Results 11 to 20 of about 28,079 (244)

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

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 ...
Bar-Magen, Tamara, Donahue, Daniel A, Faltenbacher, Verena H, Kuhl, Björn D, Oliveira, Maureen, Sloan, Richard D, Wainberg, Mark A, Xu, Hongtao   +7 more
core   +5 more sources

HIV Dynamics and Integrase Inhibitors [PDF]

Antiviral Chemistry and Chemotherapy, 2009
The integrase inhibitor (INI) raltegravir has shown promising results in clinical trials to date, reducing second phase HIV RNA levels by 70% in comparison with standard regimens. These trial results have been limited by the 50 copies/ml detection limit of the HIV RNA assay and have not investigated the effect of an INI regimen on levels of latently ...
John M. Murray
openaire   +4 more sources

Novel therapeutic strategies targeting HIV integrase [PDF]

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 ...
A Brigo, A Zamborlini, AA Mathias, AM Meehan, Annonymous, AP Toropova, AR Zolopa, B Grinsztejn, B Taiwo, B Van Maele, BC Johnson, BG Brenner, C Fenwick, C Garrido, C Garrido, C Liao, C Marchand, C Maurin, D Hazuda, DA Cooper, DA Donahue, DJ Hazuda, DJ McColl, E DeJesus, E Muraglia, E Vispo, EZ Loizidou, F Canducci, F Canducci, F Christ, F Dyda, GN Maertens, I Malet, I Malet, I Malet, IB Dicker, J Eron, J Rockstroh, J Tang, JJ Eron, JJ Eron, JJ Kessl, JL Blanco, JM Coffin, JS Wai, JY Nagasawa, K Shimura, KE Hightower, KK Pandey, L De Luca, L De Luca, L De Luca, L Krishnan, L Van Wesenbeeck, LH Hall, LQ Al-Mawsawi, M Kobayashi, M Lanzafame, M Markowitz, M McNeely, M Métifiot, M Métifiot, M Sato, M Terreni, M Underwood, Mark A Wainberg, ME Seegulam, MJ Buzon, MJ Rosemond, MS Egbertson, N Jing, N Sluis-Cremer, O Delelis, O Goethals, O Goethals, OM Klibanov, P Cherepanov, P Madlala, P Pace, Peter K Quashie, PK Quashie, Q Liu, R Di Santo, R Reinke, RD Sloan, RD Sloan, Richard D Sloan, RT Steigbigel, S Aslanyan, S Hare, S Hare, S Hare, S Hare, S Min, S Min, S Ramanathan, SB Singh, SP Gupta, T Bar-Magen, T Bar-Magen, T Bar-Magen, TM Jenkins, TM Jenkins, TW Johnson, VA Johnson, VN Telvekar, VR de Soultrait, X Li, Y Goldgur, Y Yoshinaga, Z Hu, Z Wang   +111 more
core   +5 more sources

HIV/HCV-coinfection: which role can new antiretrovirals such as integrase inhibitors play? [PDF]

European Journal of Medical Research, 2009
End-stage liver disease has become one of the most frequent causes of death in HIV/HCV-coinfected patients. The role of new antiretrovirals in the progression of liver fibrosis has yet to be defined.
Vogel Martin, Nelson Mark
doaj   +2 more sources

Dimerization inhibitors of HIV-1 reverse transcriptase, protease and integrase: A single mode of inhibition for the three HIV enzymes? [PDF]

, 2006
The genome of human immunodeficiency virus type 1 (HIV-1) encodes 15 distinct proteins, three of which provide essential enzymatic functions: a reverse transcriptase (RT), an integrase (IN), and a protease (PR).
Camarasa Rius, María José, Gago Badenas, Federico, Pérez Pérez, María Jesús, San Félix García, Ana, Velázquez Díaz, Sonsoles   +4 more
core   +4 more sources

Investigation of furo[2,3-h]- and pyridazino[3,4-f]cinnolin-3-ol scaffolds as substrates for the development of novel HIV-1 integrase inhibitors [PDF]

, 2011
With the aim to develop novel HIV-1 integrase inhibitors, we obtained a set of condensed ring systems based on the furo[2,3-h]cinnolin-3(2H)-one and pyridazino[3,4-f]cinnolin-3-ol scaffolds bearing a potential chelating pharmacophore, which can be ...
Casule, Paola, Derudas, Marco, El-Tamany, El-Sayed H, Gomaa, Mohamed F Y, Hasanen, Jehan Abd-Elrazik, Mariani, Alberto, Pala, Nicolino, Sechi, Mario   +7 more
core   +3 more sources

Viral Dynamic Model of Antiretroviral Therapy Including the Integrase Inhibitor Raltegravir in Patients with HIV-1

Biomath, 2012
Antiviral combination therapies consisting of reverse transcriptase inhibitors, protease inhibitors and an integrase inhibitor, have been developed to suppress HIV below the limit of detection.
Dimitra Bon, Christoph Stephan, Oliver Keppler, Eva Herrmann   +3 more
doaj   +3 more sources

Raltegravir: first in class HIV integrase inhibitor

Therapeutics and Clinical Risk Management, 2008
On October 16, 2007, the US Food and Drug Administration (FDA) approved raltegravir for treatment of human immunodeficiency virus (HIV)-1 infection in combination with other antiretroviral agents in treatment-experienced adult patients who have evidence of viral replication and HIV-1 strains resistant to multiple antiretroviral agents.
Zelalem Temesgen, Dawd S. Siraj
openaire   +6 more sources

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

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