literature

HIV mutation literature information.

Short Communication: Population-Based Surveillance of HIV-1 Drug Resistance in Cameroonian Adults Initiating Antiretroviral Therapy According to the World Health Organization Guidelines.

PMID: 26602836 2016 AIDS research and human retroviruses

Abstract: Level of DRMs was low (3.77%) versus moderate (7.55%), respectively, following the WHO list (T69D, K103N) versus Stanford HIVdb (T69D, A98G, K103N, K238T), respectively.

Development of Novel Dihydrofuro[3,4-d]pyrimidine Derivatives as HIV-1 NNRTIs to Overcome the Highly Resistant Mutant Strains F227L/V106A and K103N/Y181C.

PMID: 26650686 2016 Journal of molecular graphics & modelling

Abstract: The effects of two of the most clinically relevant RT mutations (Y181C; K103N) were studied by a computational approach.

Sub-Epidemics Explain Localized High Prevalence of Reduced Susceptibility to Rilpivirine in Treatment-Naive HIV-1-Infected Patients: Subtype and Geographic Compartmentalization of Baseline Resistance Mutations.

PMID: 26651266 2016 AIDS research and human retroviruses

Method: Evidence of transmitted HIV-1 drug resistance (TDR) was defined by the presence of at least one surveillance drug resistance mutation (SDRM) from the consensus genotypic definition of Bennett et al., including major RVP-RAMs L100I+K103N, Y181C/I/V, Y188L, and M230L, and minor RPV-RAMs L100I, K103S, V106A, V179F, and G190A/E/S.

Method: Major RPV resistance-associated mutations (RPV-RAMs) were defined based on data from the clinical trials, phenotypic RPV resistance analyses, and package inserts: K101E/P, E138A/G/K/Q/R<

Simplified Paper Format for Detecting HIV Drug Resistance in Clinical Specimens by Oligonucleotide Ligation.

PMID: 26751207 2016 PloS one

Abstract: Analysis of mutations at four HIV-1 DR codons (K103N, Y181C, M184V, and G190A) in 26 blood specimens showed a strong correlation of the ratios of mutant signal to total signal between the paper CDD and the plate CDD.

Method: The selected specimens included HIV subtypes A (N = 8), C (N = 1), D (N = 5), AE (N = 9) and G (N = 3), and one or more drug resistance mutations at four codons in HIV reverse transcriptase (K103N, Y181C, G190A and M184V) spanning a wide range of frequencies in each subjects' HIV population.

Result: Clinical specimens (N = 26) from Kenyan's infected with HIV-1 subtypes A, C, D, AE and G, and plasmid standards at 0, 5 and 50% MUT were test

Ribonuclease H/DNA Polymerase HIV-1 Reverse Transcriptase Dual Inhibitor: Mechanistic Studies on the Allosteric Mode of Action of Isatin-Based Compound RMNC6.

PMID: 26800261 2016 PloS one

Conclusion: This double-site binding mode seems to confirm that it could be possible to target both RT-associated functions by a single molecule, retaining full potency of inhibition on drug-resistant mutant RTs such as K103N, Y181C and Y188L.

Method: HIV RT-associated RNase H activity was measured as described in 100 muL reaction volume containing 50 mM Tris-HCl buffer pH 7.8, 6 mM MgCl2, 1 mM dithiothreitol (DTT), 80 mM KCl, 0.25 muM hybrid RNA/DNA 5'-GAUCUGAGCCUGGGAGCU-Fluorescin-3' (HPLC, dry, QC: Mass Check) (available from Metabion) 5'-Dabcyl-AGCTCCCAGGCTCAGATC-3'(HPLC, dry, QC: Mass Check), increasing concentrations of inhibitors, whose dilution were made in water, and different amount of enzymes according to a linear r

Table: K103N

Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.

PMID: 26802545 2016 European journal of medicinal chemistry

Abstract: In particular, the inhibition of IIb against the K103N mutation (EC50 = 49 nM), which confers resistance to a wide variety of NNRTIs, was about 140 times more effective than NVP (EC50 = 6.78 muM), 50 times more than DLV (EC50 = 2.48 muM) and about 3 times more than EFV (EC50 = 0.12 muM), indicating that the newly designed compounds have great potential to be further developed as new anti-HIV-1 agents.

Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor.

PMID: 26804933 2016 Journal of medicinal chemistry

Abstract: Optimization of the phosphinate aryl substituent led to the discovery of the 3-Me,5-acrylonitrile-phenyl analogue RP-13s (IDX899) having an EC50 of 11 nM against the Y181C/K103N double mutant.

Abstract: Since a major problem associated with NNRTI treatment is the emergence of drug resistant virus, this work focused on optimization of the APhI against clinically relevant HIV-1 Y181C and K103N mutants and the Y181C/K103N double mutant.

Prevalence of Primary HIV Drug Resistance in Thailand Detected by Short Reverse Transcriptase Genotypic Resistance Assay.

PMID: 26828876 2016 PloS one

Abstract: Fourteen major mutations of codon 99-191 on the RT gene were selected (K103N, V106A/M, V108I, Q151M, Y181C/I, M184V/I, Y188C/L/H, and G190S/A) at a cost of testing of 35 USD.

Abstract: The prevalence of each HIVDR mutation were K103N 6.0%, V106I 1.1%, V108I 0.4%, Y181C 2.3%, Y181I 0.7%, Y181V 0.4%, M184V 3.0%, M184I 1.5%, and

PMID: 26833152 2016 Antimicrobial agents and chemotherapy

Abstract: DOR displayed IQs of 39, 27, and 25 against the K103N, Y181C, and K103N/Y181C mutants, respectively.

Abstract: DOR exhibits potent antiviral activity against wild-type virus and K103N, Y181C, and K103N/Y181C mutant viruses, with 50% inhibitory concentrations (IC50s) of 12, 21, 31, and 33 nM, respectively, when measured in 100% normal human serum (NHS).

Abstract: No viral breakthrough was observed with DOR, whereas breakthrough viruses were readily detected with RPV and EFV against Y181C and K103N viruses, respectively.

Novel indole sulfides as potent HIV-1 NNRTIs.

PMID: 26876929 2016 Bioorganic & medicinal chemistry letters

Abstract: In a previous communication we described a series of indole based NNRTIs which were potent inhibitors of HIV replication, both for the wild type and K103N strains of the virus.

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