Resistance mutation info of target

Target General Information
Target ID T39087
Target Name HIV Integrase
Species Human immunodeficiency virus type 1 (HIV-1)
UniProt ID POL_HV1B1(1160-1447)
Sequence FLDGIDKAQDEHEKYHSNWRAMASDFNLPPVVAKEIVASCDKCQLKGEAMHGQVDCSPGI
WQLDCTHLEGKVILVAVHVASGYIEAEVIPAETGQETAYFLLKLAGRWPVKTIHTDNGSN
FTSATVKAACWWAGIKQEFGIPYNPQSQGVVESMNKELKKIIGQVRDQAEHLKTAVQMAV
FIHNFKRKGGIGGYSAGERIVDIIATDIQTKELQKQITKIQNFRVYYRDSRNPLWKGPAK
LLWKGEGAVVIQDNSDIKVVPRRKAKIIRDYGKQMAGDDCVASRQDED [Human immu
nodeficiency virus type 1 (HIV-1)]
Drug and Corresponding Resistance Mutations
Mutation Info Missense: E138A
Drugs
Drug Name Dolutegravir Drug Info [3], [4]
Targeted Disease HIV infection
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: E138A/K/T + G140A/C/S
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: E138K
Drugs
Drug Name Dolutegravir Drug Info [3], [4]
Targeted Disease HIV infection
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: E138T
Drugs
Drug Name Dolutegravir Drug Info [3], [4]
Targeted Disease HIV infection
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: E157Q
Drugs
Drug Name Raltegravir Drug Info [10]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [18]
Targeted Disease HIV infection
Mutation Info Missense: E92G
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [11]
Targeted Disease HIV infection
Mutation Info Missense: E92Q
Drugs
Drug Name Dolutegravir Drug Info [3], [4]
Targeted Disease HIV infection
Drug Name Raltegravir Drug Info [8], [11], [12]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [12], [16], [17]
Targeted Disease HIV infection
Mutation Info Missense: E92V
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: F121Y
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [18]
Targeted Disease HIV infection
Mutation Info Missense: G118R
Drugs
Drug Name Dolutegravir Drug Info [3], [4]
Targeted Disease HIV infection
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: G140A
Drugs
Drug Name Dolutegravir Drug Info [3], [4]
Targeted Disease HIV infection
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: G140C
Drugs
Drug Name Dolutegravir Drug Info [3], [4]
Targeted Disease HIV infection
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: G140S
Drugs
Drug Name Dolutegravir Drug Info [3], [4]
Targeted Disease HIV infection
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: G163K
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: G163R
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: H51Y
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [18], [19], [20]
Targeted Disease HIV infection
Mutation Info Missense: H51Y + R263K
Drugs
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: N155H
Drugs
Drug Name Dolutegravir Drug Info [3], [4]
Targeted Disease HIV infection
Drug Name Raltegravir Drug Info [6]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [12], [16], [17]
Targeted Disease HIV infection
Mutation Info Missense: N155S
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: N155T
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: P145S
Drugs
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: Q146P
Drugs
Drug Name Elvitegravir Drug Info [18]
Targeted Disease HIV infection
Mutation Info Missense: Q148H
Drugs
Drug Name Dolutegravir Drug Info [3], [4]
Targeted Disease HIV infection
Drug Name Raltegravir Drug Info [6]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [6]
Targeted Disease HIV infection
Mutation Info Missense: Q148K
Drugs
Drug Name Dolutegravir Drug Info [3], [4]
Targeted Disease HIV infection
Drug Name Raltegravir Drug Info [6]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [6]
Targeted Disease HIV infection
Mutation Info Missense: Q148N
Drugs
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: Q148R
Drugs
Drug Name Dolutegravir Drug Info [3], [4]
Targeted Disease HIV infection
Drug Name Raltegravir Drug Info [6]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [6]
Targeted Disease HIV infection
Mutation Info Missense: R263K
Drugs
Drug Name Dolutegravir Drug Info [1], [2]
Targeted Disease HIV infection
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: S147G
Drugs
Drug Name Elvitegravir Drug Info [11], [16]
Targeted Disease HIV infection
Mutation Info Missense: S153F
Drugs
Drug Name Dolutegravir Drug Info [3], [4]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: S153Y
Drugs
Drug Name Dolutegravir Drug Info [5]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [18], [20]
Targeted Disease HIV infection
Mutation Info Missense: S230R
Drugs
Drug Name Raltegravir Drug Info [8]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: T66A
Drugs
Drug Name Raltegravir Drug Info [13], [14]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [11], [16]
Targeted Disease HIV infection
Mutation Info Missense: T66I
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: T66K
Drugs
Drug Name Dolutegravir Drug Info [3], [4]
Targeted Disease HIV infection
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [20], [16]
Targeted Disease HIV infection
Mutation Info Missense: T97A
Drugs
Drug Name Raltegravir Drug Info [7], [10], [11]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [11]
Targeted Disease HIV infection
Mutation Info Missense: V151A
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: V151L
Drugs
Drug Name Dolutegravir Drug Info [3], [4]
Targeted Disease HIV infection
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Drug Name Elvitegravir Drug Info [4], [21]
Targeted Disease HIV infection
Mutation Info Missense: Y143A
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Mutation Info Missense: Y143C
Drugs
Drug Name Raltegravir Drug Info [7], [8], [9]
Targeted Disease HIV infection
Mutation Info Missense: Y143G
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Mutation Info Missense: Y143H
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Mutation Info Missense: Y143K
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
Mutation Info Missense: Y143R
Drugs
Drug Name Raltegravir Drug Info [7], [8], [9]
Targeted Disease HIV infection
Mutation Info Missense: Y143S
Drugs
Drug Name Raltegravir Drug Info [4], [15]
Targeted Disease HIV infection
References
REF 1 Viral fitness cost prevents HIV-1 from evading dolutegravir drug pressure. Retrovirology. 2013 Feb 22;10:22.
REF 2 Evolution of a novel pathway leading to dolutegravir resistance in a patient harbouring N155H and multiclass drug resistance. J Antimicrob Chemother. 2015 Feb;70(2):405-11.
REF 3 HIV drug development: the next 25 years. Nat Rev Drug Discov. 2007 Dec;6(12):959-66.
REF 4 The HIVdb system for HIV-1 genotypic resistance interpretation. Intervirology. 2012;55(2):98-101.
REF 5 In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother. 2011 Feb;55(2):813-21.
REF 6 Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection. N Engl J Med. 2008 Jul 24;359(4):355-65.
REF 7 Genotypic/phenotypic patterns of HIV-1 integrase resistance to raltegravir. J Antimicrob Chemother. 2010 Mar;65(3):425-33.
REF 8 HIV-1 integrase inhibitor resistance and its clinical implications. J Infect Dis. 2011 May 1;203(9):1204-14.
REF 9 Broad phenotypic cross-resistance to elvitegravir in HIV-infected patients failing on raltegravir-containing regimens. Antimicrob Agents Chemother. 2012 Jun;56(6):2873-8.
REF 10 Mutations associated with failure of raltegravir treatment affect integrase sensitivity to the inhibitor in vitro. Antimicrob Agents Chemother. 2008 Apr;52(4):1351-8.
REF 11 Efficacy and safety of once daily elvitegravir versus twice daily raltegravir in treatment-experienced patients with HIV-1 receiving a ritonavir-boosted protease inhibitor: randomised, double-blind, phase 3, non-inferiority study. Lancet Infect Dis. 2012 Jan;12(1):27-35.
REF 12 Infrequent development of drug resistance in HIV-1-infected treatment-naive subjects after 96 weeks of treatment with elvitegravir/cobicistat/emtri... Antivir Ther. 2017;22(5):443-446.
REF 13 Drug resistance profiles for the HIV integrase gene in patients failing raltegravir salvage therapy. HIV Med. 2008 Oct;9(9):765-70.
REF 14 Long-term efficacy and safety of the HIV integrase inhibitor raltegravir in patients with limited treatment options in a Phase II study. J Acquir Immune Defic Syndr. 2010 Apr 1;53(4):456-63.
REF 15 Resistance to direct-acting antiviral agents: clinical utility and significance. Curr Opin HIV AIDS. 2015 Sep;10(5):381-9.
REF 16 Development of elvitegravir resistance and linkage of integrase inhibitor mutations with protease and reverse transcriptase resistance mutations. PLoS One. 2012;7(7):e40514.
REF 17 Co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir disoproxil fumarate versus ritonavir-boosted atazanavir plus co-formulated emtricitabine and tenofovir disoproxil fumarate for initial treatment of HIV-1 infection: a randomised, double-blind, phase 3, non-inferiority trial. Lancet. 2012 Jun 30;379(9835):2429-38.
REF 18 Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137). J Virol. 2008 Jan;82(2):764-74.
REF 19 Strand transfer inhibitors of HIV-1 integrase: bringing IN a new era of antiretroviral therapy. Antiviral Res. 2010 Jan;85(1):101-18.
REF 20 In vitro resistance selections using elvitegravir, raltegravir, and two metabolites of elvitegravir M1 and M4. Antiviral Res. 2012 Feb;93(2):288-96.
REF 21 Evolutionary consequences of drug resistance: shared principles across diverse targets and organisms. Nat Rev Genet. 2015 Aug;16(8):459-71.

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