HIV mutation literature information.


  The genotype distribution, infection stage and drug resistance mutation profile of human immunodeficiency virus-1 among the infected blood donors from five Chinese blood centers, 2014-2017.
 PMID: 33347449       2020       PloS one
Abstract: 48 DRMs were identified from 43 samples, indicating a drug resistance prevalence of 12.1% (43/356), which include seven protease inhibitors (PIs) accessory DRMs (Q58E, L23I and I84M), two PIs major DRMs (M46I, M46L), seven nucleoside RT inhibitors DRMs (D67N, K70Q, K219R and M184L), and 32 non-nucleoside RT inhibitors DRMs (K103N, V179E, K238N, V179D,  PMID: 33364799       2020       Infection and drug resistance
Result: The most common RAMs to NRTIs were M184V and K65R (1.3%), while those for NNRTIs were V179D (4.5%), V106I (2.7%), and K103N (1.3%), and those for PIs were L10I (13.4%), A71T (5.8%), and L10V (4.0%).
Figure: The figure shows that the most common drug resistance-associated mutations were M184V (1.3%) and K65R (1.3%) for NRTIs, V179D (4.5%), V106I (2.7%) and K103N (1.3%) for  PMID: 33654530       2020       The Pan African medical journal
Abstract: Predominant NNRTIs mutations were K103N (15), Y181C (9), G190A (7), and H221Y (6) NRTIs, M184V (17), Table: K103N
Discussion: Major mutations conferring resistance to NNRTIs with K103N, Y181C, H22Y, G190A, K101E being prevalent have also been identified.


  [Prevalence of transmitted drug resistance in HIV-infected treatment-naive patients in Chile].
 PMID: 33844760       2020       Revista medica de Chile
Abstract: The mutations in reverse transcriptase were M41L, L210W, D67N, K70E, M184V, K103N (6.36%, 95% CI 3.5-10.4), G190A, E138A, K101E, and I84V in protease.


  Use of a mutation-specific genotyping method to assess for HIV-1 drug resistance in antiretroviral-naive HIV-1 Subtype C-infected patients in Botswana.
 PMID: 34036243       2020       AAS open research
Table: K103N
Discussion: By using PANDAA, we targeted the most likely mutations to develop to these medications in HIV-1 subtype C, the M184V, K103N and V106M mutations in reverse transcriptase, a targeted and cost-effective approach to genotyping is possible .
Discussion: Common drug resistance mutations associated with resistance to efavirenz include K103N (AAA/G to AAC/T) and V106M .


  Doravirine: a new non-nucleoside reverse transcriptase inhibitor for the treatment of HIV infection.
 PMID: 32163527       2020       Drugs of today (Barcelona, Spain
Abstract: It has a novel resistance pathway so that it retains in vitro activity against clinically relevant NNRTI viral mutations K103N, Y181C and G190A.


  Drug resistance after cessation of efavirenz-based antiretroviral treatment started in pregnancy.
 PMID: 32158555       2020       Southern African journal of HIV medicine
Abstract: Thirty-five (47%) of 74 samples yielded a genotype result, and four (11%) had a major drug resistance mutation: two with K103N and two with V106M.
Result: Thirty-five (47%) of 74 samples were successfully sequenced, with 4 (11%) of 35 having a major drug resistance mutation: 2 with K103N and 2 with V106M (Table 1).
Table: K103N


  Synthesis and biological evaluation of a series of 2-(((5-akly/aryl-1H-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimi din-4(3H)-ones as potential HIV-1 inhibitors.
 PMID: 32140396       2020       Acta pharmaceutica Sinica. B
Abstract: On the other hand, it was observed that those two compounds were less effective with EC50 values of 2.77 and 4.87 mumol/L for HIV-1A17 (K103N + Y181C).
Introduction: The most promising compound DB02 exhibited potent anti-HIV-1 activity against laboratory adapted strains and primary isolated strains (EC50s (concentrations inhibiting virus replication by 50%) range from 2.40 to 41.8 nmol/L), along with an improved sensitivity against K103N or Y181C than S-DABOs26.
Result: However, for HIV-1A17, a multi-drug resistant strain of NNRTIs carrying the K103N and Y181C mutations, I-11, I-12 and DB02 all showed a significantly reduced inhibitory activity with EC50 values of 2.77, 4.87 and 6.01 mumol/L.


  HIV-1 reverse transcriptase and protease mutations for drug-resistance detection among treatment-experienced and naive HIV-infected individuals.
 PMID: 32119691       2020       PloS one
Conclusion: SDRMs (D67N and D67E) belonging to the NRTIs class were found in two subjects and
Result: K103N is a non-polymorphic mutation that induces high-level reductions in the susceptibility to Nevirapine (NVP) and Efavirenz (EFV).
Result: It was also observed that the SDRMs belonged to the NNRTIs class including K103N and V106A detected in three patients.


  Design of Biphenyl-Substituted Diarylpyrimidines with a Cyanomethyl Linker as HIV-1 NNRTIs via a Molecular Hybridization Strategy.
 PMID: 32111013       2020       Molecules (Basel, Switzerland)
Abstract: Compound 10p exhibited the best activity against wild-type HIV-1 with an EC50 (50% HIV-1 replication inhibitory concentration) value of 0.027 microM, an acceptable CC50 (50% cytotoxic concentration) value of 36.4 microM, and selectivity index of 1361, with moderate activities against the single mutants (EC50: E138K, 0.17 microM; Y181C, 0.87 microM; K103N, 0.9 microM; L100I, 1.21 microM, respectively), and an IC50 value of 0.059 microM against the RT enzyme, which was six-fold higher than nevirapine (
Conclusion: The best compound 10p exhibited EC50 values of 0.027, 0.17, 0.87, 0.90, and 1.21 microM against the WT, E138K, Y181C, K103N, and L100I variants, respectively.



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