Persistence of Human Immunodeficiency Virus-1 Drug Resistance Mutations in Proviral Deoxyribonucleic Acid After Virologic Failure of Efavirenz-Containing Antiretroviral Regimens.
PMID: 30863788
2019
Open forum infectious diseases
Introduction: Studies of drug resistance mutations (DRMs) in plasma virus ribonucleic acid (RNA) by Sanger consensus sequencing frequently identify mutations associated with nonnucleoside reverse-transcriptase inhibitors (NNRTIs); most often K103N, followed by G190S, V106A/M, Y181C, Y188L, and P225H.
Prevalence of predicted resistance to doravirine in HIV-1-positive patients after exposure to non-nucleoside reverse transcriptase inhibitors.
PMID: 30769200
2019
International journal of antimicrobial agents
Abstract: High-level DOR resistance was defined as detection of any of Y188L, M230L, G190E, V106A/M+F227L, and V106A/M+L234I.
Abstract: Intermediate DOR resistance was defined as detection of any of V106A/M, Y188C/H, V108I, and K103N+P225H.
Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
PMID: 30624934
2019
Journal of medicinal chemistry
Conclusion: For double mutant HIV-1 strains F227L+V106A and RES056, both inhibitors displayed comparable activities with those of ETV.
Result: As noted above, 13c2 can inhibit single (L100I, K103N, Y181C, Y188L, E138K) and double (F227+V106A) mutated HIV-RT variants (see Figure S3 for the location of these mutations).
Result: For F227L+V106A, 13c3 (EC50 = 7.2 nM) showed the highest potency and was 2.7-fold more potent than ETV (EC50 = 19.7 nM).
Result: Moreover, 13a1, 13c1, 13c2, and 13c4 also inhibited F227L+V106A (EC
Drug resistance evolution in patients with human immunodeficiency virus-1 under long-term antiretroviral treatment-failure in Yunnan Province, China.
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 NNRTIs, and confirmed that the most common mutations are as follows: Y181C/I/V > K103 N/R/S > G190A > V106A.
Rare occurrence of doravirine resistance-associated mutations in HIV-1-infected treatment-naive patients.
PMID: 30476106
2019
The Journal of antimicrobial chemotherapy
Abstract: We studied the prevalence of doravirine resistance-associated mutations previously identified in vitro: V106A/M, V108I, Y188L, V190S, H221Y, F227C/L/V, M230I/L, L234I, P236L, Y318F and K103N/Y181C.
Moderate-to-High Levels of Pretreatment HIV Drug Resistance in KwaZulu-Natal Province, South Africa.
PMID: 30430843
2019
AIDS research and human retroviruses
Abstract: The most prevalent SDRMs were K103NS (7.5%), M184VI (2.4%), and V106AM (1.4%).
"Discovery of novel diarylpyrimidines as potent HIV-1 NNRTIs by investigating the chemical space of a less explored ""hydrophobic channel""."
Discussion: The major TDRMs observed in this study have been reported in a previous study of HIV Drug Resistance among ART-failure individuals in Yunnan Province, which figured out mutations such as M184 V/I, K103 N, V106A, Y181C and G190A were common.
Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
PMID: 29635166
2018
European journal of medicinal chemistry
Conclusion: In general, a series of novel diarylnicotinamide triazole analogues were rationally designed based on structure-guided approach, synthesized and evaluated for their bioactivities against HIV-1 (IIIB, K103 N + Y181C, L100I, K103 N, E138K, Y181C, Y188L and F227L + V106A) and HIV-2 (ROD) in MT-4 cells.
Method: HIV-1 (IIIB, K103 N/Y181C (RES056), F227L/V106A, L100I, K103 N, E138K, Y181C, and Y1
Long-term virological outcome in children receiving first-line antiretroviral therapy.
Result: K103N (48%), Y181C (37%), G190A/S (25%), Y188C/L (10%), V106M/A (8%), K65R (8%) and L100I (4%) were the major NNRTI DRMs observed in these 52 children.
HIV mutation literature information.
PMID: 
2019
Open forum infectious diseases
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