메뉴 건너뛰기




Volumn 91, Issue 2, 2011, Pages 167-176

Resistance to raltegravir highlights integrase mutations at codon 148 in conferring cross-resistance to a second-generation HIV-1 integrase inhibitor

Author keywords

HIV 1; Integrase; MK 2048; Raltegravir; Resistance

Indexed keywords

2 [(3 CHLORO 4 FLUOROPHENYL)METHYL] 8 ETHYL 1,2,6,7,8,9 HEXAHYDRO 10 HYDROXY N,6 DIMETHYL 1,9 DIOXOPYRAZINO[1',2':1,5]PYRROLO[2,3 D]PYRIDAZINE 4 CARBOXAMIDE; 3 HYDROXY 4 OXO 4,6,7,8,9,10 HEXAHYDROPYRIMIDO[1,2 A]AZEPINE 2 CARBOXYLAMIDE; 9H PYRIDO[3,4 B]INDOLE 3 CARBOXAMIDE; ELVITEGRAVIR; INTEGRASE; INTEGRASE INHIBITOR; MK 2048; N (4 FLUOROBENZYL) 8 HYDROXY 5 (TETRAHYDRO 2H 1,2 THIAZIN 2 YL) 1,6 NAPHTHYRIDINE 7 CARBOXAMIDE S,S DIOXIDE; RALTEGRAVIR; UNCLASSIFIED DRUG; VIRUS DNA;

EID: 79959574846     PISSN: 01663542     EISSN: 18729096     Source Type: Journal    
DOI: 10.1016/j.antiviral.2011.05.011     Document Type: Article
Times cited : (28)

References (54)
  • 1
    • 55949107646 scopus 로고    scopus 로고
    • (No authors listed), Phase III trial begins for elvitegravir. AIDS Patient Care STDS 22, 762-763.
    • (No authors listed), 2008. Phase III trial begins for elvitegravir. AIDS Patient Care STDS 22, 762-763.
    • (2008)
  • 2
    • 77951672581 scopus 로고    scopus 로고
    • (No authors listed), FDA notifications. FDA approves raltegravir for HIV-1 treatment-naive patients. AIDS Alert 24, 106-107.
    • (No authors listed), 2009. FDA notifications. FDA approves raltegravir for HIV-1 treatment-naive patients. AIDS Alert 24, 106-107.
    • (2009)
  • 3
    • 38949110763 scopus 로고    scopus 로고
    • Raltegravir (MK-0518): a novel integrase inhibitor for the treatment of HIV infection
    • Anker M., Corales R.B. Raltegravir (MK-0518): a novel integrase inhibitor for the treatment of HIV infection. Expert. Opin. Investig. Drugs 2008, 17:97-103.
    • (2008) Expert. Opin. Investig. Drugs , vol.17 , pp. 97-103
    • Anker, M.1    Corales, R.B.2
  • 5
    • 79960146675 scopus 로고    scopus 로고
    • Potassium salt of an HIV integrase inhibitor. Merck, Patent WO2006060712.
    • Belyk, K.M., Morisson, H.G., Jones, P., Summa, V., 2006. Potassium salt of an HIV integrase inhibitor. Merck, Patent WO2006060712.
    • (2006)
    • Belyk, K.M.1    Morisson, H.G.2    Jones, P.3    Summa, V.4
  • 10
    • 74249083449 scopus 로고    scopus 로고
    • The SWITCHMRK studies: substitution of lopinavir/ritonavir with raltegravir in HIV-positive individuals
    • Cocohoba J. The SWITCHMRK studies: substitution of lopinavir/ritonavir with raltegravir in HIV-positive individuals. Expert Rev. Anti. Infect. Ther. 2009, 7:1159-1163.
    • (2009) Expert Rev. Anti. Infect. Ther. , vol.7 , pp. 1159-1163
    • Cocohoba, J.1
  • 12
    • 79960133863 scopus 로고    scopus 로고
    • Mutations patterns in the HIV-1 integrase related to virological failure on raltegravir-containing regimens, XVII International HIV Drug Resistance Workshop, Sitges, Spain.
    • Da Silva, D., Pellegrin, I., Anies, G., Breilh, D., Wittkop, L., Morlat, P., Dupon, M., Neau, D., Pellegrin, J.L., Fleury, H., Masquelier, B., 2008. Mutations patterns in the HIV-1 integrase related to virological failure on raltegravir-containing regimens, XVII International HIV Drug Resistance Workshop, Sitges, Spain.
    • (2008)
    • Da Silva, D.1    Pellegrin, I.2    Anies, G.3    Breilh, D.4    Wittkop, L.5    Morlat, P.6    Dupon, M.7    Neau, D.8    Pellegrin, J.L.9    Fleury, H.10    Masquelier, B.11
  • 14
    • 0026649557 scopus 로고
    • Identification of conserved amino acid residues critical for human immunodeficiency virus type 1 integrase function in vitro
    • Engelman A., Craigie R. Identification of conserved amino acid residues critical for human immunodeficiency virus type 1 integrase function in vitro. J. Virol. 1992, 66:6361-6369.
    • (1992) J. Virol. , vol.66 , pp. 6361-6369
    • Engelman, A.1    Craigie, R.2
  • 16
    • 0032601402 scopus 로고    scopus 로고
    • HIV integrase structure and function
    • Esposito D., Craigie R. HIV integrase structure and function. Adv. Virus Res. 1999, 52:319-333.
    • (1999) Adv. Virus Res. , vol.52 , pp. 319-333
    • Esposito, D.1    Craigie, R.2
  • 18
    • 77953022020 scopus 로고    scopus 로고
    • Primary mutations selected in vitro with raltegravir confer large fold changes in susceptibility to first-generation integrase inhibitors, but minor fold changes to inhibitors with second-generation resistance profiles
    • Goethals O., Vos A., Van Ginderen M., Geluykens P., Smits V., Schols D., Hertogs K., Clayton R. Primary mutations selected in vitro with raltegravir confer large fold changes in susceptibility to first-generation integrase inhibitors, but minor fold changes to inhibitors with second-generation resistance profiles. Virology 2010, 402:338-346.
    • (2010) Virology , vol.402 , pp. 338-346
    • Goethals, O.1    Vos, A.2    Van Ginderen, M.3    Geluykens, P.4    Smits, V.5    Schols, D.6    Hertogs, K.7    Clayton, R.8
  • 19
    • 77949365510 scopus 로고    scopus 로고
    • Retroviral intasome assembly and inhibition of DNA strand transfer
    • Hare S., Gupta S.S., Valkov E., Engelman A., Cherepanov P. Retroviral intasome assembly and inhibition of DNA strand transfer. Nature 2010, 464:232-236.
    • (2010) Nature , vol.464 , pp. 232-236
    • Hare, S.1    Gupta, S.S.2    Valkov, E.3    Engelman, A.4    Cherepanov, P.5
  • 23
    • 33947482804 scopus 로고
    • Nucleosides V. The monomesylates of 1-(2'-deoxy-bèta-d-lyxofuranosyl)thymidine
    • Horwitz J., Chua J., Noel M. Nucleosides V. The monomesylates of 1-(2'-deoxy-bèta-d-lyxofuranosyl)thymidine. J. Org. Chem. 1964, 29:2076-2078.
    • (1964) J. Org. Chem. , vol.29 , pp. 2076-2078
    • Horwitz, J.1    Chua, J.2    Noel, M.3
  • 26
    • 79960111344 scopus 로고    scopus 로고
    • HIV-integrase inhibitors, pharmaceutical compositions, and methods for their use. In: Agouron Pharmaceuticals, I., Patent US2005165040.
    • Kuki, A., Li, X., Plewe, M.B., Wang, H., Zhang, J., 2005. HIV-integrase inhibitors, pharmaceutical compositions, and methods for their use. In: Agouron Pharmaceuticals, I., Patent US2005165040.
    • (2005)
    • Kuki, A.1    Li, X.2    Plewe, M.B.3    Wang, H.4    Zhang, J.5
  • 27
    • 0026719238 scopus 로고
    • Residues critical for retroviral integrative recombination in a region that is highly conserved among retroviral/retrotransposon integrases and bacterial insertion sequence transposases
    • Kulkosky J., Jones K.S., Katz R.A., Mack J.P., Skalka A.M. Residues critical for retroviral integrative recombination in a region that is highly conserved among retroviral/retrotransposon integrases and bacterial insertion sequence transposases. Mol. Cell Biol. 1992, 12:2331-2338.
    • (1992) Mol. Cell Biol. , vol.12 , pp. 2331-2338
    • Kulkosky, J.1    Jones, K.S.2    Katz, R.A.3    Mack, J.P.4    Skalka, A.M.5
  • 28
    • 0026459411 scopus 로고
    • Requirement of active human immunodeficiency virus type 1 integrase enzyme for productive infection of human T-lymphoid cells
    • LaFemina R.L., Schneider C.L., Robbins H.L., Callahan P.L., LeGrow K., Roth E., Schleif W.A., Emini E.A. Requirement of active human immunodeficiency virus type 1 integrase enzyme for productive infection of human T-lymphoid cells. J. Virol. 1992, 66:7414-7419.
    • (1992) J. Virol. , vol.66 , pp. 7414-7419
    • LaFemina, R.L.1    Schneider, C.L.2    Robbins, H.L.3    Callahan, P.L.4    LeGrow, K.5    Roth, E.6    Schleif, W.A.7    Emini, E.A.8
  • 29
    • 34447263572 scopus 로고    scopus 로고
    • Natural polymorphism of the HIV-1 integrase gene and mutations associated with integrase inhibitor resistance
    • Lataillade M., Chiarella J., Kozal M.J. Natural polymorphism of the HIV-1 integrase gene and mutations associated with integrase inhibitor resistance. Antivir. Ther. 2007, 12:563-570.
    • (2007) Antivir. Ther. , vol.12 , pp. 563-570
    • Lataillade, M.1    Chiarella, J.2    Kozal, M.J.3
  • 32
    • 78149434355 scopus 로고    scopus 로고
    • The mechanism of retroviral integration from X-ray structures of its key intermediates
    • Maertens G.N., Hare S., Cherepanov P. The mechanism of retroviral integration from X-ray structures of its key intermediates. Nature 2010, 468:326-329.
    • (2010) Nature , vol.468 , pp. 326-329
    • Maertens, G.N.1    Hare, S.2    Cherepanov, P.3
  • 33
    • 0032544311 scopus 로고    scopus 로고
    • Crystal structures of the catalytic domain of HIV-1 integrase free and complexed with its metal cofactor: high level of similarity of the active site with other viral integrases
    • Maignan S., Guilloteau J.P., Zhou-Liu Q., Clement-Mella C., Mikol V. Crystal structures of the catalytic domain of HIV-1 integrase free and complexed with its metal cofactor: high level of similarity of the active site with other viral integrases. J. Mol. Biol. 1998, 282:359-368.
    • (1998) J. Mol. Biol. , vol.282 , pp. 359-368
    • Maignan, S.1    Guilloteau, J.P.2    Zhou-Liu, Q.3    Clement-Mella, C.4    Mikol, V.5
  • 35
    • 79960128850 scopus 로고    scopus 로고
    • Resistance analysis of a Phase 2 study of the integrase inhibitor elvitegravir (GS-9137), 11th European Aids Conference, Madrid, Spain.
    • McColl, D., Fransen, S., Gupta, S., Parkin, N., Margot, N., Chuck, S., Cheng, A., Miller, M., 2007. Resistance analysis of a Phase 2 study of the integrase inhibitor elvitegravir (GS-9137), 11th European Aids Conference, Madrid, Spain.
    • (2007)
    • McColl, D.1    Fransen, S.2    Gupta, S.3    Parkin, N.4    Margot, N.5    Chuck, S.6    Cheng, A.7    Miller, M.8
  • 36
    • 73549123203 scopus 로고    scopus 로고
    • Strand transfer inhibitors of HIV-1 integrase: bringing IN a new era of antiretroviral therapy
    • McColl D.J., Chen X. Strand transfer inhibitors of HIV-1 integrase: bringing IN a new era of antiretroviral therapy. Antiviral Res. 2010, 85:101-118.
    • (2010) Antiviral Res. , vol.85 , pp. 101-118
    • McColl, D.J.1    Chen, X.2
  • 38
    • 2642709177 scopus 로고    scopus 로고
    • Declining morbidity and mortality among patients with advanced human immunodeficiency virus infection. HIV outpatient study investigators
    • Palella F.J., Delaney K.M., Moorman A.C., Loveless M.O., Fuhrer J., Satten G.A., Aschman D.J., Holmberg S.D. Declining morbidity and mortality among patients with advanced human immunodeficiency virus infection. HIV outpatient study investigators. N. Engl. J. Med. 1998, 338:853-860.
    • (1998) N. Engl. J. Med. , vol.338 , pp. 853-860
    • Palella, F.J.1    Delaney, K.M.2    Moorman, A.C.3    Loveless, M.O.4    Fuhrer, J.5    Satten, G.A.6    Aschman, D.J.7    Holmberg, S.D.8
  • 39
    • 73549084507 scopus 로고    scopus 로고
    • Clinical management of HIV-1 resistance
    • Paredes R., Clotet B. Clinical management of HIV-1 resistance. Antiviral Res. 2010, 85:245-265.
    • (2010) Antiviral Res. , vol.85 , pp. 245-265
    • Paredes, R.1    Clotet, B.2
  • 41
    • 0035912249 scopus 로고    scopus 로고
    • HIV chemotherapy
    • Richman D.D. HIV chemotherapy. Nature 2001, 410:995-1001.
    • (2001) Nature , vol.410 , pp. 995-1001
    • Richman, D.D.1
  • 42
    • 33747095403 scopus 로고    scopus 로고
    • Antiviral drug resistance
    • Richman D.D. Antiviral drug resistance. Antiviral Res. 2006, 71:117-121.
    • (2006) Antiviral Res. , vol.71 , pp. 117-121
    • Richman, D.D.1
  • 46
    • 79960120218 scopus 로고    scopus 로고
    • Schrödinger, Suite Protein Preparation Wizard; Epik version 2.0, Schrödinger, LLC, New York, NY, 2009; Impact version 5.5, Schrödinger, LLC, New York, NY, 2009; Prime version 2.1, Schrödinger, LLC, New York, NY, 2009.
    • Schrödinger, 2009. Suite Protein Preparation Wizard; Epik version 2.0, Schrödinger, LLC, New York, NY, 2009; Impact version 5.5, Schrödinger, LLC, New York, NY, 2009; Prime version 2.1, Schrödinger, LLC, New York, NY, 2009.
    • (2009)
  • 47
    • 63549089353 scopus 로고    scopus 로고
    • Raltegravir, elvitegravir, and metoogravir: the birth of " me-too" HIV-1 integrase inhibitors
    • Serrao E., Odde S., Ramkumar K., Neamati N. Raltegravir, elvitegravir, and metoogravir: the birth of " me-too" HIV-1 integrase inhibitors. Retrovirology 2009, 6:25.
    • (2009) Retrovirology , vol.6 , pp. 25
    • Serrao, E.1    Odde, S.2    Ramkumar, K.3    Neamati, N.4
  • 48
    • 77953293159 scopus 로고    scopus 로고
    • Scaffold rearrangement of dihydroxypyrimidine inhibitors of HIV integrase: docking model revisited
    • Tang J., Maddali K., Pommier Y., Sham Y.Y., Wang Z. Scaffold rearrangement of dihydroxypyrimidine inhibitors of HIV integrase: docking model revisited. Bioorg. Med. Chem. Lett. 2010, 20:3275-3279.
    • (2010) Bioorg. Med. Chem. Lett. , vol.20 , pp. 3275-3279
    • Tang, J.1    Maddali, K.2    Pommier, Y.3    Sham, Y.Y.4    Wang, Z.5
  • 49
    • 79960116037 scopus 로고    scopus 로고
    • Discovery of MK-2048: subtle changes confer unique resistance properties to a series of tricyclic hydroxypyrrole integrase strand transfer inhibitors, 4th International AIDS Society (IAS) Conference, Sydney, Australia.
    • Vacca, J.P., Wai, J.S., Fisher, T.E., Embrey, M., Hazuda, D.J., Miller, M.D., Felock, P.J., Witmer, M.V., Gabryelski, L., Lyle, T., 2007. Discovery of MK-2048: subtle changes confer unique resistance properties to a series of tricyclic hydroxypyrrole integrase strand transfer inhibitors, 4th International AIDS Society (IAS) Conference, Sydney, Australia.
    • (2007)
    • Vacca, J.P.1    Wai, J.S.2    Fisher, T.E.3    Embrey, M.4    Hazuda, D.J.5    Miller, M.D.6    Felock, P.J.7    Witmer, M.V.8    Gabryelski, L.9    Lyle, T.10
  • 51
    • 68949172373 scopus 로고    scopus 로고
    • A combined genotypic and phenotypic human immunodeficiency virus type1 recombinant virus assay for the reverse transcriptase and integrase genes
    • Van Baelen K., Rondelez E., Van Eygen V., Ariën K., Clynhens M., Van den Zegel P., Winters B., Stuyver L.J. A combined genotypic and phenotypic human immunodeficiency virus type1 recombinant virus assay for the reverse transcriptase and integrase genes. J. Virol. Methods 2009, 161:231-239.
    • (2009) J. Virol. Methods , vol.161 , pp. 231-239
    • Van Baelen, K.1    Rondelez, E.2    Van Eygen, V.3    Ariën, K.4    Clynhens, M.5    Van den Zegel, P.6    Winters, B.7    Stuyver, L.J.8
  • 52
    • 0029967722 scopus 로고    scopus 로고
    • Similarities between initiation of V(D)J recombination and retroviral integration
    • van Gent D.C., Mizuuchi K., Gellert M. Similarities between initiation of V(D)J recombination and retroviral integration. Science 1996, 271:1592-1594.
    • (1996) Science , vol.271 , pp. 1592-1594
    • van Gent, D.C.1    Mizuuchi, K.2    Gellert, M.3
  • 53
    • 77649112672 scopus 로고    scopus 로고
    • GSK-1349572, a novel integrase inhibitor for the treatment of HIV infection
    • Vandeckerckhove L. GSK-1349572, a novel integrase inhibitor for the treatment of HIV infection. Curr. Opin. Investig. Drugs 2010, 11:203-212.
    • (2010) Curr. Opin. Investig. Drugs , vol.11 , pp. 203-212
    • Vandeckerckhove, L.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.