Abstract: The most frequent TDR mutations were M46I (2) in the protease region and Y181C (2) from the reverse transcriptase fragment.
Result: Two TDR mutations, M46I (2) and I50V (1) were found in the protease region, and the other eight TDR mutations, K65E(1), D67N(1), T69N(1), K103N(1), Y181C(2), G190E(1), L210W(1), and P225H(1) were from the reverse transcriptase fragment.
Discussion: The most common TDR mutations were
[Indicators of the human immunodeficiency virus drug resistance to antiretroviral drugs in HIV-infected individuals in the Siberian Federal District in 2010-2012].
Abstract: Among the main drug resistance mutations for the entire period of observation was a high frequency of the occurrence M184V mutation, K101E, K103N, Y181C, and G190S influencing the development of the HIV resistance to nucleoside and non-nucleoside reverse transcriptase inhibitors.
Identification of mechanistically distinct inhibitors of HIV-1 reverse transcriptase through fragment screening.
Abstract: Three compounds were found to inhibit RNA- and DNA-dependent DNA polymerase activity of HIV-1 RT in the micromolar range while retaining potency against RT variants carrying one of three major NNRTI resistance mutations: K103N, Y181C, or G190A.
The HEPT Analogue WPR-6 Is Active against a Broad Spectrum of Nonnucleoside Reverse Transcriptase Drug-Resistant HIV-1 Strains of Different Serotypes.
PMID: 26055365
2015
Antimicrobial agents and chemotherapy
Abstract: In addition, WPR-6 showed excellent antiviral potency against the most prevalent NNRTI-resistant viruses containing the K103N and Y181C mutations.
The prevalence and determinants of drug-resistance-associated mutations in the HIV-1-infected MSM population of Henan Province in China.
Abstract: VF was associated with emergence of usual nevirapine mutations (Y181C/I/D, K103N and V106A/I), M184V (n = 16; 12 with lamivudine vs. 4 with emtricitabine, p = 0.04), and K65R (n = 7).
Result: Sixteen out of 23 (70%) had NNRTI mutations (Y181C/I/D: 10; K103N: 6; V106A/I: 3; Y188C/L: 2; K101Q/E: 2; M230L: 1; P225H: 1; A98G: 1; V108I: 1; F227L: 1; K238T: 1), and 10 had >1
Natural Plant Alkaloid (Emetine) Inhibits HIV-1 Replication by Interfering with Reverse Transcriptase Activity.
Introduction: K65R mutation is associated with resistance to all NRTIs except zidovudine (AZT); M184V confers resistance to abacavir (ABC), emtricitabine (FTC), and lamivudine (3TC), whereas Y181C mutation confers resistance to all NNRTIs.
Development of Nevirapine Resistance in Children Exposed to the Prevention of Mother-to-Child HIV-1 Transmission Programme in Maputo, Mozambique.
Method: A NVP RAM was considered if at least one of the following genetic changes in reverse transcriptase was detected: A98G, K101E, K101H, K101P, K103N
Result: Of these, the most frequent mutations were K103N (n = 16, 24.2%, 95% CI 13.4-34.6) and Y181C (n = 15, 22.7%, 95% CI 12.6-32.8), and G190A (n = 10, 15.2%, 95% CI 6.5-23.8).
Result: The NNRTI RAM most frequently represented in this ARV class were K103N (n = 16, 21.6%, 95% CI 12.2-31.0) and Y181C (n = 15, 20.3%, 95% CI 11.1-29.4) and G190A (n = 10, 13.5%, 95% CI 5.7-21.3).
Discovery and crystallography of bicyclic arylaminoazines as potent inhibitors of HIV-1 reverse transcriptase.
Introduction: A methyl group is expected to better fill the space vacated upon the Tyr181Cys exchange than a fluorine.
Introduction: Assays tested activity against wild-type HIV-1 and the most common clinically observed viral variants, which contain Tyr181Cys (Y181C) and Lys103Asn (K103N) point mutations in the reverse transcriptase enzyme.
Introduction: Overall, 3 is among the best examples with EC50 values of 0.31, 46, and 24 nM towards wild-type HIV-1, and virus containing the Y181C mutation and the particularly challenging K103N/Y181C double variant.
Introduction: The indolizine 4 shows excellent potency towards the wild-type virus and the double variant,
The use of dried blood spot specimens for HIV-1 drug resistance genotyping in young children initiating antiretroviral therapy.
PMID: 26192603
2015
Journal of virological methods
Abstract: Non-nucleoside reverse transcriptase inhibitor mutations were most commonly detected in both specimen types, particularly Y181C/I and K103N/S.
Introduction: Non-nucleoside reverse transcriptase inhibitor (NNRTI) mutations were the most commonly detected in DBS and plasma, particularly Y181C/I (28% and 27%) and K103N/S (15% and 13%) respectively (Figure 1).
HIV mutation literature information.
PMID: 
2015
Medicine
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