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.
Frequent cross-resistance to rilpivirine among subtype C HIV-1 from first-line antiretroviral therapy failures in South Africa.
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.
Result: No other RPV-associated mutations in this sample set including K101E, E138A/K
Genotypic Characterization of Human Immunodeficiency Virus Type 1 Prevalent in Kepulauan Riau, Indonesia.
PMID: 29589465
2018
AIDS research and human retroviruses
Abstract: Furthermore, major mutations, including M184V (2.2%) and Y188L (2.2%), were identified in the viral pol gene encoding reverse transcriptase derived from a study participant, suggesting that the prevalence of HIVDR is low in the region.
Surveillance of HIV-1 drug resistance in Xinjiang: high prevalence of K103N in treatment-naive individuals.
Abstract: K103N occurred at the highest rate, accounting for 22% (6/27), followed by P225H (7%) and Y188L (4%).
Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
PMID: 29635166
2018
European journal of medicinal chemistry
Conclusion: In general, a series of novel diarylnicotinamide triazole analogues were rationally designed based on structure-guided approach, synthesized and evaluated for their bioactivities against HIV-1 (IIIB, K103 N + Y181C, L100I, K103 N, E138K, Y181C, Y188L and F227L + V106A) and HIV-2 (ROD) in MT-4 cells.
Method: HIV-1 (IIIB, K103 N/Y181C (RES056), F227L/V106A, L100I, K103 N, E138K, Y181C, and Y1
"Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the ""NNRTI Adjacent"" Binding Site."
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.
Identification of Adjacent NNRTI Binding Pocket in Multi-mutated HIV1- RT Enzyme Model: An in silico Study.
Abstract: METHODS: An in Silico model of HIV-1 RT enzyme with multiple mutations K103N, Y181C and Y188L was developed and evaluated.
Abstract: Mutations Y181C and Y188L prevented NNRTI binding by eliminating aromatic pi interactions offered by tyrosine rings.
Antiretroviral resistance among HIV-1 patients on first-line therapy attending a comprehensive care clinic in Kenyatta National Hospital, Kenya: a retrospective analysis.
PMID: 30061964
2018
The Pan African medical journal
Abstract: They included K103N (n = 10), G190A (n = 1), Y181C (n = 1) and Y188L (n = 1).
Result: They included K103N (n=10), G190A (n=1), Y181C (n=1) and Y188L (n=1) (Table 2).
Table: Y188L
Long-term virological outcome in children receiving first-line antiretroviral therapy.
Result: K103N (48%), Y181C (37%), G190A/S (25%), Y188C/L (10%), V106M/A (8%), K65R (8%) and L100I (4%) were the major NNRTI DRMs observed in these 52 children.
Research on the treatment effects and drug resistances of long-term second-line antiretroviral therapy among HIV-infected patients from Henan Province in China.
HIV mutation literature information.
PMID: 
2018
European journal of medicinal chemistry
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