
  • TURNER SR, STROHBACH JW, TOMMASI RA et al.: Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4- hydroxy-2-pyrone sulfonamide class. J. Med. Chem. (1998) 41:3467-3476.
  • RUSCONI S, LA SETA CATAMANCIO S, CITTERIO P et al.: Susceptibility to PNU-140690 (tipranavir) of human immunodeficiency virus type 1 isolates derived from patients with multidrug resistance to other protease inhibitors. Antimicrob. Agents Chemother. (2000) 44:1328-1332.
  • LARDER BA, HERTOGS K, BLOOR S et al.: Tipranavir inhibits broadly protease inhibitor-resistant HIV-1 clinical samples. AIDS (2000) 14:1943-1948.
  • BULGHERONI E, CITTERIO P, CROCE F et al.: Analysis of protease inhibitor combinations in vitro: activity of lopinavir, amprenavir and tipranavir against HIV type 1 wild-type and drug-resistant isolates. J. Antimicrob. Chemother. (2004) 53:464-468.
  • GHOSH AK, SHIN D, SWANSON L et al.: Structure-based design of non-peptide HIV protease inhibitors. Farmaco (2001) 56:29-32.
  • SURLERAUX DL, DE KOCK HA, VERSCHUEREN WG et al.: Design of HIV-1 protease inhibitors active on multidrug-resistant virus. J. Med. Chem. (2005) 48:1965-1973.
  • SURLERAUX DL, TAHRI A, VERSCHUEREN WG et al.: Discovery and selection of TMC-114, a next generation HIV-1 protease inhibitor J. Med. Chem. (2005) 48:1813-1822.
  • LO CICERO M, BULGHERONI E, ZAMPIERO A et al.: TMC114: in vitro activity against HIV-1 primary isolates with reduced susceptibility to multiple protease inhibitors. 7th International Congress on Drug Therapy in HIV Infection, Glasgow, Scotland. (2004) Abstract P315.
  • ARASTEH K, CLUMECK N, POZNIAK A et al.; TMC114-C207 STUDY TEAM: TMC114/ritonavir substitution for protease inhibitor(s) in a non-suppressive antiretroviral regimen: a 14-day proof-of-principle trial. AIDS (2005) 19:943-947.
  • KATLAMA C, BERGER D, BELLOS N et al.: Efficacy of TMC114/r in 3-class experienced patients with limited treatment options: 24-week planned interim analysis of 2 96-week multinational dose-finding trials. Proceedings of the 12th Conference on Retroviruses and Opportunistic Infections. Boston, MA, USA, Abstract 164LB (2005).
  • LEE YS, LEE YS, LEE JY, KIM SN, LEE CK, PARK H: 6-Hydroxy-1,3-dioxin- 4-ones as non-peptidic HIV protease inhibitors. Bioorg. Med. Chem. Lett (2000) 10:2625-2627.
  • HULTEN J, BONHAM NM, NILLROTH U et al.: Cyclic HIV-1 protease inhibitors derived from mannitol: synthesis, inhibitory potencies, and computational predictions of binding affinities. J. Med. Chem. (1997) 40:885-897.
  • BACKBRO K, LOWGREN S, OSTERLUND K et al.: Unexpected binding mode of a cyclic sulfamide HIV-1 protease inhibitor. J. Med. Chem. (1997) 40:898-902.
  • HULTEN J, ANDERSSON HO, SCHAAL W et al.: Inhibitors of the C(2)-symmetric HIV-1 protease: nonsymmetric binding of a symmetric cyclic sulfamide with ketoxime groups in the P2/P2' side chains. J. Med. Chem. (1999) 42:4054-4061.
  • AX A, SCHAAL W, VRANG L, SAMUELSSON B, HALLBERG A, KARLEN A: Cyclic sulfamide HIV-1 protease inhibitors, with sidechains spanning from P2/P2' to P1/P1'. Bioorg. Med. Chem. (2005) 13:755-764.
  • ALA PJ, CHANG CH: HIV aspartate proteinase: resistance to inhibitors. In: Proteinase and Peptidase Inhibition: Recent Potential Targets for Drug Development. Smith HJ, Simons C (Eds) Taylor & Francis Publishing House, London and New York, (2002):367-382.
  • CHOY N, CHOI H, JUNG WH et al.: Synthesis of irreversible HIV-1 protease inhibitors containing sulfonamide and sulfone as amide bond isosteres. Bioorg. Med. Chem. Lett. (1997) 7:2635-2638.
  • LU Z, BOHN J, RANO T et al.: Orally bioavailable highly potent HIV protease inhibitors against PI-resistant virus. Bioorg. Med. Chem. Lett. (2005) 15:5311-5314.
  • SHERRILL RG, FURFINE ES, HAZEN RJ et al.: Synthesis and antiviral activities of novel N-alkoxy- arylsulfonamide-based HIV protease inhibitors. Bioorg. Med. Chem. Lett. (2005) 15:3560-3564.
  • CIGLER P, KOZISEK M, REZACOVA P et al.: From nonpeptide toward noncarbon protease inhibitors: metallacarboranes as specific and potent inhibitors of HIV protease. Proc. Natl. Acad. Sci. USA (2005) 102:15394-15399.
  • SCHÜRMANN D, GATHE J, SANNE I, WOOD R ON BEHALF OF THE SOLO STUDY TEAM: Efficacy and safety of GW433908/ritonavir once daily in therapy-naïve subjects, 48 week results: the SOLO Study. 6th International Congress on Drug Therapy in HIV Infection, Glasgow, Scotland (2002), Abstract PL14.4.
  • FORD SL, REDDY YS, ANDERSON MT et al.: Single-dose safety and pharmacokinetics of brecanavir, a novel human immunodeficiency virus protease inhibitor. Antimicrob. Agents Chemother. (2006) 50:2201-2206.
  • CARR A: Toxicity of antiretroviral therapy and implications for drug development. Nature Rev. Drug Des. (2003) 2:624-634.
  • ROWE TC, WEISSIG V, LAWRENCE JW: Mitochondrial DNA metabolism targeting drugs. Advan. Drug Deliv. Rev. (2001) 49:175-187.
  • CARR A, SAMARAS K, THORISDOTTIR A, KAUFMANN GR, CHISHOLM DJ, COOPER DA: Diagnosis, prediction, and natural course of HIV-1 protease-inhibitor-associated lipodystrophy, hyperlipidaemia, and diabetes mellitus: a cohort study. Lancet (1999) 353:2093-2099.
  • JAIN RG, FURFINE ES, PEDNEAULT L, WHITE AJ, LEHNARD JM: Metabolic complications associated with antiretroviral therapy. Antivir. Res. (2001) 51:151-177.
  • BARBARO G: HIV infection, highly active antiretroviral therapy and the cardiovascular system. Cardiovas. Res. (2003) 60:87-95.
  • BARBARO G, KLATT EC: Highly active antiretroviral therapy and cardiovascular complications in HIV-infected patients. Curr. Pharm. Des. (2003) 9:1475-1481.
  • VOLBERDING PA, MURPHY RL, BARBARO G et al.: The Pavia consensus statement. AIDS (2003) 17:S170-S179.
  • CHAI H, YAN S, LIN P, LUMSDEN AB, YAO Q, CHEN C: Curcumin blocks HIV protease inhibitor ritonavir-induced vascular dysfunction in porcine coronary arteries. J. Am. Coll. Surg. (2005) 200:820-830.
  • CHAI H, ZHOU W, LIN P, LUMSDEN A, YAO Q, CHEN C: Ginsenosides block HIV protease inhibitor ritonavir-induced vascular dysfunction of porcine coronary arteries. Am. J. Physiol. Heart Circ. Physiol. (2005) 288:H2965-H2971.
  • BOSHOFF C, WEISS R: AIDS-related malignancies. Nature Rev. Cancer (2002) 2:373-382.
  • MONINI P, SGADARI C, TOSCHI E, BARILLARI G, ENSOLI B: Antitumour effects of antiretroviral therapy. Nature Rev. Cancer. (2004) 4:861-875.
  • CATTELAN AM, CALABRO ML, AVERSA SM et al.: Regression of AIDS-related Kaposi's sarcoma following antiretroviral therapy with protease inhibitors: biological correlates of clinical outcome. Eur. J. Cancer. (1999) 35:1809-1815.
  • SGADARI C, MONINI P, BARILLARI G, ENSOLI B: Use of HIV protease inhibitors to block Kaposi's sarcoma and tumour growth. Lancet Oncol. (2003) 4:537-547.
  • SGADARI C, BARILLARI G, TOSCHI E et al.: HIV protease inhibitors are potent anti-angiogenic molecules and promote regression of Kaposi sarcoma. Nat. Med. (2002) 8:225-232.
  • MONINI P, SGADARI C, BARILLARI G, ENSOLI B: HIV protease inhibitors: antiretroviral agents with anti-inflammatory, anti-angiogenic and anti-tumour activity. J. Antimicrob. Chemother. (2003) 51:207-211.
  • MAGGIORELLA L, WEN B, FRASCOGNA V, OPOLON P, BOURHIS J, DEUTSCH E: Combined radiation sensitizing and anti-angiogenic effects of ionizing radiation and the protease inhibitor ritonavir in a head and neck carcinoma model. Anticancer Res. (2005) 25:4357-4362.
  • GUPTA AK, CERNIGLIA GJ, MICK R, MCKENNA WG, MUSCHEL RJ: HIV protease inhibitors block Akt signaling and radiosensitize tumor cells both in vitro and in vitro. Cancer Res. (2005) 65:8256-8265.
  • YANG Y, IKEZOE T, TAKEUCHI T et al.: HIV-1 protease inhibitor induces growth arrest and apoptosis of human prostate cancer LNCaP cells in vitro and in vitro in conjunction with blockade of androgen receptor STAT3 and AKT signaling. Cancer Sci. (2005) 96:425-433.
  • POZIO E, MORALES MA: The impact of HIV-protease inhibitors on opportunistic parasites. Trends Parasitol. (2005) 21:58-63.
  • DE BERNARDIS F, TACCONELLI E, MONDELLO F et al.: Anti-retroviral therapy with protease inhibitors decreases virulence enzyme expression in vitro by Candida albicans without selection of avirulent fungus strains or decreasing their anti-mycotic susceptibility. FEMS Immunol. Med. Microbiol. (2004) 41:27-34.
  • MIGLIORATI CA, BIRMAN EG, CURY AE: Oropharyngeal candidiasis in HIV-infected patients under treatment with protease inhibitors. Oral. Surg. Oral. Med. Oral. Pathol. Oral. Radiol. Endod. Endod. (2004) 98:301-310.
  • ASENCIO MA, GARDUNO E, PEREZ-GIRALDO C, BLANCO MT, HURTADO C, GOMEZ-GARCIA AC: Exposure to therapeutic concentrations of ritonavir, but not saquinavir, reduces secreted aspartyl proteinase of Candida parapsilosis. Chemotherapy (2005) 51:252-255.
  • EQUILS O, SHAPIRO A, MADAK Z, LIU C, LU D: Human immunodeficiency virus type 1 protease inhibitors block toll-like receptor 2 (TLR2)- and TLR4-Induced NF-κB activation. Antimicrob. Agents Chemother. (2004) 48:3905-3911.
  • RIBERA E, AZUAJE C, LOPEZ RM et al.: Once-daily regimen of saquinavir, ritonavir, didanosine, and lamivudine in HIV-infected patients with standard tuberculosis therapy (TBQD Study). J. Acquir. Immune Defic. Syndr. (2005) 40:317-323.
  • KABBESH M, KOOMER A, MOLTENI A, AMAJOYI R, QUINN T, HERNDON B: The effect of treatment with a protease inhibitor on mycobacterial infection. Diagn. Microbiol. Infect. Dis. (2005) 51:251-258.
  • SKINNER-ADAMS TS, MCCARTHY JS, GARDINER DL, HILTON PM, ANDREWS KT: Antiretrovirals as antimalarial agents. J. Infect. Dis. (2004) 190:1998-2000.
  • PARIKH S, GUT J, ISTVAN E, GOLDBERG DE, HAVLIR DV, ROSENTHAL PJ: Antimalarial activity of human immunodeficiency virus type 1 protease inhibitors. Antimicrob. Agents Chemother. (2005) 49:2983-2985.
  • SAVARINO A: Expanding the frontiers of existing antiviral drugs: possible effects of HIV-1 protease inhibitors against SARS and avian influenza. J. Clin. Virol. (2005) 34:170-178.

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