Abstract: Notably, Z13 also showed the most potent activity against HIV-1 mutant strains including K103N (EC50 = 10 nM), E138K (EC50 = 22 nM) and RES056 (EC50 = 0.935 muM).
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.
First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
Abstract: Compound 6 was found to inhibit the wild-type (WT) and K103N/Y181C double mutant HIV-1 strains at nano- and submicromolar concentrations, respectively.
Frequent cross-resistance to rilpivirine among subtype C HIV-1 from first-line antiretroviral therapy failures in South Africa.
Abstract: Rilpivirine resistance was strongly associated with K103N especially in combination with other rilpivirine-associated mutations.
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 M
Transmission of HIV-1 drug resistance mutations within partner-pairs: A cross-sectional study of a primary HIV infection cohort.
Abstract: All children had wild-type viruses through both Sanger sequencing and UDPS, except for 1 PMTCT-exposed infant harboring minority K103N (8.31%), born to a mother exposed to AZT+3TC+NVP.
Result: By using UDPS, 1 (aged 1 year) of 7 children (14.3%) from the case-group harbored viruses with K103N (8.3% prevalence; mutational load: 190,567 copies/mL), a nonpolymorphic mutation causing high-level resistance to NVP and efavirenz (EFV).
Discussion: Interestingly, a vertically transmitted minority DRM (K103N), known to be associated with resistance to NNRTIs used both for PMTCT and first-line HAART in SSA, was found in a PMTCT-exposed infant, thus suggesting NNRTI-sparing regimens for such children.
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%).
Abstract: Among the drug-treated individuals, the results showed that K103N in the RT region was the most frequent mutation, found in 67% (6/9) of the cases, followed by M184V with 56% (5/9).
Abstract: Our study revealed that the prevalence of drug resistance was relatively high in Xinjiang and that K103N occurred at the highest rate.
Abstract: These results suggest that it is important to carry out HIV drug resistance testing, especially for the K103N mutation in the RT region, before and during the treatment process.
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, Method: HIV-1 (IIIB, K103 N/Y181C (RES056), F227L/V106A, L100I, K103 N, E138K, Y181C, and Y188L) or HIV-2 (ROD) stock (50 muL at 100-300 CCID50) (50% cell culture infectious dose) or culture medium was added to either the infected or mock-infected wells of the microtiter tray.
Low prevalence of transmitted HIV-1 drug resistance detected by a dried blood spot (DBS)-based next-generation sequencing (NGS) method in newly diagnosed individuals in Cameroon in the years 2015-16.
PMID: 29635462
2018
The Journal of antimicrobial chemotherapy
Abstract: The NNRTI mutation K103N was most commonly detected (2.7%).
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: RESULT AND DISCUSSION: K103N mutation narrowed the entrance of NNRTI binding pocket and forbade electrostatic interaction with alpha amino group of LYS103.
HIV mutation literature information.
PMID: 
2018
Organic & biomolecular chemistry
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