Conclusion: Etravirine RAMs include V90I, A98G, L100I, K101E/H/P, V106I, Introduction: A total of 13 mutations were initially identified as etravirine RAMs, including V90I, A98G, L100I, K101E/P, V106I, V179D/F, Y181C/I/V and G190A/S (Table 5).
Introduction: Initial drug development employed a parallel screening strategy of candidate compounds from the diarylpyrimidines, testing their activity against both wild-type HIV-1 as well as single and double mutants (including K101E + K103N and K103N + Y181C).
Role of the K101E substitution in HIV-1 reverse transcriptase in resistance to rilpivirine and other nonnucleoside reverse transcriptase inhibitors.
PMID: 17441703
2007
Journal of medicinal chemistry
Abstract: In a mutated NNRTI pocket, GW420867X either remains in a similar position compared to wild-type (RT(Leu100Ile) and RT(Tyr188Cys)) or rearranges within the pocket (RT(Lys101Glu)).
HIV-1 subtype B protease and reverse transcriptase amino acid covariation.
Abstract: The mutations involving 10 of these positions were associated with a reduced susceptibility to antiretroviral drugs; K20R, T39A, K43EQN, E203KD, H208Y, and D218E were correlated with NRTI resistance while mutations K101EQP, H221Y, K223EQ, L228HR were associated to NNRTI resistance.
In vitro selection of mutations in human immunodeficiency virus type 1 reverse transcriptase that confer resistance to capravirine, a novel nonnucleoside reverse transcriptase inhibitor.
Abstract: Both RT(Glu138Lys) and RT(Lys101Glu) have remarkably similar protein conformations to wild-type RT, except for significant movement of the mutated side-chains away from the NNRTI pocket induced by charge inversion.
Abstract: However, nevirapine contacts Lys101 and Glu138 only indirectly, via water molecules, thus the structural basis of drug resistance induced by Lys101Glu is unclear.
Abstract: However, the reduction in hydrogen bonds in the drug-water-side-chain network resulting from the mutated side-chain movement appears to be the most significant contribution to nevirapine resistance for RT(Lys101Glu).
Characterization of mutations in CRF01_AE virus isolates from antiretroviral treatment-naive and -experienced patients in Singapore.
PMID: 15608517
2005
Journal of acquired immune deficiency syndromes (1999)
Abstract: There were differences between CRF01_AE and subtype B viruses in several drug resistance mutations including the following: D67N, L210F, K101E, V106M, V179I/D, G190A/S/E, and G48V (which were more common in CRF01_AE virus) and M41L, T215Y, and V82A (which were less common in CRF01_AE virus).
Emergence of antiretroviral resistance in HIV-positive women receiving combination antiretroviral therapy in pregnancy.
Abstract: Seven primary mutations, V106A (one), Y181C (two), G190A (one), K101E (one), M184V (one), T215S (one) were detected in five (13%) women.
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
PMID: 15771439
2005
Journal of medicinal chemistry
Abstract: When tested further, it was shown that these molecules, and in particular compound 35, are globally more active than 9, 10, and efavirenz against an additional eight single [L100I, K101E, V106A, E138K, V179E, G190A/S, and F227C] and four double HIV mutant strains [L100I + K103N, K101E + K103N, K103N + Y181C, and F227L + V106A], which are clinically relevant.
Antiviral activity of GW678248, a novel benzophenone nonnucleoside reverse transcriptase inhibitor.
PMID: 16189079
2005
Antimicrobial agents and chemotherapy
Abstract: In HeLa CD4 MAGI cell culture virus replication assays, GW678248 has an IC(50) of < or =21 nM against HIV-1 isogenic strains with single or double mutations known to be associated with NNRTI resistance, including L100I, K101E, K103N, V106A/I/M, V108I, E138K, Y181C, Y188C, Y188L, G190A/E, P225H, and P236L and various combinations.
HIV mutation literature information.
PMID: 
2008
Future HIV therapy
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