Results 1 to 10 of about 30,099 (284)

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   +4 more sources

Arylamide Inhibitors of HIV-1 Integrase

Journal of Medicinal Chemistry, 1997
Based on data derived from a large number of HIV-1 integrase inhibitors, similar structural features can be observed, which consist of two aryl units separated by a central linker. For many inhibitors fitting this pattern, at least one aryl ring also requires ortho bis-hydroxylation for significant inhibitory potency.
H, Zhao, N, Neamati, A, Mazumder, S, Sunder, Y, Pommier, T R, Burke   +5 more
openaire   +3 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   +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   +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

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   +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

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

, 2013
Background: Optimal 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.
A Talbot, AJ Viera, Annemarie M. J. Wensing, AR Zolopa, Axel Fun, B Grinsztejn, B Taiwo, B Young, C Cohen, C Garrido, D McMahon, D Moher, DK Owens, DV Cordery, E DeJesus, E Martinez, E Vispo, EM Gardner, F Caby, F Canducci, F Smith, H Byakwaga, H Hatano, J Reynes, J van Lunzen, JJ Eron, JJ Eron Jr, JK Rockstroh, JL Lennox, JL Lennox, JM Gatell, JM Molina, JR Santos, L Van Wesenbeeck, L Wittkop, Linos Vandekerckhove, Luis Menéndez-Arias, M Harris, M Markowitz, M Markowitz, MA Thompson, MJ Buzon, MJ Kozal, Monique Nijhuis, N Mantel, Nele Brusselaers, O Goethals, PE Sax, Peter Messiaen, R Qaqish, R Relevo, RT Gandhi, RT Gandhi, RT Steigbigel, RT Steigbigel, S Gallien, S Nozza, V Dahl, W Towner, Y Yazdanpanah   +59 more
core   +8 more sources