Preclinical and Clinical Profile of HIV-1 Integrase Strand-transfer Inhibitor GS-9224 Compared to its Parent Compound GS-9160

2014 ◽  
Vol 06 (03) ◽  
Author(s):  
Gregg S Jones Rebecca Hluhanich
Keyword(s):  
Parent Compound ◽  
Clinical Profile ◽  
Strand Transfer ◽  
Transfer Inhibitor ◽  
Integrase Strand Transfer Inhibitor ◽  
Hiv 1

Transmission of integrase strand-transfer inhibitor multidrug-resistant HIV-1: case report and response to raltegravir-containing antiretroviral therapy

2011 ◽  
Vol 16 (2) ◽  
pp. 253-256 ◽  
Author(s):  
Benjamin Young ◽  
Signe Fransen ◽  
Kenneth S Greenberg ◽  
Amy Thomas ◽  
Sharon Martens ◽  
...  
Keyword(s):  
Case Report ◽  
Antiretroviral Therapy ◽  
Multidrug Resistant ◽  
Strand Transfer ◽  
Transfer Inhibitor ◽  
Integrase Strand Transfer Inhibitor ◽  
Hiv 1

HIV-1 Integrase Diversity and Resistance-Associated Mutations and Polymorphisms Among Integrase Strand Transfer Inhibitor-Naive HIV-1 Patients from Cameroon

2020 ◽  
Vol 36 (5) ◽  
pp. 450-455 ◽  
Author(s):  
Sello Given Mikasi ◽  
Josiah Otwoma Gichana ◽  
Cheri Van der Walt ◽  
Dominik Brado ◽  
Adetayo Emmanuel Obasa ◽  
...  
Keyword(s):  
Strand Transfer ◽  
Transfer Inhibitor ◽  
Integrase Strand Transfer Inhibitor ◽  
Hiv 1

Weight gain in antiretroviral therapy-naive HIV-1-infected patients starting a regimen including an integrase strand transfer inhibitor or darunavir/ritonavir

Infection ◽  
2019 ◽  
Vol 48 (2) ◽  
pp. 213-221 ◽  
Author(s):  
Leonardo Calza ◽  
Vincenzo Colangeli ◽  
Marco Borderi ◽  
Isabella Bon ◽  
Aurora Borioni ◽  
...  
Keyword(s):  
Weight Gain ◽  
Antiretroviral Therapy ◽  
Strand Transfer ◽  
Transfer Inhibitor ◽  
Integrase Strand Transfer Inhibitor ◽  
Hiv 1

scholarly journals Lack of impact of pre-existing T97A HIV-1 integrase mutation on integrase strand transfer inhibitor resistance and treatment outcome

PLoS ONE ◽  
2017 ◽  
Vol 12 (2) ◽  
pp. e0172206 ◽  
Author(s):  
Michael E. Abram ◽  
Renee R. Ram ◽  
Nicolas A. Margot ◽  
Tiffany L. Barnes ◽  
Kirsten L. White ◽  
...  
Keyword(s):  
Treatment Outcome ◽  
Strand Transfer ◽  
Transfer Inhibitor ◽  
Inhibitor Resistance ◽  
Integrase Strand Transfer Inhibitor ◽  
Hiv 1

scholarly journals In SilicoandIn VitroComparison of HIV-1 Subtypes B and CRF02_AG Integrases Susceptibility to Integrase Strand Transfer Inhibitors

2012 ◽  
Vol 2012 ◽  
pp. 1-13 ◽  
Author(s):  
Xiaoju Ni ◽  
Safwat Abdel-Azeim ◽  
Elodie Laine ◽  
Rohit Arora ◽  
Osamuede Osemwota ◽  
...  
Keyword(s):  
Structural Features ◽  
Strand Transfer ◽  
Binding Modes ◽  
Medical Treatments ◽  
Sequence Variations ◽  
Transfer Inhibitor ◽  
Dna Substrate ◽  
Integrase Strand Transfer Inhibitor ◽  
Hiv 1

Most antiretroviral medical treatments were developed and tested principally on HIV-1 B nonrecombinant strain, which represents less than 10% of the worldwide HIV-1-infected population. HIV-1 circulating recombinant form CRF02_AG is prevalent in West Africa and is becoming more frequent in other countries. Previous studies suggested that the HIV-1 polymorphisms might be associated to variable susceptibility to antiretrovirals. This study is pointed to compare the susceptibility to integrase (IN) inhibitors of HIV-1 subtype CRF02_AG IN respectively to HIV-1 B. Structural models of B and CRF02_AG HIV-1 INs as unbound enzymes and in complex with the DNA substrate were built by homology modeling. IN inhibitors—raltegravir (RAL), elvitegravir (ELV) and L731,988—were docked onto the models, and their binding affinity for both HIV-1 B and CRF02_AG INs was compared. CRF02_AG INs were cloned and expressed from plasma of integrase strand transfer inhibitor (INSTI)-naïve infected patients. Ourin silicoandin vitrostudies showed that the sequence variations between the INs of CRF02_AG and B strains did not lead to any notable difference in the structural features of the enzyme and did not impact the susceptibility to the IN inhibitors. The binding modes and affinities of INSTI inhibitors to B and CRF02_AG INs were found to be similar. Although previous studies suggested that several naturally occurring variations of CRF02_AG IN might alter either IN/vDNA interactions or INSTIs binding, our study demonstrate that these variations do affect neither IN activity nor its susceptibility to INSTIs.

Sign in / Sign up

Export Citation Format

Share Document