Result: Major DRAMs to NNRTIs seen in the Prophylaxis plus ART Group (Group 1) were K103 N, Y181C, M230 L and L100IL and the minor DRAMs to NNRTIs seen was A98G.
Discussion: When K103 N is seen in combination with L100I as seen in this group, it confers high-level resistance to both NVP and EFV, leaving the patient with only the AZT and 3TC combination to counter the virus.
HIV Reverse Transcriptase and Protease Genes Variability Can Be a Biomarker Associated with HIV and Hepatitis B or C Coinfection.
Discussion: Patient 91_co (HIV/HCV) has the codons T12S, L19I, L74V, K103R, E122K, D123E, I135T, S163C, M184V, L214F, K219E, E224K, V245M, L100I, V106I, V179D and M230L and used the drugs 3TC, EFV and TDF for treatment.
"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.
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
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.
Result: All six compounds showed same sensitivity order against the six mutant viruses as follows: Y188L (least sensitive to these compounds) < L100I < F227L + V106A < K103 N < Y181L < E138K (
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] Figure: FC resistance was evaluated based on the contribution of the number of RPV-associated mutations (L100I, K101E/P, E138A/G/K/Q/R, V179L, Y181C/I/V, Y188L, H221Y, F227C and M230I/L) per sample with and without K103N.
Discussion: Other studies have reported an association of RPV resistance with K103N combined with other NNRTI resistance mutations, especially L100I, in clinical samples.
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.
Abstract: Among them, the most promising N1-aryl-2-arylthioacetamido-benzimidazoles and N1-aryl-2-aryloxyacetamido-benzimidazoles were also tested toward a panel of single- and double-mutants strain responsible for resistance to NNRTIs, showing in vitro antiviral activity toward single mutants L100I, K103N, Y181C, Y188L and E138K.
HIV Drug Resistance Mutations in Non-B Subtypes After Prolonged Virological Failure on NNRTI-Based First-Line Regimens in Sub-Saharan Africa.
PMID: 28129253
2017
Journal of acquired immune deficiency syndromes (1999)
Result: After adjustment, participants on zidovudine at failure were more likely to have T215F, T215Y, M41L, K70R, D67N, L210W, type-1 thymidine analog, type-2 thymidine analog, and any thymidine analogue mutations (TAMs); those on tenofovir to have K65R, K70E, Y115F, and M184I; those on efavirenz to have K103N, P225H, Y188L, and L100I; and those on nevirapine to have Y181C and G190A.
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.
Upward trends of acquired drug resistances in Ethiopian HIV-1C isolates: A decade longitudinal study.
Discussion: But on the other side, a stable rate of selection was also observed for some NRTI mutations (such as Y115F, L210W) and several NNRTI mutations (such as L100I, K101E, P225H and M230L).
HIV mutation literature information.
PMID: 
2018
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