literature

HIV mutation literature information.

Effect of alpha-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.

PMID: 30525601 2019 Journal of medicinal chemistry

1Abstract: The various alpha-methoxy DABO series (12-14) present different SAR at the dihalo benzyl substitution, with the most potent compounds (12d,e and 13c) showing similar (picomolar/nanomolar) anti-HIV-1 potency as the corresponding alpha-methyl analogues against wt HIV-1, and 10-100-fold increased potency (up to low nanomolar) against clinically relevant K103N, Y181C, Y188L, IRLL98, and K103N+Y181C HIV-1 mutant strains, highlighting the importance of the alpha-methoxy substitution to provide highly efficient DABOs as ""second generation"" NNRTIs."

Rare occurrence of doravirine resistance-associated mutations in HIV-1-infected treatment-naive patients.

PMID: 30476106 2019 The Journal of antimicrobial chemotherapy

Abstract: Overall, the presence of at least one doravirine resistance-associated mutation (n = 137; 1.4%) or the K103N/Y181C mutations (n = 5; 0.05%) was very rare.

Abstract: We studied the prevalence of doravirine resistance-associated mutations previously identified in vitro: V106A/M, V108I, Y188L, V190S, H221Y, F227C/L/V, M230I/L, L234I, P236L, Y318F and K103N/Y181C.

Torsional flexibility of undecorated catechol diether compound as potent NNRTI targeting HIV-1 reverse transcriptase.

PMID: 30445408 2019 Journal of molecular graphics & modelling

Abstract: In this study, torsional flexibility of an undecorated catechol diether compound in the binding pocket of wild type and mutants (Y181C and K103N/Y181C) HIV-1 RT is investigated by using QM/MM calculations.

A comparison between two dolutegravir-based two-drug regimens as switch strategies in a multicentre cohort of HIV-1-infected patients.

PMID: 30277466 2019 Antiviral therapy

Abstract: In the RPV group, during 371.0 PYFU, there were 5 VF (1 developed non-nucleoside reverse transcriptase inhibitor mutations Y181C and E138Q) and 13 TD.

Trends in the Molecular Epidemiology and Genetic Mechanisms of Transmitted Human Immunodeficiency Virus Type 1 Drug Resistance in a Large US Clinic Population.

PMID: 29846534 2019 Clinical infectious diseases

Result: Figure 5 contains a time-scaled Bayesian phylogenetic tree that illustrates in red the likely origin of the cluster of 12 viruses containing the NNRTI DRM Y181C plus the PI DRM L90M.

Result: The mutations K103N/S, Y181C, Y188L, and G190A accounted for 88.5% of the 348 NNRTI SDRMs.

Figure: One individual (PID 50) was also primarily infected with this virus as a 2002 sequence obtained prior to therapy contained Y181C + L90M (indicated in red with an open triangle) and later developed

PMID: 30606670 2019 Bioorganic & medicinal chemistry

Abstract: Besides, 8i and 8k shown moderate activity against the double RT mutant (K103N + Y181C) HIV-1 RES056 strain.

Drug resistance evolution in patients with human immunodeficiency virus-1 under long-term antiretroviral treatment-failure in Yunnan Province, China.

PMID: 30621727 2019 Virology journal

Discussion: A competitive relationship among drug-resistant strains during long-term antiviral treatment (especially with NNRTIs) exists due to the presence of Y181C/I/V and K103 N/R/S, which affect the binding of NNRTIs to the active sites of the enzymes.

Discussion: In this study, the occurrence rates for K103 N/R/S, G190A, and V106A were higher than that for Y181C/I/V; however, after a long period, the Y181C/I/V and K103 N/R/S mutations showed a greater prevalence.

Discussion: Previous studies have performed adaptive sequencing of subjects receiving

Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.

PMID: 30624934 2019 Journal of medicinal chemistry

Result: As noted above, 13c2 can inhibit single (L100I, K103N, Y181C, Y188L, E138K) and double (F227+V106A) mutated HIV-RT variants (see Figure S3 for the location of these mutations).

Result: Five mutations (L100I, Y181C, Y188L, F227L, and V106) are located in the hydrophobic pocket that accommodates the benzonitrile and benzamide moieties of the ligand.

Result: In the case of L100I, Y181C, Y188L, and E138K, 13c2, 13c3, and 13c4 provided single-digit nanom

High Levels of HIV-1 Drug Resistance in Children Who Acquired HIV Infection Through Mother to Child Transmission in the Era of Option B+, Haiti, 2013 to 2014.

PMID: 30640198 2019 The Pediatric infectious disease journal

Abstract: The most frequent mutations were K103N/S (48.0%), M184V (37.5%), G190A/S (15.1%), and Y181C/G/V (14.1%).

Result: The most frequent mutations observed were K103N/S (48.0%), M184V (37.5%), G190A/S/E/Q/R (15.1%), and Y181C/G/V (13.8%) (Table 1).

Development of the R263K Mutation to Dolutegravir in an HIV-1 Subtype D Virus Harboring 3 Class-Drug Resistance.

PMID: 30648124 2019 Open forum infectious diseases

Conclusion: At that time, resistance testing showed NRTI (M184V, T69D, T215S, D67N, K219Q), NNRTI (Y181C, Y188L, H221Y) and PI (L10I, D30N, K20T, L33F, K43T, N88D) resistance, with PI resistance to nelfinavir.

Table: Y181C

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