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.
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.
Discussion: Some of these mutations have been identified in other similar studies in Kenya with K103N and M184V being predominant.
[Prevalence of transmitted drug resistance in HIV-infected treatment-naive patients in 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.
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 .
Discussion: Firstly, we only examined the most common relevant resistant mutations, V106M, K103N and M184V of the reverse transcriptase; therefore, there was a limited number of positive mutations available
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.
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.
Result: Since the new gen
HIV-1 reverse transcriptase and protease mutations for drug-resistance detection among treatment-experienced and naive HIV-infected individuals.
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.