Persistence of HIV-1 transmitted drug resistance mutations.
PMID: 23904291
2013
The Journal of infectious diseases
Table: V82F
Trends in Genotypic HIV-1 Antiretroviral Resistance between 2006 and 2012 in South African Patients Receiving First- and Second-Line Antiretroviral Treatment Regimens.
5Result: Then, the most prevalent mutation found with
Method: In our study, samples with at least one of the major PI RAM of the IAS-USA list as follows: D30N, V32I, M46I/L, I47A/V, G48V, I50L/V, I54L/M, Q58E, T74P, L76V, V82A/F/L/T/S, N83D, I84V, N88S, L90M were considered as PI-resistant issued from PI-experienced patients.
[Study on HIV-1 drug resistance profile of 257 AIDS patients with failure on the first-line antiretroviral treatment in Henan].
PMID: 22613387
2012
Zhonghua liu xing bing xue za zhi
Abstract: Two PIs mutations were detected in 257 patients: M46I/L, (1.17%) and V82F (0.39%).
Potent antiviral HIV-1 protease inhibitor GRL-02031 adapts to the structures of drug resistant mutants with its P1'-pyrrolidinone ring.
PMID: 22401672
2012
Journal of medicinal chemistry
Introduction: Mutations of V82A/T/F/S/L are very common in PI resistance and show reduced susceptibility to all the clinical PIs except DRV.
Interaction of I50V mutant and I50L/A71V double mutant HIV-protease with inhibitor TMC114 (darunavir): molecular dynamics simulation and binding free energy studies.
PMID: 22239286
2012
The journal of physical chemistry. B
Result: For example, L90M and V82F/I84V mutations open the flap a bit more in the mutant than the WT, whereas M46I mutation makes the flap more closed.
The L76V drug resistance mutation decreases the dimer stability and rate of autoprocessing of HIV-1 protease by reducing internal hydrophobic contacts.
Result: For example, Tm values for ATV resistant mutant I50L/A71V and multi-drug resistant mutant V82F/I84V were both higher than the values observed for PR by 2.2 and 4 C, respectively.
The L76V mutation in HIV-1 protease is potentially associated with hypersusceptibility to protease inhibitors Atazanavir and Saquinavir: is there a clinical advantage?
Method: The final list of mutations included M41L, E44D, D67N, T69D, K70R, L74V, L100I, K103N, V108I, V118I, Y181C, M184V, G190A, L210W, T215F, T215Y and K219Q in RT; and L33F, L33I, M46I, M46L, G48V, <
Increased expression and immunogenicity of HIV-1 protease following inactivation of the enzymatic activity.
Abstract: Mutations resulting in enzymatic inactivation (D25N) and resistance to standard antiretroviral drugs (V82F/I84V) were introduced in order to examine the impact of the enzymatic activity on immunogenicity and the possibility to induce immune responses against drug resistant protease, respectively.