literature

HIV mutation literature information.

Pharmaceutical, clinical, and resistance information on doravirine, a novel non-nucleoside reverse transcriptase inhibitor for the treatment of HIV-1 infection.

PMID: 32180823 2020 Drugs in context

Introduction: In almost all cases, DOR selected first for V106A/M substitutions.

Introduction: Mutations that emerged secondary to V106A/M included F227L/C/V or L234I.

Introduction: Other in vitro studies confirmed that viruses bearing both V106A and F227L substitutions reduced DOR susceptibility >500-fold.

Prevalence of acquired drug resistance mutations in antiretroviral- experiencing subjects from 2012 to 2017 in Hunan Province of central South China.

PMID: 32183889 2020 Virology journal

Result: The most frequent mutations to NNRTIs were K103N (41.90%), Y181C (28.12%), G190A (26.48%), K101E (11.71%), V106M/A (10.94%), V108I (7.44%), 221Y (7.22%) and Y188H (5.91%).The proportion of PI-associated DRMs showed a tendency to increase from 2012 to 2017(0, 0, 0.22, 0.98, 1.86 and 3.81%).

Table: V106M/A

Scaffold Hopping in Discovery of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: From CH(CN)-DABOs to CH(CN)-DAPYs.

PMID: 32235557 2020 Molecules (Basel, Switzerland)

5Result: As shown in Figure 5A-C, B4 efficiently occupied the pockets of the single amino acid mutations K103N and E138K and the double mutants F227L + V106A with an approximately ""U"" conformation, which was one of the essential condition for the antiviral activity in the DAPY scaffold."

Result: Compound B6 exhibited the highest potency against the double mutant F227L + V106A among all target compounds with EC50 values of 1.52 muM.

Result: Furthermore, compounds B3-B6 were superior to NVP (EC50 = 4.28 muM) toward the virus with double mutations F227L + V106A.

Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.

PMID: 32712537 2020 European journal of medicinal chemistry

Abstract: Toward double mutant virus strains (F227L + V106A, RES056), (S)-(-)-12a possessed submicromolar antiviral activities.

Increased HIV-1 pretreatment drug resistance with consistent clade homogeneity among ART-naive HIV-1 infected individuals in Ethiopia.

PMID: 32993693 2020 Retrovirology

Abstract: The most frequently observed NNRTIs-associated mutations common to both algorithms were K103N (2%), Y188L (2%), K101E (2%), and V106A (2%), while E138A (2%) was observed according to IAS-USA only.

Result: Both CPR tool and IAS-USA algorithms were concordant in identifying five NNRTIs resistance-associated mutations: K103N in one patient (1.96%), Y188L, and H221Y in another patient (1.96%), K101E in one patient (1.96%), and V106A in another patient (1.96%).

Table: V106A

Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.

PMID: 32977301 2020 European journal of medicinal chemistry

Abstract: More encouragingly, 14d2 (RF = 0.4) possessed higher antiresistance profile than ETV (RF = 6.3) and K-5a2 (RF = 3.0) toward the double mutant strain F227L + V106A.

Review of Doravirine Resistance Patterns Identified in Participants During Clinical Development.

PMID: 32925358 2020 Journal of acquired immune deficiency syndromes (1999)

Table: V106A

Discussion: First and foremost, in vitro studies show that, in contrast to V106A or V106M, V106I does not confer a potency reduction to DOR.

Discussion: In this NNRTI-experienced population (N = 6893), intermediate-level (defined as detection of any RT V106A/M, Y188C/H, V108I, and K103N + P225H substitution) and high-level (defined as detection of any RT Y188L, M230L, G190E, V106A/M

Prevalence and characteristics of HIV drug resistance among antiretroviral treatment (ART) experienced adolescents and young adults living with HIV in Ndola, Zambia.

PMID: 32804970 2020 PloS one

Abstract: There was a relatively high occurrence of other NNRTI mutations V106A (36.2%), as well as Y188C (36.2%) and Y181C (36.2%) which confer resistance to etravirine.

Result: Overall, the 10 most common mutations were M184V (81%), K103N (65.5%), Y188C (36.2%), Y181C (36.2%), V106A (36.2), K65R (34.5%), K70RTQNE (32.8%), G190ASV (31.0%), K101EHP (31.0%) and E138AGQ (29.3%).

Result: The ten most common mutations to the drug class

PMID: 32528834 2020 Acta pharmaceutica Sinica. B

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: For double-mutant HIV-1 strain F227L + V106A, compounds 23 and 27 were proved to be the most potent inhibitors and exhibited EC50 values of 46.6 and 49.2 nmol/L, respectively, being far more potent than NVP (EC50 > 9510 nmol/L) and EFV (EC50 = 268 nmol/L), and comparable to ETR (EC50 = 14.2 nmol/L).

Table: V106A

HIV-1 Drug Resistance in ART-Naive Individuals in Myanmar.

PMID: 32368103 2020 Infection and drug resistance

Discussion: Furthermore, we found that the major NNRTI-related SDRMs were K101P, K103N, V106A, E138A, Y181C, and Y188H, and the major NRTI-related SDRMs were L74V/I and M184V.

Discussion: Some SDRMs, including NRTI-related mutations (M41L, D67E/G/N, K70E/R, M184V, T215any, and K219any) and NNRTI-related mutations (K101E/P, K103N/

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