PMID: 34740228
2022
Current opinion in HIV and AIDS
Abstract: Doravirine has a high genetic barrier to resistance with retained activity in the presence of single NNRTI mutations K103N, Y181C and G190A.
Single Oral Doses of MK-8507, a Novel Non-Nucleoside Reverse Transcriptase Inhibitor, Suppress HIV-1 RNA for a Week.
PMID: 34654041
2022
Journal of acquired immune deficiency syndromes (1999)
Introduction: Preclinical studies demonstrated MK-8507 has high antiviral potency, has a half-maximal inhibitory concentration (IC50) of approximately 50 nM, and shows only modest changes in activity to the most prevalent NNRTI-associated resistance mutations (eg, K103N, Y181C).
Method: Inclusion criteria included diagnosis of HIV-1 infection >=3 months before screening, plasma HIV-1 RNA >=10,000 copies/mL, CD4+ T-cell count >200/mm3, no evidence of NNRTI-associated resistance mutations (eg, K103N, Y181C, and V108I) appearing in the Stanford University HIV Drug Resistance Database, and no evidence of active hepatitis C or hepatitis B infection.
HIV-1 molecular transmission network among sexually transmitted populations in Liaoning Province, China.
Result: Among them, 9 cases were protease inhibitor-related resistance, and the main resistance sites were L33F, V82A, Q58E, M46L, M46I; There were 4 cases of nucleoside reverse transcriptase inhibitor resistance, the main mutation sites were V75VI, K219Q, T215A, K65R; There were 5 cases of non-nucleoside reverse transcriptase inhibitor resistance,
Discussion: Mutations K65R, Y181C+G190S, which produced high drug resistance, did not enter the transmission network.
Near-point-of-care assay with a visual readout for detection of HIV-1 drug resistance mutations: A proof-of-concept study.
Abstract: Here, we present a proof-of-concept study of a rapid and simple molecular method to detect two major mutations (K103 N, Y181C) conferring resistance to first-line nonnucleoside reverse transcriptase inhibitor regimens.
High Detection Rate of HIV Drug Resistance Mutations among Patients Who Fail Combined Antiretroviral Therapy in Manaus, Brazil.
Discussion: Due to the presence of mutations, such as L100I, K101P, Y181C, M230L, observed in of individuals failing in the use of EFV, the viability of using ETR in a rescue scheme is reduced for few individuals (data not shown).
HIV-1 non-group M phenotypic susceptibility in vitro to bictegravir and cabotegravir.
PMID: 34151963
2021
The Journal of antimicrobial chemotherapy
Abstract: Around 50% of the strains of this group naturally show a mutation (Y181C) providing them with resistance to NNRTIs and making therapeutic management more difficult.
High HIV-1 Virological Failure and Drug Resistance among Adult Patients Receiving First-Line ART for At least 12 Months at a Decentralized Urban HIV Clinic Setting in Senegal before the Test-and-Treat.
Abstract: Of the 27 viraemic isolates successfully genotyped, 20 (74.1%) carried DR mutations; most frequent were M184VI (55.6%), K103N (37.1%), thymidine analog mutations (29.6%), Y181CY (22.2%).
Result: The most frequent resistant genotypes to NNRTIs were K103N (37.04%), Y181CY (22.2%), and A98AG (18.5%).
Table: Y181C
Discussion: EFV and NVP have a lower genetic barrier, thus facilitating the selection of K103N and Y181C mutations.
HIV Drug Resistance Mutations Detection by Next-Generation Sequencing during Antiretroviral Therapy Interruption in China.
Result: However, some minority DRMs at frequencies of 1%-5% disappeared, including N83D with PI-related, K70E, T215A, and K219E with NRTI-related and K101E, Y181C, H221Y and K238T with NNRTI-related, while others emerged, such as NNRTI-related V106A in patient GX088 at a frequency of 8.7%, and L23I, I47V and I84V with PI-related, D67N and
Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
Abstract: Y181C is selected in patients receiving nevirapine, etravirine and rilpivirine, and together with K103N is the most prevalent NNRTI-associated mutation in HIV-infected patients.
Abstract: Compounds I-7 and I-9 demonstrated higher selectivity towards the Y181C mutant than against the wild-type RT, in nucleotide incorporation inhibition assays.
Application of Molecular Docking for the Development of Improved HIV-1 Reverse Transcriptase Inhibitors.
PMID: 32598265
2021
Current computer-aided drug design
Abstract: Here, protein-ligand interactions and possible binding modes of novel compounds with the HIV-1 RT binding pocket (the wild-type as well as Y181C and K103N mutants) were obtained and discussed.
HIV mutation literature information.
PMID: 
2022
Current opinion in HIV and AIDS
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