Abstract: In addition, it showed moderate inhibitory potency (EC50 = 1.329 muM) against the HIV-1 K103N/Y181C double mutant strain (MT-4 cells).
Prevalence and determinants of virological failure, genetic diversity and drug resistance among people living with HIV in a minority area in China: a population-based study.
Result: The most common mutations in NNRTIs were K103N/KN (64.69%), V179D/E (23.47%) and Y181C/YC/I (14.00%), they were M184V/MV/I (36.29%), T215F/FS/TNSY (7.50%) and K219Q (5.92%) in NRTIs, and they were Q58E/QE (4.93%), L10F/LFI (0.39%) and M46L (0.39%) in PIs.
HIV-1 re-suppression on a first-line regimen despite the presence of phenotypic drug resistance.
Introduction: Patients failing an NNRTI-based first-line regimen with genotypic drug resistance mutations typically present with M184V/I, K65R, and/or thymidine analogue mutations (TAMs) and K103N, V106M/A and/or Y181C as the most prevalent NRTI and NNRTI mutations, respectively.
Result: The prevalence of other major NNRTI resistance mutations (Y181CS, Y188CH, G190A and M230L) was <=8%.
Exploring the hydrophobic channel of NNIBP leads to the discovery of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs.
Abstract: Especially, compound 26 exhibited the most potent activity against wild-type and a panel of single mutations (L100I, K103N, Y181C, Y188L and E138K) with an EC50 ranging from 6.02 to 23.9 nmol/L, which were comparable to those of etravirine (ETR).
Result: 4) with average distances of (Y188/P227) 4.4 +- 0.6/3.3 +- 0.6 A for WT RT, 3.9 +- 0.4/3.4 +- 0.6 A for the K103N variant, and 4.5 +- 0.7/4.7 +- 0.7 A for the K103N/Y181C mutated enzyme.
Result: All the compounds were further evaluated against a panel of clinically relevant NNRTIs-resistant single-mutant strains (L100I, PMID: 32522826
2020
Journal of clinical microbiology
Abstract: In a cross-sectional study (June 2018 to September 2019), we evaluated the diagnostic accuracy of a simple and rapid HIVDR assay (the pan-degenerate amplification and adaptation [PANDAA] assay targeting the mutations K65R, K103NS, M184VI, Y181C, and G190A) compared to Sanger sequencing and next-generation sequencing (NGS).
Abstract: PANDAA showed strong agreement with Sanger sequencing for K65R, K103NS, M184VI, and G190A (kappa > 0.85) and substantial agreement for Y181C (kappa = 0.720).
Pretreatment resistance mutations and treatment outcomes in adults living with HIV-1: a cohort study in urban Malawi.
Result: Three TCs were formed by strains carrying two SDRMs, including L33F/V179T-carrying strains, A62V/V179T-carrying strains and A98G/Y181C-carrying strains (Figure 4).
Discussion: Furthermore, we found that the major NNRTI-related SDRMs were K101P, K103N, V106A, E138A, Y181C, and Y188H, and the major NRTI-related SDRMs were L74V/I and M184V.
Natural presence of the V179D and K103R/V179D mutations associated with resistance to nonnucleoside reverse transcriptase inhibitors in HIV-1 CRF65_cpx strains.
Introduction: For example, most of the HIV-1 O group viruses are considered to be naturally resistant to nonnucleoside reverse transcriptase inhibitors (NNRTIs) due to the presence of the Y181C mutation.
Result: V179D, Y181C, and H221Y were detected in the one treatment-experienced patient.
Table: Y181C
Prevalence of doravirine-associated resistance mutations in HIV-1-infected antiretroviral-experienced patients from two large databases in France and Italy.
PMID: 31976534
2020
The Journal of antimicrobial chemotherapy
Abstract: In comparison, the prevalence of the common NNRTI mutations V90I, K101E/P, K103N/S, E138A/G/K/Q/R/S, Y181C/I/V and G190A/E/S/Q were higher (8.9%, 7.9%, 28.6%, 12.6%, 14.2% and 8.9%, respectively).
Abstract: RESULTS: The frequencies of doravirine-associated resistance mutations (total dataset versus NNRTI-failing patients) were: V106A/M, 0.8% versus 2.6%; V108I, 3.3% versus 9.2%; Y188L, 1.2% versus 2.6%; G190S, 0.3% versus 2.1%; F227C/L/V
HIV mutation literature information.
PMID: 
2020
Bioorganic & medicinal chemistry letters
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