Result: A Slovenian cluster was identified that contributed to the spread of HIV in Serbia, and one person carrying Y181C, which originated from Serbia, was within a Serbian part of the identified cluster; however, none of the Serbian sequences showed the same mutational profile.
Discussion: Equally fit are K103N, K103S, and Y181C mutations, which were detected in four individuals from Slovenia.
HIV-1 transmission networks across Cyprus (2010-2012).
Result: The second study subject, also a Romanian citizen living in Cyprus, was also infected with a sub-subtype F1strain dual-class RT and PI resistant strain carrying D67N, K70R, M184V, T215F, Y181C, M46L, I54V and V82F mutations associated with drug resistance.
"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.
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
Result: And the inhibition assay for a panel of more mutant strains L100I, K103 N, E138K, Y181C, Y188L and F227L + V106A were conducted as well for selected compounds.
Result: Besides, all six triazole analogues had lower EC50 values than both NVP and DLV against K103 N, Y181C, F227L + V106A, meanwhile they have better potency against Y188L than NVP.
Result: But since the two compounds and 3b9 had better cytotoxic properties, they showed much higher selectivity (3b2: SI = 2631, 3b8: SI = 4189, 3b9: SI = 6800 against E138K; 3b2:
Next-generation sequencing provides an added value in determining drug resistance and viral tropism in Cameroonian HIV-1 vertically infected children.
Result: UDPS revealed a virus harboring 2 major DRMs: L74 V at minority-level (2.5%), causing high- and intermediate-level resistance respectively to didanosine and to ABC; Y181C at population-level (96.7%), causing high- and intermediate-level resistance respectively to NVP and to EFV, ETR, and RPV (Table 3).
Transmission of HIV-1 drug resistance mutations within partner-pairs: A cross-sectional study of a primary HIV infection cohort.
Result: L100I, V108I and Y181C also showed a trend toward increased cross-resistance, but when adjusted for multiple comparisons, these were no longer significant.
Table: Y181C
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.
Biophysical Characterization of Novel DNA Aptamers against K103N/Y181C Double Mutant HIV-1 Reverse Transcriptase.
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.
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.
HIV mutation literature information.
PMID: 
2018
PloS one
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