literature

HIV mutation literature information.

Development of Novel Dihydrofuro[3,4-d]pyrimidine Derivatives as HIV-1 NNRTIs to Overcome the Highly Resistant Mutant Strains F227L/V106A and K103N/Y181C.

PMID: 30839042 2019 Organic & biomolecular chemistry

Abstract: Among them, meta-methylbenzoate (ZL2, EC50(IIIB) = 0.020 muM, EC50(K103N) = 0.043 muM, CC50 > 241.52 muM), para-methylbenzoate (ZL3, EC50(IIIB) = 0.013 muM, EC50 (K103N) = 0.022 muM, CC50 > 241.52 muM) and para-phenol (ZL7, EC50(IIIB) = 0.014 muM, EC50 (K103N) = 0.054 muM, CC50 = 2.1 muM) derivatives are the three most promising compounds which are superior to the first-line antiretroviral drug efavirenz (EC50(IIIB) = 0.003 muM, EC50 (K103N) = 0.11 muM, CC50 > 6.34 muM) against the K103N mutant strain.

Abstract: Interestingly, some compounds displayed remarkable potency in inhibiting K103N mutant virus, a key drug-resistant mutant to NNRTIs.

Persistence of Human Immunodeficiency Virus-1 Drug Resistance Mutations in Proviral Deoxyribonucleic Acid After Virologic Failure of Efavirenz-Containing Antiretroviral Regimens.

PMID: 30863788 2019 Open forum infectious diseases

Abstract: In an adjusted model including years since suppression, persistent proviral K103N was 2.6 times more likely (95% confidence interval, 1.0-6.4) per log10 higher human immunodeficiency virus RNA at EFV failure.

Abstract: Methods: Participants with virologic failure of EFV-based regimens and drug-resistant viremia with the K103N mutation in plasma ribonucleic acid (RNA) were identified from AIDS Clinical Trials Group (ACTG) studies A364 and A5095.

Abstract: Sanger sequencing of proviral DNA detected K103N as well as additional reverse-transcriptase inhibitor (RTI) mutations.

High predictive efficacy of integrase strand transfer inhibitors in perinatally HIV-1-infected African children in therapeutic failure of first- and second-line antiretroviral drug regimens recommended by the WHO.

PMID: 30891603 2019 The Journal of antimicrobial chemotherapy

Discussion: Otherwise, in our study we found that a large proportion (9/13; 69.2%) of the HIV-1 strains remained susceptible to second-generation rilpivirine, which has also been described as a good candidate for an optimized dolutegravir-based treatment, although the presence of the K103N mutation could limit the efficiency of rilpivirine.

Two Coselected Distal Mutations in HIV-1 Reverse Transcriptase (RT) Alter Susceptibility to Nonnucleoside RT Inhibitors and Nucleoside Analogs.

PMID: 30894467 2019 Journal of virology

Introduction: Compound 13 is similar to RPV in terms of its therapeutic index and its antiretroviral efficacy against a panel of HIV-1 mutants containing RT mutations, including L100I, K103N, V106A, E138K, Y181C, Y188L, H221Y, and K103N/Y181C.

Introduction: In those trials, the viruses in participants who failed RPV-containing therapies had the RT mutations L100I, K101E, K103N, V108I, E138K/R, Y1

The Utility of Efavirenz-based Prophylaxis Against HIV Infection. A Systems Pharmacological Analysis.

PMID: 30918485 2019 Frontiers in pharmacology

Abstract: Trough concentrations achieved after 600 mg once daily dosing (median: 2017 ng/mL, 95% CI:445-9830) and after reduced dose (400 mg) efavirenz (median: 1349ng/mL, 95% CI: 297-6553) provided complete protection against wild-type virus and the Y181C mutant, and median trough concentrations provided about 90% protection against the K103N and G190S mutants.

Abstract: We predicted that plasma concentrations of 11, 36, 1287 and 1486ng/mL prevent 90% sexual transmissions with wild type and Y181C, K103N and G190S mutants, respectively.

Incidence and types of HIV-1 drug resistance mutation among patients failing first-line antiretroviral therapy.

PMID: 30928089 2019 Journal of pharmacological sciences

Abstract: RESULTS: 103 cases were successfully amplified, and the main drug resistance mutations in the reverse transcriptase (RT) region were M184V (50.49%), K103N (28.16%), Y181C (25.24%), and K65R (27.18%), while no drug main resistance mutation was found in the protease (PR) region.

The rate of mother-to-child transmission of antiretroviral drug-resistant HIV strains is low in the Swiss Mother and Child HIV Cohort Study.

PMID: 30946481 2019 Swiss medical weekly

Abstract: HIV-sDRM (M184V 23%; K103N 4.5%; D67N 13.6%) occurred in 16/22 (73%) after 4 years, half of whom were treatment naïve.

Diversity of HIV-1 genotypes and high prevalence of pretreatment drug resistance in newly diagnosed HIV-infected patients in Shanghai, China.

PMID: 30961560 2019 BMC infectious diseases

Result: The most frequent NNRTI associated mutation was V179D/E, which was observed in 10.1% (32/317) of patients, followed by Y181C (2.5%, 8/55) and K103 N (1.9%, 6/317).

Prevalence of drug resistance mutations among ART-naive and -experienced HIV-infected patients in Sierra Leone.

PMID: 30989237 2019 The Journal of antimicrobial chemotherapy

Abstract: The most prevalent PDR mutations were K103N (14.3%), M184V (8.2%) and Y181C (4.1%).

Abstract: The most prevalent RAMs were K103N (40.7%),

Result: The most prevalent RT PDR mutations were as follows: K103N (n = 7, 14.3%), M184V (n = 4, 8.2%) and Y181C (n = 2, 4.1%).

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.

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