literature

HIV mutation literature information.

1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.

PMID: 21903401 2011 Bioorganic & medicinal chemistry

Result: Interestingly, benzophenone 17 displayed even higher inhibitory activity toward the mutant G190A RT form, while 20 exhibited somewhat lower activity (2.3-fold), more closely in line with efavirenz (2.7-fold decrease) but in sharp contrast to nevirapine (423-fold decrease).

Result: Moreover, the resistance index for the compounds against the Y181C, Y188L and K103N/Y181C mutant RTs was comparable to that of efavirenz, and even lower for the L100I, K103N and G190A mutants, although for the V106A mutant, efavirenz was more potent than 17 and 20.

Result: Next, in order to more fully underst

Docking analysis and resistance evaluation of clinically relevant mutations associated with the HIV-1 non-nucleoside reverse transcriptase inhibitors nevirapine, efavirenz and etravirine.

PMID: 21953939 2011 ChemMedChem

Abstract: A support vector regression model, based on matched genotypic/phenotypic data (n=850), showed that among 6365 analyzed mutations, K103N, Y181C and G190A have the first, third, and sixth greatest significance for nevirapine resistance, respectively.

Abstract: Mutations detected for nevirapine virological failure with a prevalence greater than 10% in the used patient set were: K103N, Y181C, G190A, and K101E.

Abstract: The most common indicator of treatment failure for efavirenz was K103N mutation present in 56.7% of the patients where the drug failed, followed by V108I, L100I, and G190A.

Etravirine and rilpivirine resistance in HIV-1 subtype CRF01_AE-infected adults failing non-nucleoside reverse transcriptase inhibitor-based regimens.

PMID: 22024527 2011 Antiviral therapy

Abstract: The common NNRTI mutations were Y181C (41%), G190A (22%) and K103N (19%).

Resistance patterns selected by nevirapine vs. efavirenz in HIV-infected patients failing first-line antiretroviral treatment: a bayesian analysis.

PMID: 22132100 2011 PloS one

Method: RT mutations were identified from the International AIDS Society USA Drug (IAS-USA) mutation tables, spring 2008 (http://www.iasusa.org/resistance_mutations): M41L, K65R, D67N, insertion 69, K70R/E, L74I/V, L100I, K103N, V106A/M, V108I, Q151M, Y181I/C, M184V, Y188C/L, G190A/S, L210W, T215Y/F,

PMID: 22155917 2011 Antiviral therapy

Abstract: DRM to non-nucleoside reverse transcriptase inhibitors were found in 5 samples (11.6% [95% CI, 2.0-21.2]) involving K103N, Y181C and G190A mutations.

Emerging trends of drug-resistant HIV-1 among drug-treated patients in former blood donors in Hubei, China: a three-year surveillance from 2004 to 2006.

PMID: 22160938 2011 Virologica Sinica

Abstract: Genotypic drug resistance analysis showed significant increases in percentages of patients carrying HIV-1 strains with M41L, T215Y/F, D67N, K103N, G190A/S, Y181C/F or L210W mutations.

Antiretroviral drug resistance in HIV-infected patients in Colombia.

PMID: 19665910 2010 International journal of infectious diseases

Abstract: The most common mutations were 184V (n=48; 62.3%), 103N (n=37; 48.1%), G190A/S (n=9; 11.7%), and L90M (n=9; 11.7%).

N348I in HIV-1 reverse transcriptase decreases susceptibility to tenofovir and etravirine in combination with other resistance mutations.

PMID: 20010074 2010 AIDS (London, England)

Introduction: Since the presence of three or more NNRTI mutations V90I, A98G, L100I, K101E/P, V106I, V179D/F, Y181C/I/V and G190A/S results in no response to etravirine treatment, the presence of two of these NNRTI mutations and N348I at baseline may also reduce etravirine efficacy in vivo.

Low frequency nonnucleoside reverse-transcriptase inhibitor-resistant variants contribute to failure of efavirenz-containing regimens in treatment- experienced patients.

PMID: 20102272 2010 The Journal of infectious diseases

Method: For single-genome sequencing analyses, a total of 27 subjects (15 NNRTI-naive and 12 NNRTI-experienced) were randomly selected from enrollees meeting the following criteria: i) entry sample negative for NNRTI-resistance mutations by standard genotype analysis (ViroSeq platform; Celera, Alameda, CA); ii) reached a protocol-defined virologic failure endpoint by study week 24, and iii) the virologic failure sample had one or more major NNRTI-resistance mutations (L100I, K101E, K103N, V106A or M, V108I, Y181C or I, Y188C, H, or L, G

Efficacy and safety of 1-month postpartum zidovudine-didanosine to prevent HIV-resistance mutations after intrapartum single-dose nevirapine.

PMID: 20158398 2010 Clinical infectious diseases

Abstract: Consensus sequencing and the more sensitive oligonucleotide ligation assay were performed on samples obtained on postpartum days 7-10, 37-45, and 120 (if the HIV load was >500 copies/mL) to detect K103N/Y181C/G190A mutations.

Method: The K103N, G190A, and Y181C NNRTI resistance mutations were tested using oligonucleotides designed for the CRF01_AE subtype prevalent in Thailand.

Result: Using OLA, the K103N, G190A or Y181C mutations were detected postpartum in four (1.8%) PHPT-4 subjects versus 42 (18.9%) controls.

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