Transmitted HIV-1 drug resistance in a large international cohort using next-generation sequencing: results from the Strategic Timing of Antiretroviral Treatment (START) study.
Abstract: Using the 2% detection threshold, individual DRMs with the highest prevalence were: PI M46IL (5.5%), RT K103NS (3.5%), RT Discussion: However, mutations like the RT K103NS, the T215 revertants and the PI L90M appear to have little effect on viral fitness and may persist for prolonged periods in individuals with TDR.
Discussion: Of the most frequent NNRTI DRMs, G190ASE occurred predominately as minor variants while K103NS was dominant in the quasispecies.
"Detection of Drug Resistance Mutations in the Reverse Transcriptase Gene of HIV-1-Infected North Indian Population Failing First-Line Antiretroviral Therapy ""A Follow-Up Cohort Study""."
PMID: 33390085
2021
AIDS research and human retroviruses
Abstract: Drug resistance mutation M184V (ATG to GTA) (63.15%) associated with lamivudine and abacavir and K103N (AAG or AAA to AAU) (36.84%) associated with efavirenz and nevirapine were predominantly identified in first-line ART failure patients.
Analysis and Molecular Determinants of HIV RNase H Cleavage Specificity at the PPT/U3 Junction.
Introduction: However, nevirapine had no effect on PPT removal in reactions carried out with HIV-1 RT containing the drug resistance-associated substitution K103N.
Discussion: However, doravirine appears to be more efficient than efavirenz and/or rilpivirine in suppressing resistance breakthrough of HIV-1 strains with the common NNRTI resistance-associated mutations such as K103N, Y181C or K103N/Y181C.
Discussion: The effectiveness of doravirine in suppressing transmitted drug resistance mediated by K103N was crucial for its approval.
Discussion: The highest levels of doravirine resistance (fold-change >100) have been associated with amino acid substitutions V106A
Increase in HIV-1-transmitted drug resistance among ART-naive youths at the China-Myanmar border during 2009 ~ 2017.
Abstract: The most common mutations Y181I/C and K103N, were found in 7 and 9 youths, respectively.
Result: <
Result: K103N and Y181C were the most common TDRMs in NNRTI.
Table: K103N
Discussion: Among these mutations, K103N (n = 9) and Y181C/I (n = 7) were the most common TDRMs.
Discussion: In summary, large sample size and more epidemiological data are required to evaluate the potential role of three classes of TDR (NNRTI/NRTI/PI) or K103N, Y181C in affecting the decline of CD4 count.
HIV drug resistance and HIV transmission risk factors among newly diagnosed individuals in Southwest China.
Discussion: High-level resistance to efavirenz and nevirapine primarily resulted from the mutations K103N, L100I, and P225H.
Identification of novel potent HIV-1 inhibitors by exploiting the tolerant regions of the NNRTIs binding pocket.
PMID: 33567378
2021
European journal of medicinal chemistry
Abstract: Compounds 16a1 and 16b1 turned out to be the most potent inhibitors against WT and mutant HIV-1 strains (L100I, K103N, and E138K), with EC50 values ranging from 0.007 muM to 0.043 muM.
Prevalence of transmitted HIV-1 drug resistance among treatment-naive individuals in China, 2000-2016.
Result: Four SDRMs increased in prevalence in RTI-naive persons including K103N, V106M, and G190A/E while L100I decreased in prevalence among RTI-naive persons.
Result: The SDRMs with the lowest treated/naive prevalence ratios were G190E (11-fold) and K103N (22-fold).
High HIV-1 Virological Failure and Drug Resistance among Adult Patients Receiving First-Line ART for At least 12 Months at a Decentralized Urban HIV Clinic Setting in Senegal before the Test-and-Treat.
Abstract: Of the 27 viraemic isolates successfully genotyped, 20 (74.1%) carried DR mutations; most frequent were M184VI (55.6%), K103N (37.1%), thymidine analog mutations (29.6%), Y181CY (22.2%).
Result: The most frequent resistant genotypes to NNRTIs were K103N (37.04%), Y181CY (22.2%), and A98AG (18.5%).
Discu
Discussion: EFV and NVP have a lower genetic barrier, thus facilitating the selection of K103N and Y181C mutations.
Discussion: In subgroup analysis of DR, most widespread DRMs among failing patients were 3TC-resistance M184V and NVP-resistance K103N.
Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
Abstract: Interestingly, few compounds displayed remarkable activity in inhibiting K103N mutant virus with EC50 values ranging from 39 nM to 1.708 microM.
Abstract: Notably, FS2 (EC50(IIIB) = 16 nM, EC50(K103N) = 39 nM, SI = 294) was identified as the most significant compound, which was considerably more potent than nevirapine, lamivudine, and comparable to zidovudine.
HIV mutation literature information.
PMID: 
2021
HIV medicine
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