Design, synthesis, and antiviral evaluation of novel piperidine-substituted arylpyrimidines as HIV-1 NNRTIs by exploring the hydrophobic channel of NNIBP.
Abstract: In addition, most of the compounds displayed micromolar activity against K103N and E138K mutant strains, while FT1 (EC50(K103N) = 50 nM, EC50(E138K) = 0.19 microM) still has the most effective activity.
Characterizing HIV-1 Genetic Subtypes and Drug Resistance Mutations among Children, Adolescents and Pregnant Women in Sierra Leone.
Abstract: Among children and adolescents, the most common RAMs were M184V (76.6%, n = 49/64), K103N (45.3%, n = 29/64), Y181C/V/I (28.1%, n = 18/64), T215F/Y (25.0%, n = 16/64), and V108I (18.8%, n = 12/64).
Abstract: Among pregnant women, the most frequent RAMs were K103N (20.6%, n = 7/34), M184V (11.8%, n = 4/34), Y181C/V/I (5.9%, n = 2/34), P225H (8.8%, n = 3/34), and K219N/E/Q/R (5.9%, n = 2/34).
Result: The most prevalent RT RAMs among children and adolescents and their relative proportions were as follows: M184V
Correlation of HIV-1 drug resistant mutations and virologic failure.
PMID: 34584606
2021
The Pan African medical journal
Introduction: These mutations included M184V, K65R,D67N,K70R,K219Q,Q151M, T215F, M41L, T69N, V75M, M41L, T69N, V75M, D67G, V75M, M184I, T215N, M41LM, T215N, K219N,210W, T215Y as NRT
Table: K103N
Prevalence and factors associated with HIV-1 drug resistance mutations in treatment-experienced patients in Nairobi, Kenya: A cross-sectional study.
Abstract: NRTI primary mutations M184 V/I and K65R/E/N were found in 28.8% and 8.9% of subjects respectively, while NNRTI primary mutations K103N/S, G190A, and Y181C were found in 21.0%, 14.6%, and 10.9% of subjects.
Discussion: The high levels of resistance are due to the K103N, G190A, and Y181C mutations, which confer resistance to NVP (81.0%) and EFV (71.2%).
HIV-1 Drug Resistance Among Treatment-Naive Transgenders from India.
PMID: 34652967
2021
AIDS research and human retroviruses
Abstract: Mutations M184V, A98G, K103N, G190A, and Y318F associated with resistance to nucleoside reverse transcriptase inhibitor and non-nucleoside reverse transcriptase inhibitors were observed.
Prevalence and Molecular Epidemiology of Transmitted Drug Resistance and Genetic Transmission Networks Among Newly Diagnosed People Living With HIV/AIDS in a Minority Area, China.
Result: As for the NNRTI resistance, the majority of the HIV-1 strains showed high-level resistance to NVP (3.95%) and EFV (3.64%), and the main mutation was K103N/KN (data not shown).
Result: Besides, 37.38% (40/107) of individuals carrying TDR were involved in the network, and K103N (42.5%, 17/40) was the most frequent TDR-associated mutation, followed by E138A (15%, 6/40), I54M (7.5%, 3/40), and Discussion: K103N (42.5%, 17/40) were the most frequent TDR-associated mutations and were in five clusters in which they linked with those carrying the same mutations.
Discussion: K103N mutations might have been in circulation for a while and were unsuspectingly propagated onward in the community as new infections.
HIV-1 drug resistance among individuals who seroconverted in the ASPIRE dapivirine ring trial.
PMID: 34762770
2021
Journal of the International AIDS Society
Abstract: Overall, 18/168 (11%) had NNRTI mutations including K101E
Result: Major NNRTI mutations detected included K101E, K103N, K103S, V106M, V108I, E138A/G, V179D/I/T and H221Y, but the frequency of detection of each of these mutations did not differ by arm (Table 1).
Result: Of these six, only one participant from the placebo arm had an NNRTI resistance mutation detected (K103N) in a sample collected 8 weeks after cessation of the placebo ring.
Table: K103N
Rapid HIV-1 drug resistance testing in a resource limited setting: the Pan Degenerate Amplification and Adaptation assay (PANDAA).
PMID: 34795836
2021
The Pan African medical journal
Introduction: Briefly, the PANDAA assay is an allelic discrimination test designed with differentially labeled TaqMan probes to discriminate wild-type DNA (K65, M184, K103, Y181 and G190) from the DRMs (substitution at a specific codon position by the mutant amino acid known as K65R, M184VI, K103NS, Y181C and G190A).
Introduction: Several groups have developed point mutation assays (PMAs) that detect key DRMs (K65R and M184V for NRTIs; and K103NS, V106AM, Y181C, and G190A for NNRTIs) which are found in 98.8% o
[HIV-1 drug resistance and subtypes in newly reported HIV/AIDS patients before antiretroviral therapy in Taizhou city, 2016-2018].
PMID: 34814456
2021
Zhonghua liu xing bing xue za zhi
Abstract: The resistance mutations of NNRTIs and NRTIs were mainly K103 N (0.7%) and M184I/V (0.5%).
Genetic Diversity and Acquired Drug Resistance Mutations Detected by Deep Sequencing in Virologic Failures among Antiretroviral Treatment Experienced Human Immunodeficiency Virus-1 Patients in a Pastoralist Region of Ethiopia.
Abstract: Among NRTI resistance mutations, M184V (73.2%), K219Q (63.4%) and T215 (56.1%) complex were the most mutated positions, while the most common NNRTI resistance mutations were K103N (24.4%), K101E, P225H and V108I 7.5% each.
Result: Of the 41 viraemic specimens genotyped, the major NNRTI resistance-associated mutations detected were: K103N (24.4%), P225H (7.3%), K101E (7.3%), V108I (7.3%), V90I (4.9%), V106M/A (9.8%),
ViMRT
HIV mutation literature information.
PMID: 
2021
Bioorganic chemistry
