literature

HIV mutation literature information.

"Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the ""NNRTI Adjacent"" Binding Site."

PMID: 29670696 2018 ACS medicinal chemistry letters

Abstract: Especially, 20 showed marked antiviral activity, which was 1.5-fold greater against WT and 1.5- to 3-fold greater against L100I, K103N, Y181C, Y188L, and E138K when compared with ETV.

Rapid Development of High-Level Resistance to Dolutegravir With Emergence of T97A Mutation in 2 Treatment-Experienced Individuals With Baseline Partial Sensitivity to Dolutegravir.

PMID: 30568974 2018 Open forum infectious diseases

Discussion: In an analysis of individual derived isolates with E138K, G140S, and Q148H, the FC to bictegravir is reported to be as high as 19-fold (2-19), whereas baseline DTG FC was 63 (3-63).

Discussion: In these cases, genotypic analysis revealed that T97A emerged in addition to other mutations, including E92E/Q, E138E/K, and N155H.

Characterization of minority HIV-1 drug resistant variants in the United Kingdom following the verification of a deep sequencing-based HIV-1 genotyping and tropism assay.

PMID: 30409215 2018 AIDS research and therapy

Result: Most of the minority mutations in viruses from both groups of naive patients were observed in the RT, e.g., M41L, E44D, A62V, K65R, D67N, D67G, V75I, L100I, K103N, K103R, V188I, M184I, L210W, K219Q, Y318F, etc., although a number of minority mutations associated with resistance to PI (L10F, V11I, M46I/

The High Genetic Barrier of EFdA/MK-8591 Stems from Strong Interactions with the Active Site of Drug-Resistant HIV-1 Reverse Transcriptase.

PMID: 30174310 2018 Cell chemical biology

Discussion: EFdA also retained its potency against the viruses containing not only M184V/I mutation, but also E138K mutation, which caused virological failure during the clinical trials that evaluated rilpivarine with emtricitabine as a first-line therapy.

Detection of minority drug resistant mutations in Malawian HIV-1 subtype C-positive patients initiating and on first-line antiretroviral therapy.

PMID: 29977795 2018 African journal of laboratory medicine

Result: The common minority NNRTI mutations detected were V106M, V179T and G190A (3/20 each), followed by E138K and Y181C (2/20 each), and K101P, K103N, V108I, E138A, V179D, A190E and H221Y (1/20 each).

Table: E138K

Selective resistance profiles emerging in patient-derived clinical isolates with cabotegravir, bictegravir, dolutegravir, and elvitegravir.

PMID: 30119633 2018 Retrovirology

Result: In contrast, the loss of T66I in 14624 was accompanied by the acquisition of L74M/E138K/S147G/M154IM and L74M/G140GS/S147G at week 27 with DTG and CAB, respectively.

Result: Resistance profiles associated with escape from EVG drug pressure were associated with T66I and the accumulation of major resistance including Q148R/K, E138K, and S147G.

Result: Selection of strain E78004 with CAB resulted in high level resistance along a Q148R/E138K/

PMID: 29699924 2018 Bioorganic & medicinal chemistry letters

Abstract: The result showed that RT- E138K/M184V mutant virus conferred 4.7-9.1-fold resistance to 4c, 4f, 2 and 6b, but only showed slight resistance to 4b (2-fold) which was better than SG-1.

Etravirine combined with antiretrovirals other than darunavir/ritonavir for HIV-1-infected, treatment-experienced adults: Week 48 results of a phase IV trial.

PMID: 28382208 2017 SAGE open medicine

Result: Other etravirine RAMs that each emerged in <5 VFs were V90I, E138G, E138K, and E138Q.

Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.

PMID: 28465101 2017 Bioorganic & medicinal chemistry letters

Abstract: Newly synthesized p-cyanovinyl-DAANs (8a-8g) with different R1 side chains plus prior active p-cyanoethyl-DAANs (4a-4c) were evaluated not only for anti-HIV potency against both wild-type HIV virus and rilpivirine-resistant (E138K, E138K+M184I) viral replication, but also for multiple drug-like properties, including aqueous solubility, lipophilicity, and metabolic stability in human liver microsomes and human plasma.

Abstract: This study revealed that both ester and amide R1 substituents led to low nanomolar anti-HIV potency against wild-type and rilpivirine-resistant viral strains (E138K-resistance fold changes<3).

Introduction: Furthermore, these same DAANs also inhibited the E138K+M184I viral strain with resistance FCs ranging from 1.4 to 6.3, better than or sim

Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.

PMID: 28254696 2017 European journal of medicinal chemistry

Abstract: Activity against the clinic prevalent mutant strains was also tested, suggesting that 16d was sensitive to E138K (EC50 = 34.2 nM).

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