نتایج جستجو برای: integrase inhibitors

تعداد نتایج: 191203  

2014
S Kumar

Substance abuse remains a major obstacle in treating HIV-infected patients. The high prevalence of drug use is responsible for lack of adherence and severe drug interactions to antiretroviral therapy in HIV positive individuals. Over the past decade, newer therapies for HIV have been developed by targeting different stages of HIV life cycle. Of importance, targeting initial binding with recepto...

Journal: :Chembiochem : a European journal of chemical biology 2015
Francesca Esposito Cristina Tintori Riccardo Martini Frauke Christ Zeger Debyser Roberto Ferrarese Gianluigi Cabiddu Angela Corona Elisa Rita Ceresola Andrea Calcaterra Valentina Iovine Bruno Botta Massimo Clementi Filippo Canducci Maurizio Botta Enzo Tramontano

HIV-1 integrase (IN) active site inhibitors are the latest class of drugs approved for HIV treatment. The selection of IN strand-transfer drug-resistant HIV strains in patients supports the development of new agents that are active as allosteric IN inhibitors. Here, a docking-based virtual screening has been applied to a small library of natural ligands to identify new allosteric IN inhibitors ...

Journal: :Bioorganic & Medicinal Chemistry Letters 2016

Journal: :Current Treatment Options in Infectious Diseases 2019

2006
Elena A. Semenova Allison A. Johnson Christophe Marchand David A. Davis Robert Yarchoan Yves Pommier

Integration is a crucial step in the life cycle of human immunodeficiency virus type 1 (HIV-1); therefore, inhibitors of HIV-1 integrase are candidates for antiretroviral therapy. Two 7-hydroxytropolone derivatives ( -hydroxytropolones) were found to inhibit HIV-1 integrase. A structure-activity relationship investigation with several tropolone derivatives from The National Cancer Institute com...

Journal: :Antimicrobial agents and chemotherapy 2015
Vincent Cutillas Thibault Mesplede Kaitlin Anstett Said Hassounah Mark A Wainberg

Clinical studies have shown that integrase strand transfer inhibitors (INSTIs) can be used effectively against HIV-1 infection. To date, no resistance substitution has been found in INSTI-naive patients treated with the new integrase inhibitor dolutegravir (DTG). In a recent selection study with DTG, using a virus bearing the H51Y substitution in integrase, the emergence of an R to K substituti...

Journal: :The Journal of biological chemistry 2009
Koen Bartholomeeusen Frauke Christ Jelle Hendrix Jean-Christophe Rain Stéphane Emiliani Richard Benarous Zeger Debyser Rik Gijsbers Jan De Rijck

Lens epithelium-derived growth factor/p75 (LEDGF/p75) is a prominent cellular interaction partner of human immunodeficiency virus-1 (HIV-1) integrase, tethering the preintegration complex to the host chromosome. In light of the development of LEDGF/p75-integrase interaction inhibitors, it is essential to understand the cell biology of LEDGF/p75. We identified pogZ as new cellular interaction pa...

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