Result: The most frequently detected DRMs were M184I/V (68/82; 82.9%), K70E/R (16/82; 19.5%), and T215F/Y (17/82; 20.7%) to NRTI and K103N/S (51/82; 62.1%), P225H (15/82; 18.2%), and V106A/I/M (11/82; 13.4%) to NNRTI (Figure 1).
Temporal Trends in HIV-1 Mutations Used for the Surveillance of Transmitted Drug Resistance.
Result: Seven SDRMS increased in prevalence among NNRTI-experienced persons including K101E, Y181V, Y188C, G190S, P225H, and M230L while four decreased in prevalence including L100I, V106A, K101P, and V181I.
HIV Drug Resistance Mutations Detection by Next-Generation Sequencing during Antiretroviral Therapy Interruption in China.
Result: However, some minority DRMs at frequencies of 1%-5% disappeared, including N83D with PI-related, K70E, T215A, and K219E with NRTI-related and K101E, Y181C, H221Y and K238T with NNRTI-related, while others emerged, such as NNRTI-related V106A in patient GX088 at a frequency of 8.7%, and L23I, I47V and I84V with PI-related, D67N and
Analysis and Molecular Determinants of HIV RNase H Cleavage Specificity at the PPT/U3 Junction.
Discussion: The highest levels of doravirine resistance (fold-change >100) have been associated with amino acid substitutions V106A/G190A/F227L, E138K/Y181C/M230L and Y188L (alone or in combination with K103N or V106I).
Design of Biphenyl-Substituted Diarylpyrimidines with a Cyanomethyl Linker as HIV-1 NNRTIs via a Molecular Hybridization Strategy.
Result: The binding modes of 10p with double mutant (F227L + V106A, K103N + Y181C) RT were also predicted (see Figure S1, Supplementary Materials).
Result: These compounds were also tested in the MT-4 cells for their activities against the single mutant (L100I, E138K, Y181C, K103N, Y188L) and double RT mutant (K103N + Y181C, F227L + V106A) HIV-1 strains (Table 2).
Result: Unfortunately, these compounds were devoid of satisfactory activity against HIV-1 doub
Scaffold Hopping in Discovery of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: From CH(CN)-DABOs to CH(CN)-DAPYs.
5Result: As shown in Figure 5A-C, B4 efficiently occupied the pockets of the single amino acid mutations K103N and E138K and the double mutants F227L + V106A with an approximately ""U"" conformation, which was one of the essential condition for the antiviral activity in the DAPY scaffold."
Result: Compound B6 exhibited the highest potency against the double mutant F227L + V106A among all target compounds with EC50 values of 1.52 muM.
Result: Furthermore, compounds B3-B6 were superior to NVP (EC50 = 4.28 muM) toward the virus with double mutations F227L + V106A.
Prevalence of acquired drug resistance mutations in antiretroviral- experiencing subjects from 2012 to 2017 in Hunan Province of central South China.
Result: The most frequent mutations to NNRTIs were K103N (41.90%), Y181C (28.12%), G190A (26.48%), K101E (11.71%), V106M/A (10.94%), V108I (7.44%), 221Y (7.22%) and Y188H (5.91%).The proportion of PI-associated DRMs showed a tendency to increase from 2012 to 2017(0, 0, 0.22, 0.98, 1.86 and 3.81%).
Table: V106M/A
Pharmaceutical, clinical, and resistance information on doravirine, a novel non-nucleoside reverse transcriptase inhibitor for the treatment of HIV-1 infection.
Conclusion: SDRMs (D67N and D67E) belonging to the NRTIs class were found in two subjects and SDRMs) K103N and V106A (belonging to the NNRTIs class were found in three subjects.
Result: V106A is a non-polymorphic mutation that can cause high-level resistance to Nevirapine (NVP) and intermediate resistance to Efavirenz (EFV).
Result: V106A is associated with high-level resistance to DOR when accompanied by other DOR-associated DRMs.
Result: It was also observed that the SDRMs belonged to the NNRTIs class including K103N and V106A detected in three patients.
Table: PMID: 31976534
2020
The Journal of antimicrobial chemotherapy
Abstract: RESULTS: The frequencies of doravirine-associated resistance mutations (total dataset versus NNRTI-failing patients) were: V106A/M, 0.8% versus 2.6%; V108I, 3.3% versus 9.2%; Y188L, 1.2% versus 2.6%; G190S, 0.3% versus 2.1%; F227C/L/V, 0.5% versus 1.8%; M230I/L, 2.8% versus 0%; L234I, 0.1% versus 0.5%; K103N + Y181C, 3.9% versus 3.9%; K103N + P225H, 2.9% versus 4.7%; and K103N + L100I, 1.7% versus 3.9%, with a significantly higher proportion of these mutations in the
HIV mutation literature information.
PMID: 
2021
BioMed research international
Browser Board
Co-occurred Entities
Filtrator
ViMRT