Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
PMID: 28628334
2017
Journal of medicinal chemistry
Abstract: The new IASs 8-37 showed potent inhibition of the HIV-1 WT NL4-3 strain and of the mutant K103N, Y181C, Y188L, and K103N-Y181C HIV-1 strains.
Multimethod Longitudinal HIV Drug Resistance Analysis in Antiretroviral-Therapy-Naive Patients.
PMID: 28659324
2017
Journal of clinical microbiology
Abstract: ART-naive HIV-1-infected patients from Cameroon were subjected to a multimethod HIVDR analysis using amplification-refractory mutation system (ARMS)-PCR, Sanger sequencing, and longitudinal next-generation sequencing (NGS) to determine their profiles for the mutations K103N, Y181C, K65R, M184V, and T215F/Y.
HIV-1 genetic diversity and primary drug resistance mutations before large-scale access to antiretroviral therapy, Republic of Congo.
Abstract: Two samples (4%) harboring the mutations M230L and Y181C associated with the TAMs M41L and T215Y, respectively, were found.
Method: In addition, one sample (CgCHU38) from a patient attending the Centre Hospitalier et Universitaire de Brazzaville (CHU-B) and subtyped as G in all 3 regions has the mutations Y181C, M41L and T215Y.
Discussion: Additionally, the sample harboring the mutation T215Y and the TAMs M41L and Y181C sampled at the CHU de Brazzaville (subtype G) was male, but the transmission of these HIV-1 mutations from nevirapine-exposed patients can be suspected.
HIV drug resistance in HIV positive individuals under antiretroviral treatment in Shandong Province, China.
Abstract: M184V was the most frequently found point mutation, conferring resistance to the nucleoside reverse transcriptase inhibitor, while Y181C, G190A, K103N
Result: We found that M184V and Y181C were also the most frequent point mutations in these patients.
Result: We found that M184V was the most frequent point mutation conferring resistance against NRTIs, whereas Y181C, G190A, K103N and V179D/E/F were the most frequent point mutations conferring resistance to NNRTIs.
High level of HIV-1 drug resistance mutations in patients with unsuppressed viral loads in rural northern South Africa.
Result: 1) DRM were present, always in combination with Y181C.
Result: Although H221Y has minimal detectable effect on NNRTI susceptibility, it has been found to frequently occur in combination with Y181C in RPV exposed patients.
Result: More than half of these mutations (K65R, D67N, K70R, L74V, V75I/S, Y115F, K219Q/E, Table: Y181C
Discussion: The mutations V106A/M and Y181C were 13.3 and 4.8% more common in Pretoria than in Limpopo, respectively.
HIV Resistance and Prevention of Mother-to-Child Transmission Regimen in HIV-Infected Infants in Northern Tanzania.
PMID: 28797181
2017
AIDS research and human retroviruses
Abstract: The most common HLRMs to NVP were K103 N, Y181C, and Y188 L.
Covalent inhibitors for eradication of drug-resistant HIV-1 reverse transcriptase: From design to protein crystallography.
Abstract: Resistance associated with the Tyr181Cys mutation in HIV-1 RT has been a key roadblock in the discovery of nonnucleoside RT inhibitors (NNRTIs).
Abstract: We report covalent inhibitors of Tyr181Cys RT (CRTIs) that can completely knock out activity of the resistant mutant and of the particularly challenging Lys103Asn/Tyr181Cys variant.
Week 48 resistance analysis of Elvitegravir/Cobicistat/Emtricitabine/Tenofovir DF versus Atazanavir + Ritonavir + Emtricitabine/Tenofovir DF in HIV-1 infected women (WAVES study GS-US-236-0128).
Method: Primary NNRTI-R substitutions assessed were V90I, A98G, L100I, K101E/H/P, K103N/S, V106A/I/M, V108I, E138A/G/K/Q/R, V179D/F/L/T, Y181C/I/V, Y188C/H/L, G190A/E/Q/S, H221Y, P225H, F227C, and M230I/L in RT.
Community Based Antiretroviral Treatment in Rural Zimbabwe.
PMID: 28899102
2017
AIDS research and human retroviruses
Abstract: Seven participants had sequence data available, and five had drug resistance mutations, K65R, T69N, K101E, K103N, Y181C/I, M184V, and G190A.
Rates of virological suppression and drug resistance in adult HIV-1-positive patients attending primary healthcare facilities in KwaZulu-Natal, South Africa.
PMID: 28981637
2017
The Journal of antimicrobial chemotherapy
Abstract: DRMs were detected in 89% of 123 specimens with VF, including M184I/V, K103N/S, K65N/R, V106A/M and Y181C.