Discovery, synthesis, and optimization of an N-alkoxy indolylacetamide against HIV-1 carrying NNRTI-resistant mutations from the Isatis indigotica root.
PMID: 32004936
2020
European journal of medicinal chemistry
Abstract: Especially, 10i (EC50 = 0.43 muM) was more active to the L100I/K103N double-mutant strain as compared to both NVP (EC50 = 0.76 muM) and EFV (EC50 = 1.08 muM).
Method: The complex structure was obtained from the Protein Data Bank (WT RT: 1TL1, Y181C RT: 1JLB, K103N-Y181C double-mutated RT: 5VQY, L100I-K103N double-mutated RT: 2ZE2).
Result: As the L100I/K103N double-mutated RT resisted EFV, the docking.
Result: In order to better understand the possible binding mode of
Comparison of HIV drug resistance profiles across HIV-1 subtypes A and D for patients receiving a tenofovir-based and zidovudine-based first line regimens in Uganda.
Result: Within the NNRTI class, G190 mutations (69.1%, p = 0.015), Y181C (78.6%, p = 0.008), L100I (82.4%, p = 0.019) were significantly more in the TDF/3TC/EFV group whereas mutation K238T (71.4%, p = 0.035) was significantly more in the AZT/3TC/EFV group.
Pharmacophore-fusing design of pyrimidine sulfonylacetanilides as potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
HIV-1 acquired drug resistance to integrase inhibitors in a cohort of antiretroviral therapy multi-experienced Mexican patients failing to raltegravir: a cross-sectional study.
Discordance between Etravirine Phenotype and Genotype-Based Predicted Phenotype for Subtype C HIV-1 from First-Line Antiretroviral Therapy Failures in South Africa.
PMID: 32071061
2020
Antimicrobial agents and chemotherapy
Abstract: Mutations L100I, Y181C, or M230L were present in 27/34 (79%) of samples with an FC of >10 but only in 2/46 (4%) of samples with an FC of <2.9.
Drug Resistance Mutations Against Protease, Reverse Transcriptase and Integrase Inhibitors in People Living With HIV-1 Receiving Boosted Protease Inhibitors in South Africa.
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: All the compounds were further evaluated against a panel of clinically relevant NNRTIs-resistant single-mutant strains (L100I, K103N, Y181C, Y188L, E138K) and double-mutant strains F227L + V106A, RES056.
Result: Compound 26 demonstrated the most active potency towa
Retrospective analysis of HIV-1 drug resistance mutations in Suzhou, China from 2009 to 2014.
Abstract: Two of the mutations, M230L and L100I, which confer a high level of resistance efavirenz (EFV) and nevirapine (NVP) used as NNRTIs for first-line antiretroviral therapy (ART), were detected in this study.
HIV-1 Drug Resistance, Distribution of Subtypes, and Drug Resistance-Associated Mutations in Virologic Failure Individuals in Chengdu, Southwest China, 2014-2016.
Result: K103N (37.55%, 92/245) was the most frequent mutation, followed by G190A/E/K/Q/S/V (28.57%, 70/245), V179I/D/E/T (27.76%, 68/245), V106A/I/M (26.12%, 64/245), Y181C/V (18.78%, 46/245), K101E/H/P (14.69%, 36/245), Y188C/H/L (5.71%, 14/245), L100I (4.08%, 10/245), and M230L (4.08%, 10/245).
Discussion: The L100I and M230L mutations (4.08%) had low incidence and intermediate or high resistance to RPV and ETR but no resistance to the first-line drugs EFV and NVP.
Prevalence of acquired drug resistance mutations in antiretroviral- experiencing subjects from 2012 to 2017 in Hunan Province of central South China.
HIV mutation literature information.
PMID: 
2020
European journal of medicinal chemistry
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