Prevalence and characteristics of HIV drug resistance among antiretroviral treatment (ART) experienced adolescents and young adults living with HIV in Ndola, Zambia.
Result: The ten most common mutations to the drug class NNRTI included K103N (65.5%), V106A (36.2%), Y188C/L (36.2%), Y181C/V(36.2%), G190ASV(31%), K101EHP(31%), E138AGQ(29.3%), A98G(22.4%), P225H(20.7%), and V108I(17.2%).
Increased HIV-1 pretreatment drug resistance with consistent clade homogeneity among ART-naive HIV-1 infected individuals in Ethiopia.
Abstract: The most frequently observed NNRTIs-associated mutations common to both algorithms were K103N (2%), Y188L (2%), K101E (2%), and V106A (2%), while E138A (2%) was observed according to IAS-USA only.
Result: Both CPR tool and IAS-USA algorithms were concordant in identifying five NNRTIs resistance-associated mutations: K103N in one patient (1.96%), Y188L, and H221Y in another patient (1.96%), K101E in one patient (1.96%), and V106A in another patient (1.96%).
Table: Y188L
Patterns of acquired HIV-1 drug resistance mutations and predictors of virological failure in Moshi, Northern Tanzania.
Review of Doravirine Resistance Patterns Identified in Participants During Clinical Development.
PMID: 32925358
2020
Journal of acquired immune deficiency syndromes (1999)
Discussion: In this NNRTI-experienced population (N = 6893), intermediate-level (defined as detection of any RT V106A/M, Y188C/H, V108I, and K103N + P225H substitution) and high-level (defined as detection of any RT Y188L, M230L, G190E, V106A/M + F227L, and V106A/M + L234I substitutions) DOR resistance was seen in 12.7% and 6.1%, respectively, and the most common high-level DOR resistance-associated substitution was PMID: 32883642
2020
European journal of medicinal chemistry
Abstract: Among these, IAS 12 exhibited a remarkable antiviral activity against single and double mutants (K103N EC50 = <0.7 nM; Y181C EC50 = <0.7 nM; Y188L EC50 = 21.3 nM; K103N-Y181C EC50 = 6.2 nM), resulting equally or more active than previuosly reported IAS 6 and some approved anti-HIV-1 drugs.
Abstract: Docking and molecular dynamics simulations of compound 12 in complex with WT, Y181C, Y188L, K103N and K103N-Y181C RTs clarified a general binding mode that was consistent with biological results.
Exploring the hydrophobic channel of NNIBP leads to the discovery of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs.
Abstract: Especially, compound 26 exhibited the most potent activity against wild-type and a panel of single mutations (L100I, K103N, Y181C, Y188L and E138K) with an EC50 ranging from 6.02 to 23.9 nmol/L, which were comparable to those of etravirine (ETR).
Result: All the compounds were further evaluated against a panel of clinically relevant NNRTIs-resistant single-mutant strains (L100I, K103N, Y181C, Y188L, E138K) and double-mutant strains F227L + V106A, RES056.
Result: Compound 26 demonstrated the most active potency towa
HIV-1 Drug Resistance, Distribution of Subtypes, and Drug Resistance-Associated Mutations in Virologic Failure Individuals in Chengdu, Southwest China, 2014-2016.
Result: Among the key DRMs for NNRTIs, Y188C/F/L (0.9%, 3/322), K103N (0.6%, 2/322) and G190A (0.3%, 1/322) conferred high-level resistance, K101E (0.9%, 3/322) and P225H (0.9%, 3/322) conferred intermediate resistance and H221Y (0.9%, 3/322) conferred low-level resistance.
Table: Y188L/N
Discussion: Among the NNRTI resistance mutations in this study, the key mutations were K103N, Y188L and G190A, which usually cause high-level resistance to NNRTIs but whose frequencies were low among the participants
Prevalence of human immunodeficiency virus-1 drug-resistant mutations among adults on first- and second-line antiretroviral therapy in a resource-limited health facility in Busia County, Kenya.
PMID: 33654530
2020
The Pan African medical journal
Table: Y188L
Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
PMID: 32712537
2020
European journal of medicinal chemistry
Abstract: Among all the chiral derivatives, (S)-(-)-12a showed the best potency with the antiviral activities against wild-type (WT) and single mutant strains (L100I, K103 N, Y181C, E138K; especially Y188L), and RT enzyme in the low nanomolar concentration range.
HIV mutation literature information.
PMID: 
2020
PloS one
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