literature

HIV mutation literature information.

Enzymatic and structural analysis of the I47A mutation contributing to the reduced susceptibility to HIV protease inhibitor lopinavir.

PMID: 18560011 2008 Protein science

Abstract: Furthermore, we analyzed possible interaction of the I47A mutation with secondary mutations V32I and I54V.

Pattern and impact of emerging resistance mutations in treatment experienced patients failing darunavir-containing regimen.

PMID: 18690163 2008 AIDS (London, England)

Abstract: Emergence of DRV-associated-resistance mutations was observed in 72% (18/25) of patients, at codons L89I/M/V (32%), V32I (28%), V11I (20%), I47V/A (20%), I54L/M (20%), L33F/I (16%) and I50V (16%).

Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.

PMID: 18808097 2008 Journal of medicinal chemistry

Abstract: Darunavir, a potent antiviral drug, showed an unusual second binding site on the HIV-1 protease dimer surface of the V32I drug resistant mutant and normal binding in the active site cavity.

Introduction: An unusual second binding site for DRV was observed in the two high-resolution crystal structures of complexes with HIV-1 PR mutants with the single substitutions of V32I (0.84 A) and M46L (1.22 A).

Introduction: Here, we report on solution measurements of enzyme inhibition kinetics for an optimized wild-type HIV-1 PR denoted PRWT and the V32I mutant PR (PRV32I) with three PIs: DRV, amprenavir (APV), and saquinavir (SQV) (Figur

Combating HIV resistance - focus on darunavir.

PMID: 19209258 2008 Therapeutics and clinical risk management

Abstract: Darunavir resistance-associated mutations have been defined as V11I, V32I, L33F, I47V, I50V, I54L/M, G73S, L76V, I84V, and L89V.

A novel substrate-based HIV-1 protease inhibitor drug resistance mechanism.

PMID: 17227139 2007 PLoS medicine

Result: In three of the experiments we observed an A431V amino acid substitution in the NC/p1 cleavage site, combined with known resistance substitutions in protease (V32I, M46I/L, I54V, V82A/F, and I84V).

HIV-1 subtype B protease and reverse transcriptase amino acid covariation.

PMID: 17500586 2007 PLoS computational biology

Result: Finally, the lower-left part of the figure contains a cluster with seven of the 11 mutations recently reported to be associated with phenotypic and clinical resistance to the newest PI, darunavir (V32I, L33F, I47V, I50V, I54L/M, and L76V).

Result: For example, M46I/L were each significantly associated with L10I, L24I, V32I, L33F, I54V, V82A, and L90M.

Result: The mutations included in this analysis were the 22 positively associated mutations in Table 1

Key amprenavir resistance mutations counteract dramatic efficacy of darunavir in highly experienced patients.

PMID: 17502734 2007 AIDS (London, England)

Abstract: Patients harbouring viruses with amprenavir-specific resistance profiles, such as I50V or V32I + I47V, failed on a darunavir/ritonavir-containing regimen.

Prevalence of darunavir resistance mutations in HIV-1-infected patients failing other protease inhibitors.

PMID: 17646201 2007 The Journal of antimicrobial chemotherapy

Abstract: For minor darunavir resistance mutations, the rates were V11I 3.3%, V32I 3.9%, L33F 11%, I47V 2.1%, I54L 2.3%, G73S 12.8% and L89V 2.4%.

Ultra-high resolution crystal structure of HIV-1 protease mutant reveals two binding sites for clinical inhibitor TMC114.

PMID: 16962136 2006 Journal of molecular biology

Abstract: We report the ultra-high 0.84 A resolution crystal structure of the TMC114 complex with PR containing the drug-resistant mutation V32I (PR(V32I)), and the 1.22 A resolution structure of a complex with PR(M46L).

Fosamprenavir clinical study meta-analysis in ART-naive subjects: rare occurrence of virologic failure and selection of protease-associated mutations.

PMID: 17197380 2006 HIV clinical trials

Abstract: RESULTS: FPV-associated resistance mutations were detected in 5/74 patients with VF, with 4/5 receiving unboosted FPV; in four patients viruses developed I54L or M and one developed the V32I+I47V combination.

Browser Board

Co-occurred Entities

Filtrator