literature

HIV mutation literature information.

Frequent cross-resistance to rilpivirine among subtype C HIV-1 from first-line antiretroviral therapy failures in South Africa.

PMID: 29566538 2018 Antiviral chemistry & chemotherapy

Method: Plasma samples contained a median of 3 [Q1-Q3: 2-4] NNRTI-associated drug resistance mutations which included A98G, L100I, K101E/H, K103N/S, V106M, V108I, E138A/K, V179D/E Y181C, Y188L/C, G190A, H221Y, P225H, F227L, and M230L.

Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.

PMID: 29353724 2018 European journal of medicinal chemistry

Abstract: Compound 4b displayed an EC50 value of 1 nM against HIV-1 IIIB, 1.3 nM against L100I, 0.84 nM against K103 N, 1.5 nM against Y181C, 11 nM against Y188L, 2 nM against E138K, 10 nM against K103 N + Y181C, and almost 110 nM against F227L + V106.

Structural optimization of N1-aryl-benzimidazoles for the discovery of new non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.

PMID: 29291935 2018 Bioorganic & medicinal chemistry

Abstract: The best results were observed for derivatives 29 and 33 active also against the double mutants F227L and V106A.

"Discovery of novel diarylpyrimidines as potent HIV-1 NNRTIs by investigating the chemical space of a less explored ""hydrophobic channel""."

PMID: 29349445 2018 Organic & biomolecular chemistry

Abstract: Against mutant strains Y181C, Y188L and F227L + V106A, Z17 showed double-digit nanomolar inhibitory activity with EC50 values 27 nM, 98 nM and 30 nM, respectively.

Discovery of novel piperidine-substituted indolylarylsulfones as potent HIV NNRTIs via structure-guided scaffold morphing and fragment rearrangement.

PMID: 27750153 2017 European journal of medicinal chemistry

Abstract: Furthermore, most compounds maintained high activity agaist various single HIV-1 mutants (L100I, K103N, E138K, Y181C) as well as one double mutant (F227L/V106A) with EC50 values in low-micromolar to double-digit nanomolar concentration ranges.

Polymorphisms and Mutational Covariation Associated with Death in a Prospective Cohort of HIV/AIDS Patients Receiving Long-Term ART in China.

PMID: 28099515 2017 PloS one

Table: F227L

HIV-1 drug-resistant mutations and related risk factors among HIV-1-positive individuals experiencing treatment failure in Hebei Province, China.

PMID: 28114955 2017 AIDS research and therapy

Table: F227L

Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.

PMID: 28481112 2017 Journal of medicinal chemistry

Abstract: Compound 25a was exceptionally potent against the whole viral panel, affording 3-4-fold enhancement of in vitro antiviral potency against WT, L100I, K103N, Y181C, Y188L, E138K, and K103N+Y181C and 10-fold enhancement against F227L+V106A relative to the reference drug etravirine (ETV) in the same cellular assay.

Antiretroviral Drug Resistance Mutations among HIV Treatment Failure Patients in Tehran, Iran.

PMID: 29026792 2017 Iranian journal of public health

Table: F227L

Upward trends of acquired drug resistances in Ethiopian HIV-1C isolates: A decade longitudinal study.

PMID: 29049402 2017 PloS one

Table: F227L