literature

HIV mutation literature information.

Follow on-based optimization of the biphenyl-DAPYs as HIV-1 nonnucleoside reverse transcriptase inhibitors against the wild-type and mutant strains.

PMID: 31102693 2019 Bioorganic chemistry

Abstract: Specifically, compound 30, which had the highest selectivity index (SI = 16094) and the best anti-reverse transcriptase ability (IC50 = 39 nM), displayed marked inhibitory activity (EC50 = 13.5, 9.4, 17.0, 52.0, and 58.2 nM) against WT, K103N, E138K, L100I, Y181C mutants and moderate activity against double mutants.

HIV Drug Resistance Mutations in Patients with HIV and HIV-TB Coinfection After Failure of First-Line Therapy: A Prevalence Study in a Resource-Limited Setting.

PMID: 31117863 2019 Journal of the International Association of Providers of AIDS Care

Table: Y181C

Nonnucleoside Reverse Transcriptase Inhibitor Hypersusceptibility and Resistance by Mutation of Residue 181 in HIV-1 Reverse Transcriptase.

PMID: 31160281 2019 Antimicrobial agents and chemotherapy

Abstract: In the presence of saturating concentrations of inhibitor, the Y181C RT-T/P complex incorporated the next correct deoxynucleoside triphosphate (dNTP) more efficiently than the wild-type (WT) complex, and this phenotype correlated with decreased mobility of the RT on the T/P substrate.

Abstract: Substitutions at residue Y181 in HIV-1 reverse transcriptase (RT), in particular, Y181C, Y181I, and Y181V, are associated with nonnucleoside RT inhibitor (NNRTI) cross-resistance.

Abstract: Using pre-steady-state kinetics, we found that the dissociation constant (Kd ) values for inhibitor binding to the

Antiretroviral drug resistance mutations among patients failing first-line treatment in Hanoi, Vietnam.

PMID: 31190911 2019 Infection and drug resistance

Table: Y181C

Table: Y181I/C

Discussion: In a previous pre-treatment HIV-DR study, NNRTI resistance was K103N, Y181C, Y188C and G190A, and NRTI resistance was V75M and M184V.

Rates of HIV-1 virological suppression and patterns of acquired drug resistance among fisherfolk on first-line antiretroviral therapy in Uganda.

PMID: 31257432 2019 The Journal of antimicrobial chemotherapy

Result: The most prevalent NNRTI mutations were K103N (39.2%), Y181C (19.6%) and G190A (15.5%) (Figure 3).

Discussion: All individuals with ADR had NNRTI mutations with K103N/S, Y181C, K101E/Q and G190S/A being more prevalent, depicting extensive use of the NNRTIs nevirapine and efavirenz in first-line regimens in this setting.

Sustained virological response and drug resistance among female sex workers living with HIV on antiretroviral therapy in Kampala, Uganda: a cross-sectional study.

PMID: 31266818 2019 Sexually transmitted infections

Table: Y181C

Molecular and cellular studies evaluating a potent 2-cyanoindolizine catechol diether NNRTI targeting wildtype and Y181C mutant HIV-1 reverse transcriptase.

PMID: 31281023 2019 Bioorganic & medicinal chemistry letters

Introduction: A newer generation of NNRTIs was developed in an effort to successfully target drug resistant forms, including Y181C, which evade inhibition by early generation NNRTIs.

Introduction: Analysis of key interactions reveals the conservation of hydrogen bonding and van der Waals forces between the WT and Y181C structures.

Introduction: Clear electron density was observed at the NNRTI binding pocket, allowing unambiguous determination of the orientation and positioning of the 2-cyanoindolizine catechol diether scaffold of Compound 1 for both the WT RT and Y181C structures (Figure 3).

Switching to bictegravir/emtricitabine/tenofovir alafenamide maintained HIV-1 RNA suppression in participants with archived antiretroviral resistance including M184V/I.

PMID: 31430369 2019 The Journal of antimicrobial chemotherapy

Method: Primary NNRTI-R substitutions were L100I, K101E/P,

Result: NNRTI-R substitutions were observed in 23% (124/543) of participants; the most frequently detected substitutions were K103N/S in 12% (64/543) and rilpivirine-associated resistance substitutions (L100I, K101E/P, E138A/G/K/Q/R, V179L, Y181C/I/V, Y188L, H221Y, F227C or M320I/L) in 10% (53/543) (Table 3).

Table: Y181C/I

Discovery of novel indolylarylsulfones as potent HIV-1 NNRTIs via structure-guided scaffold morphing.

PMID: 31434039 2019 European journal of medicinal chemistry

Abstract: Furthermore, some compounds maintained excellent activity against various single HIV-1 mutants (L100I, K103 N, E138K, Y181C) as well as one double mutant (F227L/V106A) with EC50 values in low-micromolar concentration ranges.

Trend of HIV transmitted drug resistance before and after implementation of HAART regimen restriction in the treatment of HIV-1 infected patients in southern Taiwan.

PMID: 31443633 2019 BMC infectious diseases

Result: For NNRTIs, the most prevalent drug resistance mutations were K103 N (1.59%), V179D + K103R (1.33%), Y181C (0.80%), V108I (0.53%), Y188L (0.53%), G190A (0.53%), H221Y (0.53%), Y318F (0.53%), A98G (0.27%), V106A (0.27%), E138A (0.27%), E138R (0.27%), Y188C (0.27%) and M230 L (0.27%).

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