Results 21 to 30 of about 2,862,567 (165)

Screening of the NIH Clinical Collection for inhibitors of HIV-1 integrase activity

South African Journal of Science, 2018
Drug repurposing offers a validated approach to reduce drug attrition within the drug discovery and development pipeline through the application of known drugs and drug candidates to treat new indications.
Shaakira Abrahams, Salerwe Mosebi, Muhammed Q. Fish, Maria A. Papathanasopoulos, Raymond Hewer   +4 more
doaj   +1 more source

Novel therapeutic strategies targeting HIV integrase

BMC Medicine, 2012
Integration of the viral genome into host cell chromatin is a pivotal and unique step in the replication cycle of retroviruses, including HIV. Inhibiting HIV replication by specifically blocking the viral integrase enzyme that mediates this step is an ...
Quashie Peter K, Sloan Richard D, Wainberg Mark A   +2 more
doaj   +1 more source

Structural Studies of the HIV-1 Integrase Protein: Compound Screening and Characterization of a DNA-Binding Inhibitor. [PDF]

PLoS ONE, 2015
Understanding the HIV integrase protein and mechanisms of resistance to HIV integrase inhibitors is complicated by the lack of a full length HIV integrase crystal structure. Moreover, a lentiviral integrase structure with co-crystallised DNA has not been
Peter K Quashie, Ying-Shan Han, Said Hassounah, Thibault Mesplède, Mark A Wainberg   +4 more
doaj   +1 more source

Increased incidence of diabetes in people living with HIV treated with first-line integrase strand transfer inhibitors: A French multicentre retrospective study. [PDF]

HIV Med
Ursenbach A, Sireyjol A, Delpierre C, Duvivier C, Hocqueloux L, Rey D, Dat'AIDS Study Group.   +6 more
europepmc   +2 more sources

META-INSTI: metabolic adverse events following integrase strand transfer inhibitor administration in spontaneous adverse event reports

, 2023
Background: Metabolic effects of integrase strand transfer inhibitors (INSTIs) have been reported. The FDA Adverse Event Reporting System (FAERS) is a publicly available database that captures spontaneously reported adverse events.
Lara Fakhouri, Spencer E Harpe, Milena M Murray   +2 more
core   +1 more source

Nonhuman Primates and Humanized Mice for Studies of HIV-1 Integrase Inhibitors: A Review

Pathogens and Immunity, 2016
Since the discovery of the first inhibitors of HIV replication, drug resistance has been a major problem in HIV therapy, due, in part, to the high mutation rate of HIV.
Said A. Hassounah, Thibault Mesplède, Mark A. Wainberg   +2 more
doaj   +1 more source

HIV drug resistance against strand transfer integrase inhibitors

Retrovirology, 2017
Integrase strand transfer inhibitors (INSTIs) are the newest class of antiretroviral drugs to be approved for treatment and act by inhibiting the essential HIV protein integrase from inserting the viral DNA genome into the host cell’s chromatin.
Kaitlin Anstett, Bluma Brenner, Thibault Mesplede, Mark A. Wainberg   +3 more
doaj   +1 more source

Structure of a HIV-1 IN-Allosteric inhibitor complex at 2.93 Å resolution: Routes to inhibitor optimization.

PLoS Pathogens, 2023
HIV integrase (IN) inserts viral DNA into the host genome and is the target of the strand transfer inhibitors (STIs), a class of small molecules currently in clinical use.
Grant Eilers, Kushol Gupta, Audrey Allen, Saira Montermoso, Hemma Murali, Robert Sharp, Young Hwang, Frederic D Bushman, Gregory Van Duyne   +8 more
doaj   +1 more source

INSTIs and NNRTIs Potently Inhibit HIV-1 Polypurine Tract Mutants in a Single Round Infection Assay

Viruses, 2021
Integrase strand transfer inhibitors (INSTIs) are a class of antiretroviral compounds that prevent the insertion of a DNA copy of the viral genome into the host genome by targeting the viral enzyme integrase (IN).
Steven J. Smith, Andrea Ferris, Xuezhi Zhao, Gary Pauly, Joel P. Schneider, Terrence R. Burke, Stephen H. Hughes   +6 more
doaj   +1 more source

Molecular docking study of lamellarin analogues and identification of potential inhibitors of HIV-1 integrase strand transfer complex by virtual screening

Heliyon, 2019
Molecular docking has been applied to elucidate the binding of lamellarin analogues with HIV-1 integrase strand transfer complex (PDB ID: 5U1C). The results suggest hydrogen bond interaction with residue Glu92 is key, and stabilisation by π−π stacking ...
Chatchakorn Eurtivong, Kiattawee Choowongkomon, Poonsakdi Ploypradith, Somsak Ruchirawat   +3 more
doaj   +1 more source