Results 1 to 10 of about 17,322 (222)

Pharmacology of HIV integrase inhibitors [PDF]

Current Opinion in HIV and AIDS, 2012
The purpose of this paper is to review recent and relevant pharmacology data for three HIV integrase inhibitors: raltegravir (marketed), dolutegravir and elvitegravir (both in Phase III drug development).
Jessica L, Adams, Benjamin N, Greener, Angela D M, Kashuba   +2 more
core   +5 more sources

Raltegravir: first in class HIV integrase inhibitor

Therapeutics and Clinical Risk Management, 2008
Zelalem Temesgen1, Dawd S Siraj21Mayo Clinic, Rochester, MN, USA; 2East Carolina University Greenville, NC, USAAbstract: On October 16, 2007, the US Food and Drug Administration (FDA) approved raltegravir for treatment of human immunodeficiency virus ...
Zelalem Temesgen, Dawd S Siraj
doaj   +5 more sources

HIV-2 integrase variation in integrase inhibitor-naïve adults in Senegal, West Africa. [PDF]

PLoS ONE, 2011
Antiretroviral therapy for HIV-2 infection is hampered by intrinsic resistance to many of the drugs used to treat HIV-1. Limited studies suggest that the integrase inhibitors (INIs) raltegravir and elvitegravir have potent activity against HIV-2 in ...
Geoffrey S Gottlieb, Robert A Smith, Ndeye Mery Dia Badiane, Selly Ba, Stephen E Hawes, Macoumba Toure, Alison K Starling, Fatou Traore, Fatima Sall, Stephen L Cherne, Joshua Stern, Kim G Wong, Paul Lu, Moon Kim, Dana N Raugi, Airin Lam, James I Mullins, Nancy B Kiviat, Papa Salif Sow for the UW-Dakar HIV-2 Study Group   +18 more
doaj   +2 more sources

The Discovery of Indole-2-carboxylic Acid Derivatives as Novel HIV-1 Integrase Strand Transfer Inhibitors

Molecules, 2023
As an important antiviral target, HIV-1 integrase plays a key role in the viral life cycle, and five integrase strand transfer inhibitors (INSTIs) have been approved for the treatment of HIV-1 infections so far.
Yu-Chan Wang, Wen-Li Zhang, Rong-Hong Zhang, Chun-Hua Liu, Yong-Long Zhao, Guo-Yi Yan, Shang-Gao Liao, Yong-Jun Li, Meng Zhou   +8 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

Three main mutational pathways in HIV-2 lead to high-level raltegravir and elvitegravir resistance: implications for emerging HIV-2 treatment regimens. [PDF]

PLoS ONE, 2012
Human immunodeficiency virus type 2 (HIV-2) is intrinsically resistant to non-nucleoside reverse transcriptase inhibitors and exhibits reduced susceptibility to several of the protease inhibitors used for antiretroviral therapy of HIV-1. Thus, there is a
Robert A Smith, Dana N Raugi, Charlotte Pan, Matthew Coyne, Alexandra Hernandez, Brad Church, Kara Parker, James I Mullins, Papa Salif Sow, Geoffrey S Gottlieb, University of Washington-Dakar HIV-2 Study Group   +10 more
doaj   +1 more source

Small molecule inhibitors of the LEDGF site of human immunodeficiency virus integrase identified by fragment screening and structure based design. [PDF]

PLoS ONE, 2012
A fragment-based screen against human immunodeficiency virus type 1 (HIV) integrase led to a number of compounds that bound to the lens epithelium derived growth factor (LEDGF) binding site of the integrase catalytic core domain.
Thomas S Peat, David I Rhodes, Nick Vandegraaff, Giang Le, Jessica A Smith, Lisa J Clark, Eric D Jones, Jonathan A V Coates, Neeranat Thienthong, Janet Newman, Olan Dolezal, Roger Mulder, John H Ryan, G Paul Savage, Craig L Francis, John J Deadman   +15 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

Resistance to inhibitors of the human immunodeficiency virus type 1 integration

Brazilian Journal of Infectious Diseases, 2010
This review will summarize the role of integrase in HIV-1 infection, the mechanism of integrase inhibitors and resistance with an emphasis on raltegravir (RAL), the first integrase inhibitor licensed to treat HIV-1 infection.
Daria J. Hazuda, PhD
doaj   +1 more source

Comparative biochemical analysis of HIV-1 subtype B and C integrase enzymes

Retrovirology, 2009
Background Integrase inhibitors are currently being incorporated into highly active antiretroviral therapy (HAART). Due to high HIV variability, integrase inhibitor efficacy must be evaluated against a range of integrase enzymes from different subtypes ...
Kuhl Björn D, Donahue Daniel A, Faltenbacher Verena H, Sloan Richard D, Bar-Magen Tamara, Oliveira Maureen, Xu Hongtao, Wainberg Mark A   +7 more
doaj   +1 more source