메뉴 건너뛰기




Volumn 5, Issue 1, 2007, Pages 67-75

Role of integrase inhibitors in the treatment of HIV disease

Author keywords

Antiviral resistance; HAART; HIV infection; HIV RNA; Integrase; Integrase inhibitors

Indexed keywords

1 [5 (4 FLUOROBENZYL) 2 FURYL] 3 (1,2,4 TRIAZOL 3 YL) 1,3 PROPANEDIONE; 4 [1 (4 FLUOROBENZYL) 2 PYRROLYL] 2,4 DIOXOBUTYRIC ACID; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; ANTIRETROVIRUS AGENT; ANTIVIRUS AGENT; ATAZANAVIR; BETA DIKETOACID DERIVATIVE; EFAVIRENZ; ENFUVIRTIDE; ETRAVIRINE; FZ 41; GS 9137; GSK 810871; INTEGRASE INHIBITOR; JTK 303; L 708906; L 870812; L 900612; LAMIVUDINE; LIPID; MK 0518; N (4 FLUOROBENZYL) 8 HYDROXY 5 (TETRAHYDRO 2H 1,2 THIAZIN 2 YL) 1,6 NAPHTHYRIDINE 7 CARBOXAMIDE S,S DIOXIDE; NAPHTHYRIDINE DERIVATIVE; PLACEBO; RIFAMPICIN; RITONAVIR; RNA DIRECTED DNA POLYMERASE; TENOFOVIR; UNCLASSIFIED DRUG; UNINDEXED DRUG; ZIDOVUDINE;

EID: 33947715164     PISSN: 14787210     EISSN: 17448336     Source Type: Journal    
DOI: 10.1586/14787210.5.1.67     Document Type: Review
Times cited : (23)

References (47)
  • 1
    • 0023268502 scopus 로고
    • The efficacy of azidothymidine (AZT) in the treatment of patients with AIDS and AIDS-related complex. A double-blind, placebo-controlled trial
    • Fischl MA, Richman DD, Grieco MH 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. 317, 185-191 (1987).
    • (1987) N. Engl. J. Med , vol.317 , pp. 185-191
    • Fischl, M.A.1    Richman, D.D.2    Grieco, M.H.3
  • 2
    • 0030567824 scopus 로고    scopus 로고
    • Delta: A randomised double-blind controlled trial comparing combinations of zidovudine plus didanosine or zalcitabine with zidovudine alone in HIV-infected individuals
    • Delta coordinating committee
    • Delta coordinating committee. Delta: a randomised double-blind controlled trial comparing combinations of zidovudine plus didanosine or zalcitabine with zidovudine alone in HIV-infected individuals. Lancet 348, 283-291 (1996).
    • (1996) Lancet , vol.348 , pp. 283-291
  • 3
    • 0442268112 scopus 로고    scopus 로고
    • A controlled trial of two nucleoside analogues plus indinavir in persons with human immunodeficiency virus infection and CD4 cell counts of 200 per cubic millimeter or less. AIDS Clinical Trials Group 320 Study Team
    • Hammer SM, Squires KE, Hughes MD et al. A controlled trial of two nucleoside analogues plus indinavir in persons with human immunodeficiency virus infection and CD4 cell counts of 200 per cubic millimeter or less. AIDS Clinical Trials Group 320 Study Team. N. Engl. J. Med. 337, 725-733 (1997).
    • (1997) N. Engl. J. Med , vol.337 , pp. 725-733
    • Hammer, S.M.1    Squires, K.E.2    Hughes, M.D.3
  • 4
    • 33745222568 scopus 로고    scopus 로고
    • The survival benefits of AIDS treatment in the United States
    • Walensky RP, Paltiel AD, Losina E. The survival benefits of AIDS treatment in the United States. J. Infect. Dis. 194, 11-19 (2006).
    • (2006) J. Infect. Dis , vol.194 , pp. 11-19
    • Walensky, R.P.1    Paltiel, A.D.2    Losina, E.3
  • 5
    • 23244454080 scopus 로고    scopus 로고
    • The global status of resistance to antiretroviral drugs
    • Vella S, Palmisano L. The global status of resistance to antiretroviral drugs. Clin. Infect. Dis. 41 (Suppl. 4), S239-S246 (2005).
    • (2005) Clin. Infect. Dis , vol.41 , Issue.SUPPL. 4
    • Vella, S.1    Palmisano, L.2
  • 6
    • 0029998897 scopus 로고    scopus 로고
    • Human endogenous retrovirus K10 encodes a functional integrase
    • Kitamura Y, Ayukawa T, Ishikawa T, Kanda T, Yoshiike K. Human endogenous retrovirus K10 encodes a functional integrase. J. Virol. 70, 3302-3306 (1996).
    • (1996) J. Virol , vol.70 , pp. 3302-3306
    • Kitamura, Y.1    Ayukawa, T.2    Ishikawa, T.3    Kanda, T.4    Yoshiike, K.5
  • 7
    • 0035343895 scopus 로고    scopus 로고
    • Comparative architecture of transposases and integrase complexes
    • Rice PA, Baker TA. Comparative architecture of transposases and integrase complexes. Nature Struct. Biol.. 8, 302-307 (2001).
    • (2001) Nature Struct. Biol , vol.8 , pp. 302-307
    • Rice, P.A.1    Baker, T.A.2
  • 8
    • 33745248642 scopus 로고    scopus 로고
    • The innernuclear-envelope protein emerin regulates HIV-1 infectivity
    • Jacque JM, Stevenson M. The innernuclear-envelope protein emerin regulates HIV-1 infectivity. Nature 441, 641-645 (2006).
    • (2006) Nature , vol.441 , pp. 641-645
    • Jacque, J.M.1    Stevenson, M.2
  • 9
    • 33746214675 scopus 로고    scopus 로고
    • Integration of human immunodeficiency virus type 1 in untreated infection occurs preferentially within genes
    • Liu H, Dow C E, Arora R et al. Integration of human immunodeficiency virus type 1 in untreated infection occurs preferentially within genes. J. Virol. 80, 7765-7768 (2006).
    • (2006) J. Virol , vol.80 , pp. 7765-7768
    • Liu, H.1    Dow, C.E.2    Arora, R.3
  • 10
    • 0030824458 scopus 로고    scopus 로고
    • New insight on the role of extrachromosomal retroviral DNA
    • Cara A, Reitz MS. New insight on the role of extrachromosomal retroviral DNA. Leukemia 11, 1395-1398 (1997).
    • (1997) Leukemia , vol.11 , pp. 1395-1398
    • Cara, A.1    Reitz, M.S.2
  • 11
    • 0033966504 scopus 로고    scopus 로고
    • Persistence of episomal HIV-1 infection intermediates in patients on highly active antiretroviral therapy
    • Sharkey, ME, Teo L, Greenough T et al. Persistence of episomal HIV-1 infection intermediates in patients on highly active antiretroviral therapy. Nat. Med. 6, 76-81 (2000).
    • (2000) Nat. Med , vol.6 , pp. 76-81
    • Sharkey, M.E.1    Teo, L.2    Greenough, T.3
  • 12
    • 26944490692 scopus 로고    scopus 로고
    • Decay of human immunodeficiency virus type 1 unintegrated DNA containg two long terminal repeats in infected individuals after 3 to 8 years of sustained control of viremia
    • McDermott J L, Martini I, Ferrari D et al. Decay of human immunodeficiency virus type 1 unintegrated DNA containg two long terminal repeats in infected individuals after 3 to 8 years of sustained control of viremia. J. Clin. Microbiol., 43, 5272-5274 (2005).
    • (2005) J. Clin. Microbiol , vol.43 , pp. 5272-5274
    • McDermott, J.L.1    Martini, I.2    Ferrari, D.3
  • 13
    • 2942553781 scopus 로고    scopus 로고
    • Structure and function of HIV-1 integrase
    • Chu TK, Davies DR. Structure and function of HIV-1 integrase. Curr. Top. Med. Chem. 4, 965-977 (2004).
    • (2004) Curr. Top. Med. Chem , vol.4 , pp. 965-977
    • Chu, T.K.1    Davies, D.R.2
  • 14
    • 13444269378 scopus 로고    scopus 로고
    • Genetic analyses of DNA-binding mutants in the catalytic core domain of human immunodeficiency virus type 1 integrase
    • Lu R, Limon A, Ghory HZ, Engelman A. Genetic analyses of DNA-binding mutants in the catalytic core domain of human immunodeficiency virus type 1 integrase. J. Virol. 79, 2493-2505 (2005).
    • (2005) J. Virol , vol.79 , pp. 2493-2505
    • Lu, R.1    Limon, A.2    Ghory, H.Z.3    Engelman, A.4
  • 15
    • 0026549933 scopus 로고
    • Reversal of integration and DNA splicing mediated by integrase of human immunodeficiency virus
    • Chow SA, Vincent KA, Elison V, Brown PO. Reversal of integration and DNA splicing mediated by integrase of human immunodeficiency virus. Science 255, 723-726 (1992).
    • (1992) Science , vol.255 , pp. 723-726
    • Chow, S.A.1    Vincent, K.A.2    Elison, V.3    Brown, P.O.4
  • 18
    • 0028303481 scopus 로고
    • A novel assay for the DNA strand-transfer reaction of HIV-1 integrase
    • Hazuda DJ, Hastings JC, Wolf AL, Emini EA. A novel assay for the DNA strand-transfer reaction of HIV-1 integrase. Nucleic Acids Res.. 22, 1121-1122 (1994).
    • (1994) Nucleic Acids Res , vol.22 , pp. 1121-1122
    • Hazuda, D.J.1    Hastings, J.C.2    Wolf, A.L.3    Emini, E.A.4
  • 20
    • 13044295993 scopus 로고    scopus 로고
    • Structure of the HIV-1 integrase catalytic domain complexed with an inhibitor: A platform for antiviral drug design
    • Goldgur Y, Craigie R, Cohen GH et al. Structure of the HIV-1 integrase catalytic domain complexed with an inhibitor: a platform for antiviral drug design. Proc. Natl Acad. Sci. USA 96, 13040-13043 (1999).
    • (1999) Proc. Natl Acad. Sci. USA , vol.96 , pp. 13040-13043
    • Goldgur, Y.1    Craigie, R.2    Cohen, G.H.3
  • 21
    • 0034723439 scopus 로고    scopus 로고
    • Inhibitors of strand transfer that prevent integration and inhibit HIV replication in cells
    • Hazuda D, Felock P, Wilmer M et al. Inhibitors of strand transfer that prevent integration and inhibit HIV replication in cells. Science 287, 646-650 (2000).
    • (2000) Science , vol.287 , pp. 646-650
    • Hazuda, D.1    Felock, P.2    Wilmer, M.3
  • 22
    • 0037076324 scopus 로고    scopus 로고
    • Diketo acid inhibitor mechanism and HIV-1 integrase: Implications for metal binding in the active site of phosphotransferase enzymes
    • Grobler JA, Stillmock K, Hu B 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. USA 99, 6661-6666 (2002).
    • (2002) Proc. Natl Acad. Sci. USA , vol.99 , pp. 6661-6666
    • Grobler, J.A.1    Stillmock, K.2    Hu, B.3
  • 23
    • 10744226580 scopus 로고    scopus 로고
    • Development of resistance against diketo derivatives of human immunodeficiency virus type 1 by progressive accumulation of integrase mutations
    • Fikkert V, Van Maele B, Vercammen J et al. Development of resistance against diketo derivatives of human immunodeficiency virus type 1 by progressive accumulation of integrase mutations. J. Virol. 77, 11459-11470 (2003).
    • (2003) J. Virol , vol.77 , pp. 11459-11470
    • Fikkert, V.1    Van Maele, B.2    Vercammen, J.3
  • 24
    • 3843108916 scopus 로고    scopus 로고
    • A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase
    • Hazuda D, Anthony NJ, Gomez RP et al. A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase. Proc. Natl Acad. Sci. USA 101, 11233-11238 (2004).
    • (2004) Proc. Natl Acad. Sci. USA , vol.101 , pp. 11233-11238
    • Hazuda, D.1    Anthony, N.J.2    Gomez, R.P.3
  • 25
    • 3242769788 scopus 로고    scopus 로고
    • Integrase inhibitors and cellular immunity suppress retroviral replication in rhesus macaques
    • Hazuda DJ, Young SD, Guare JP et al. Integrase inhibitors and cellular immunity suppress retroviral replication in rhesus macaques. Science 305, 528-532 (2004).
    • (2004) Science , vol.305 , pp. 528-532
    • Hazuda, D.J.1    Young, S.D.2    Guare, J.P.3
  • 26
    • 24344490276 scopus 로고    scopus 로고
    • A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6] naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells
    • Embrey MW, Way JS, Funk TW et al. A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6] naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells. Bioorg. Med. Chem. Lett. 15, 4550-4554 (2005).
    • (2005) Bioorg. Med. Chem. Lett , vol.15 , pp. 4550-4554
    • Embrey, M.W.1    Way, J.S.2    Funk, T.W.3
  • 27
    • 33644863638 scopus 로고    scopus 로고
    • Novel HIV-1 integrase inhibitors derived from quinolone antibiotics
    • Sato M, Motomura T, Aramaki H et al. Novel HIV-1 integrase inhibitors derived from quinolone antibiotics. J. Med. Chem. 49, 1506-1508 (2006).
    • (2006) J. Med. Chem , vol.49 , pp. 1506-1508
    • Sato, M.1    Motomura, T.2    Aramaki, H.3
  • 28
    • 0037303182 scopus 로고    scopus 로고
    • S-1360 Shionogi-GlaxoSmithKline
    • Billich A. S-1360 Shionogi-GlaxoSmithKline. Curr. Opin. Investig. Drugs 4, 206-209 (2003).
    • (2003) Curr. Opin. Investig. Drugs , vol.4 , pp. 206-209
    • Billich, A.1
  • 29
    • 4844227300 scopus 로고    scopus 로고
    • Nuclear import of HIV-1 integrase is inhibited in vitro by styrylquinoline derivatives
    • Mousnier A, Leh H, Nouscadet JF, Dergemont C. Nuclear import of HIV-1 integrase is inhibited in vitro by styrylquinoline derivatives. Mol. Pharmacol. 66, 783-788 (2004).
    • (2004) Mol. Pharmacol , vol.66 , pp. 783-788
    • Mousnier, A.1    Leh, H.2    Nouscadet, J.F.3    Dergemont, C.4
  • 31
    • 33845366857 scopus 로고    scopus 로고
    • Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment- naive HIV-1-infected individuals
    • Markowitz M, Morales-Ramirez JO, Nguyen B-J et al. Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment- naive HIV-1-infected individuals. J. Acquir. Immune Defic. Syndr. 43, 509-515 (2006).
    • (2006) J. Acquir. Immune Defic. Syndr , vol.43 , pp. 509-515
    • Markowitz, M.1    Morales-Ramirez, J.O.2    Nguyen, B.-J.3
  • 32
    • 34247219970 scopus 로고    scopus 로고
    • Grinsztejn B, Nguyen BY, Katlama C et al. Potent antiretroviral effect of MK-0518, a novel HIV-1 integrase inihibitor, in patients with triple-class resistant virus. Proceedings of the 13th Conference on Retroviruses and Opportunistic Infection. CO, USA February 5-8 Abstr. 159LB (2006).
    • Grinsztejn B, Nguyen BY, Katlama C et al. Potent antiretroviral effect of MK-0518, a novel HIV-1 integrase inihibitor, in patients with triple-class resistant virus. Proceedings of the 13th Conference on Retroviruses and Opportunistic Infection. CO, USA February 5-8 Abstr. 159LB (2006).
  • 33
    • 34247262327 scopus 로고    scopus 로고
    • Grinsztejn B Nguyen BY, Katlama C et al. Potent antiretroviral effect of MK-0518, a novel HIV-1 integrase inhibitor, in patients with triple class resistant virus. Proceedings of the 46th ICAAC, CA, USA, September 27-30, Abstr. H-1670b (2006).
    • Grinsztejn B Nguyen BY, Katlama C et al. Potent antiretroviral effect of MK-0518, a novel HIV-1 integrase inhibitor, in patients with triple class resistant virus. Proceedings of the 46th ICAAC, CA, USA, September 27-30, Abstr. H-1670b (2006).
  • 34
    • 34247263533 scopus 로고    scopus 로고
    • Markowitz M, Nguyen B-Y, Gotuzzo F et al. Potent antiretroviral effect of MK-0518, a novel HIV-1 integrase inhibitor, as part of combination ART in treatment naive HIV-1 infected patients. Proceedings of the XVI Internatinal AIDS Conference, Toronto (Canada) August 13-18, Abstr. THLB0214 (2006).
    • Markowitz M, Nguyen B-Y, Gotuzzo F et al. Potent antiretroviral effect of MK-0518, a novel HIV-1 integrase inhibitor, as part of combination ART in treatment naive HIV-1 infected patients. Proceedings of the XVI Internatinal AIDS Conference, Toronto (Canada) August 13-18, Abstr. THLB0214 (2006).
  • 35
    • 34247252726 scopus 로고    scopus 로고
    • Minimal effect of ritonavir (RTV) and efavirenz (EFV) on the pharmacokinetics (OK) of MK0-518, San Francisco (CA) September 27-30, Abstr. A-373
    • Iwamoto M, Wenning LA, Petry SA et al. Minimal effect of ritonavir (RTV) and efavirenz (EFV) on the pharmacokinetics (OK) of MK0-518. Proceedings of the 46th ICAAC, San Francisco (CA) September 27-30, Abstr. A-373 (2006).
    • (2006) Proceedings of the 46th ICAAC
    • Iwamoto, M.1    Wenning, L.A.2    Petry, S.A.3
  • 36
    • 34247201278 scopus 로고    scopus 로고
    • Effect of tipranavir, ritonavir (tpv, rtv) on pharmacokinetics of MK-0518, CA, USA, September 27-30, Abstr. A-374
    • Wenning LA, Hanley H, Stone J et al. Effect of tipranavir + ritonavir (tpv + rtv) on pharmacokinetics of MK-0518. Proceedings of the 46th ICAAC, CA, USA, September 27-30, Abstr. A-374 (2006).
    • (2006) Proceedings of the 46th ICAAC
    • Wenning, L.A.1    Hanley, H.2    Stone, J.3
  • 37
    • 34247228339 scopus 로고    scopus 로고
    • Wenning LA, Friedman E Kost JT. Lack of a significant drug interaction between MK-0518 and tenofovir disoproxil fumarate (TDF). Proceedings of the 46th ICAAC, CA, USA September 27-30, Abstr. A-375 (2006)
    • Wenning LA, Friedman E Kost JT. Lack of a significant drug interaction between MK-0518 and tenofovir disoproxil fumarate (TDF). Proceedings of the 46th ICAAC, CA, USA September 27-30, Abstr. A-375 (2006)
  • 38
    • 33748113778 scopus 로고    scopus 로고
    • Antiviral activity, pharmacokinetics, and dose response of the HIV integrase inhibitor GS-9137 (JTK-303) in treatment-naive and treatment-experienced patients
    • DeJesus E, Berger D, Markowitz M et al. Antiviral activity, pharmacokinetics, and dose response of the HIV integrase inhibitor GS-9137 (JTK-303) in treatment-naive and treatment-experienced patients. J. Acquir. Immune Defic. Syndr. 43, 1-5 (2006).
    • (2006) J. Acquir. Immune Defic. Syndr , vol.43 , pp. 1-5
    • DeJesus, E.1    Berger, D.2    Markowitz, M.3
  • 39
    • 29144452574 scopus 로고    scopus 로고
    • The normalized inhibitory quotient of boosted protease inhibitors is predictive of viral load response in treatment-experienced HIV-1-infected individuals
    • Winston A, Hales G, Amin J et al. The normalized inhibitory quotient of boosted protease inhibitors is predictive of viral load response in treatment-experienced HIV-1-infected individuals. AIDS 19, 1393-1399 (2005).
    • (2005) AIDS , vol.19 , pp. 1393-1399
    • Winston, A.1    Hales, G.2    Amin, J.3
  • 40
    • 7744240084 scopus 로고    scopus 로고
    • Multiple mutations in human immunodeficiency virus-1 integrase confer resistance to the clinical trial drug S-1360
    • Fikkert V, Hombrouck A, Van Remoortel B et al. Multiple mutations in human immunodeficiency virus-1 integrase confer resistance to the clinical trial drug S-1360. AIDS 18, 2019-2028 (2004).
    • (2004) AIDS , vol.18 , pp. 2019-2028
    • Fikkert, V.1    Hombrouck, A.2    Van Remoortel, B.3
  • 41
    • 33747810757 scopus 로고    scopus 로고
    • Context dependent effects of mutations associated with resistance to inhibitors of HIV-1 integrase strand transfer
    • and the MRL HIV-1 Drug Discovery Team, S
    • Hazuda DJ and the MRL HIV-1 Drug Discovery Team. Context dependent effects of mutations associated with resistance to inhibitors of HIV-1 integrase strand transfer. Antiviral Ther. 10, S82, (2005).
    • (2005) Antiviral Ther , vol.10 , pp. 82
    • Hazuda, D.J.1
  • 42
    • 34247202879 scopus 로고    scopus 로고
    • Natural polymorphism of the HIV-1 integrase gene and mutations associated with integrase inhibitor resistance
    • S
    • Lataillade M, Chiarella J, Kozal MJ. Natural polymorphism of the HIV-1 integrase gene and mutations associated with integrase inhibitor resistance. Antiviral Ther. 11, S28 (2006).
    • (2006) Antiviral Ther , vol.11 , pp. 28
    • Lataillade, M.1    Chiarella, J.2    Kozal, M.J.3
  • 43
    • 34247244405 scopus 로고    scopus 로고
    • Natural variation in susceptibility of patient-derived HIV-1 to an integrase strand transfer inhibitor
    • S
    • Fransen S, Gupta S, Paxinos E et al. Natural variation in susceptibility of patient-derived HIV-1 to an integrase strand transfer inhibitor. Antiviral Ther. 11, S27 (2006).
    • (2006) Antiviral Ther , vol.11 , pp. 27
    • Fransen, S.1    Gupta, S.2    Paxinos, E.3
  • 44
    • 33645405333 scopus 로고    scopus 로고
    • Novel bifunctional quinolonyl diketo acid derivatives as HIV-1 integrase inhibitors: Design, synthesis, biological activities and mechanism of actions
    • Di Santo R, Costi R, Roux A et al. Novel bifunctional quinolonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, biological activities and mechanism of actions. J. Med. Chem. 49, 1939-1945 (2006).
    • (2006) J. Med. Chem , vol.49 , pp. 1939-1945
    • Di Santo, R.1    Costi, R.2    Roux, A.3
  • 46
    • 34047148544 scopus 로고    scopus 로고
    • Chemokine antagonists as therapeutics: Focus on HIV-1
    • Tsibris AM, Kuritzkes DR. Chemokine antagonists as therapeutics: focus on HIV-1. Annu. Rev. Med. 58, 445-459 (2007).
    • (2007) Annu. Rev. Med , vol.58 , pp. 445-459
    • Tsibris, A.M.1    Kuritzkes, D.R.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.