Conclusion: The drug resistance-associated major mutations, K103N (6.67%) and Y181C (7.14%), were detected in RT genes, suggesting the emergence of TDR in Jakarta.
Result: Two major mutations against NNRTIs, K103N and Y181C, were detected in peripheral blood samples derived from 2 patients, SS21 and SS41 (Table 1).
Table: Y181C
Discussion: ART expansion in Indonesia may be related with the high prevalence of K103N and Y181C, because NVP and EFV are used in the firstline ART regimens in this country.
Discussion: Samples from SS21 and SS41 contained K103N and Y181C mutations that
New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
PMID: 32883642
2020
European journal of medicinal chemistry
Abstract: Among these, IAS 12 exhibited a remarkable antiviral activity against single and double mutants (K103N EC50 = <0.7 nM; Y181C EC50 = <0.7 nM; Y188L EC50 = 21.3 nM; K103N-Y181C EC50 = 6.2 nM), resulting equally or more active than previuosly reported IAS 6 and some approved anti-HIV-1 drugs.
Abstract: Docking and molecular dynamics simulations of compound 12 in complex with WT, Y181C, Y188L, K103N and K103N-Y181C RTs clarified a general binding mode that was consistent with biological results.
Abstract: Kinetic experiments disclosed that derivative 12 preferentially binds WT and
Review of Doravirine Resistance Patterns Identified in Participants During Clinical Development.
PMID: 32925358
2020
Journal of acquired immune deficiency syndromes (1999)
Abstract: DOR was rationally designed to address limitations associated with other approved NNRTIs, particularly resistance from common NNRTI resistance-associated mutants containing K103N, Y181C, or G190A reverse transcriptase substitutions.
Introduction: D
Method: None of these participants had RT K103N, Y181C, or G190A substitutions at baseline.
Method: Overall, 4% (n = 24/656) of participants entered the trial with RT K103N, Y181C, and/or G190A substitutions.
Patterns of acquired HIV-1 drug resistance mutations and predictors of virological failure in Moshi, Northern Tanzania.
Abstract: Over the past 40 years, the frequency of the DRM M184V (50-64.3%, p=0.363), G190A (17.2-46.2%, p=0.021), and K103N (34.5-42.3%, p=0.551) increased, while the frequency of Y181C (17.2-7.7%, p=0.289) decreased.
Abstract: The major DRM in the NRTIs was the M184V, whereas the G190A, K103N, and Y181C were the major DRMs in the NNRTIs.
In Vivo Emergence of a Novel Protease Inhibitor Resistance Signature in HIV-1 Matrix.
Result: Baseline genotype (pre-PI) indicated that the individual had developed extensive resistance to first-line ART, with the nucleoside reverse transcriptase inhibitor (NRTI) mutations K65R and M184I conferring high-level tenofovir and lamivudine resistance, respectively, as well as K103N and Y181C conferring resistance to nonnucleoside reverse transcriptase inhibitors (NNRTI).
Table: Y181C
Prevalence of human immunodeficiency virus-1 drug-resistant mutations among adults on first- and second-line antiretroviral therapy in a resource-limited health facility in Busia County, Kenya.
PMID: 33654530
2020
The Pan African medical journal
Introduction: A study on HIV-1 drug-resistance patterns in Nairobi identified M184V, K65R, T215Y and K70R mutations conferring resistance to NRTIs and K103N, G190A, V106A, Y184V, A98G, Y181C mutations conferring resistance to NNRTIs.
Result: Predominant NNRTIs mutations were K103N, Y181C, G190A, H221Y, and K101E; NRTIs
Compromise of Second-Line Antiretroviral Therapy Due to High Rates of Human Immunodeficiency Virus Drug Resistance in Mozambican Treatment-Experienced Children With Virologic Failure.
PMID: 30364958
2020
Journal of the Pediatric Infectious Diseases Society
Abstract: M184V and Y181C were the most common mutations.
Drug resistance evolution in patients with human immunodeficiency virus-1 under long-term antiretroviral treatment-failure in Yunnan Province, China.
Discussion: A competitive relationship among drug-resistant strains during long-term antiviral treatment (especially with NNRTIs) exists due to the presence of Y181C/I/V and K103 N/R/S, which affect the binding of NNRTIs to the active sites of the enzymes.
Discussion: In this study, the occurrence rates for K103 N/R/S, G190A, and V106A were higher than that for Y181C/I/V; however, after a long period, the Y181C/I/V and K103 N/R/S mutations showed a greater prevalence.
Discussion: Previous studies have performed adaptive sequencing of subjects receiving
HIV mutation literature information.
PMID: 
2020
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