Results 11 to 20 of about 3,561 (181)

Resistance to Integrase Inhibitors [PDF]

Viruses, 2010
Integrase (IN) is a clinically validated target for the treatment of human immunodeficiency virus infections and raltegravir exhibits remarkable clinical activity. The next most advanced IN inhibitor is elvitegravir.
Mathieu Metifiot, Christophe Marchand, Kasthuraiah Maddali   +2 more
exaly   +7 more sources

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
openaire   +4 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   +2 more sources

Mutations Located outside the Integrase Gene Can Confer Resistance to HIV-1 Integrase Strand Transfer Inhibitors

mBio, 2017
Resistance to the integrase strand transfer inhibitors raltegravir and elvitegravir is often due to well-identified mutations in the integrase gene. However, the situation is less clear for patients who fail dolutegravir treatment.
Isabelle Malet, Frédéric Subra, Charlotte Charpentier, Gilles Collin, Diane Descamps, Vincent Calvez, Anne-Geneviève Marcelin, Olivier Delelis   +7 more
doaj   +2 more sources

Clinical use of HIV integrase inhibitors: a systematic review and meta-analysis. [PDF]

PLoS ONE, 2013
BackgroundOptimal regimen choice of antiretroviral therapy is essential to achieve long-term clinical success. Integrase inhibitors have swiftly been adopted as part of current antiretroviral regimens. The purpose of this study was to review the evidence
Peter Messiaen, Annemarie M J Wensing, Axel Fun, Monique Nijhuis, Nele Brusselaers, Linos Vandekerckhove   +5 more
doaj   +2 more sources

Authentic HIV-1 Integrase Inhibitors [PDF]

Future Medicinal Chemistry, 2010
HIV-1 integrase (IN) is indispensable for HIV-1 replication and has become a validated target for developing anti-AIDS agents. In two decades of development of IN inhibition-based anti-HIV therapeutics, a significant number of compounds were identified as IN inhibitors, but only some of them showed antiviral activity.
Chenzhong, Liao, Christophe, Marchand, Terrence R, Burke, Yves, Pommier, Marc C, Nicklaus   +4 more
openaire   +3 more sources

CoMFA and CoMSIA Studies on Inhibitors of HIV-1 Integrase - Bicyclic Pyrimidinones [PDF]

E-Journal of Chemistry, 2010
To understand the structural requirements of HIV-1 integrase inhibitors and to design new ligands against human HIV-1 integrase with enhanced inhibitory potency, a 3D QSAR (quantitative structure-activity relationship) study with comparative molecular ...
V. Radhika, S. Sree Kanth, M. Vijjulatha
doaj   +2 more sources

HIV Integrase Inhibitors Block Replication of Alpha-, Beta-, and Gammaherpesviruses [PDF]

mBio, 2014
The catalytic site of the HIV integrase is contained within an RNase H-like fold, and numerous drugs have been developed that bind to this site and inhibit its activity.
Zhipeng Yan, Kevin F. Bryant, Sean M. Gregory, Magdalena Angelova, David H. Dreyfus, Xue Zhi Zhao, Donald M. Coen, Terrence R. Burke, David M. Knipe   +8 more
doaj   +2 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   +1 more source

Weight gain and integrase inhibitors [PDF]

Current Opinion in Infectious Diseases, 2020
Purpose of review Weight gain and obesity among people living with HIV (PLWH) is a serious problem that occurs often after initiation of antiretroviral therapy but may be worse with integrase strand transfer inhibitors (INSTIs).
Allison Ross, Eckard, Grace A, McComsey
openaire   +2 more sources