Result: K103N, V108I, G190A, associated with resistance to NNRTIs.
Result: In addition, cluster C represents an MDR transmission network, wherein all four PHIs harboured K103N and three of the four also harboured L10I, I54V, A71V, V82A/I/T, I84I/V, and L90M.
Revealing interaction mode between HIV-1 reverse transcriptase and diaryltriazine analog inhibitor.
PMID: 19012571
2008
Chemical biology & drug design
Abstract: Lys103Asn (K103N) mutant frequently is observed in HIV-1 reverse transcriptase.
Binding modes of two novel non-nucleoside reverse transcriptase inhibitors, YM-215389 and YM-228855, to HIV type-1 reverse transcriptase.
Abstract: Although the activity of YM-228855, a derivative of YM-215389 that has two bulky and rigid cyano-moieties on the benzene ring, was 10x more potent against HIV-1 than YM-215389, its anti-HIV-1 activity was readily reduced with single substitutions as with Y181I and K103N.
Abstract: BACKGROUND: YM-215389 and YM-228855 are thiazolidenebenzenesulfonamide (TBS) derivatives and novel non-nucleoside reverse transcriptase inhibitors (NNRTIs) that inhibit not only wild-type, but also the K103N- and Y181C-substituted reverse transcriptase (RT) of HIV type-1 (HIV-1).
Short communication: Different mutation patterns in subtype CRF06_cpx after mother-to-child transmission.
PMID: 19032066
2008
AIDS research and human retroviruses
Abstract: GRT during follow-up showed selection of L74V/K103N/M184V/M230L in RT and M46I/H63Q/N88S in PR.
Variability in the plasma concentration of efavirenz and nevirapine is associated with genotypic resistance after treatment interruption.
Abstract: Emergence of resistant variants (including K103N, Y181C or G190S) after interruption was associated with a higher coefficient of variation in NNRTI plasma concentrations during the treatment period.
[Study on the threshold of HIV-1 drug resistance in Hunan province].
PMID: 19103115
2008
Zhonghua liu xing bing xue za zhi
Abstract: RESULTS: A total number of 69 patients whose HIV sequences were amplified successfully with 2 (2.9%) specimens appeared mutations associated with HIV-1 drug resistance in the reverse transcriptase region, including one as V75M and the other one as K103N and V181C.
Successful application of laboratory tools for the detection of HIV drug resistance in routine clinical care in Georgia.
Abstract: Etravirine is active against HIV with single mutations in the reverse transcriptase (e.g., K103N) that confer class resistance to first-generation NNRTIs.
Conclusion: Etravirine is a newer generation NNRTI with proven efficacy against HIV-1, which has developed resistance to earlier NNRTIs, including mutants with single K103N and Y181C mutations.
Introduction: In a multivariate analysis, the total number of baseline NRTI and/or NNRTI mutations, and not K103N or Y181C in particular, predicted virologic response.
Introduction: Initial drug development employed a paral
Genotype and phenotype patterns of drug-resistant HIV-1 subtype B' (Thai B) isolated from patients failing antiretroviral therapy in China.
PMID: 17019361
2007
Journal of acquired immune deficiency syndromes (1999)
Abstract: Five codons (101, 103, 108, 181, and 190) were involved in the NVP-resistant mutations, and K103N and Y181C mutations were predominant in these isolates.
Development of Novel Dihydrofuro[3,4-d]pyrimidine Derivatives as HIV-1 NNRTIs to Overcome the Highly Resistant Mutant Strains F227L/V106A and K103N/Y181C.
Abstract: Lys103Asn and Tyr181Cys are the two mutations frequently observed in patients exposed to various non-nucleoside reverse transcriptase inhibitor drugs (NNRTIs).
Abstract: The structure of the unliganded double mutant HIV-1 RT showed that Lys103Asn mutation facilitates coordination of a sodium ion with Lys101 O, Asn103 N and O(delta1), Tyr188 O(eta), and two water molecules.
Abstract: We have determined crystal structures of Lys103Asn/Tyr181Cys mutant HIV-1 RT with and without a bound non-nucleoside inhibitor (HBY 097, (S)-4-isopropoxycarbonyl-6-methoxy-3-(methylthio-methyl)-3,4-dihydroquinoxalin-2(1H)-thione) at 3.0 A and 2.5 A resolution, re