Results 251 to 260 of about 30,099 (284)

HIV Integrase Inhibitor Pharmacogenetics: An Exploratory Study

Clinical Drug Investigation, 2019
Integrase strand transfer inhibitors (INSTIs), dolutegravir, elvitegravir, and raltegravir, have become integral in the treatment of HIV, with close monitoring of continued efficacy and tolerability. As side effect occurrence varies among subjects receiving these drugs, we sought to perform an exploratory analysis examining the role of several single ...
Derek E. Murrell, David B. Cluck, Jonathan P. Moorman, Stacy D. Brown, Ke-Sheng Wang, Michelle M. Duffourc, Sam Harirforoosh   +6 more
openaire   +3 more sources

Caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors

Bioorganic & Medicinal Chemistry, 2003
HIV-1 integrase (IN) is an essential enzyme for retroviral replication and a rational target for the design of anti-AIDS drugs. In the present study, we have designed, synthesized and tested a series of caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors.
Yu-Wen, Xu, Gui-Sen, Zhao, Cha-Gyun, Shin, Heng-Chang, Zang, Chong-Kyo, Lee, Yong Sup, Lee   +5 more
openaire   +2 more sources

HIV‐1 integrase inhibitors: 2005–2006 update

Medicinal Research Reviews, 2007
AbstractHIV‐1 integrase (IN) catalyzes the integration of proviral DNA into the host genome, an essential step for viral replication. Inhibition of IN catalytic activity provides an attractive strategy for antiretroviral drug design. Currently two IN inhibitors, MK‐0518 and GS‐9137, are in advanced stages of human clinical trials.
Raveendra, Dayam, Rambabu, Gundla, Laith Q, Al-Mawsawi, Nouri, Neamati   +3 more
openaire   +2 more sources

Styrylquinazoline Derivatives as HIV-1 Integrase Inhibitors

Archiv der Pharmazie, 2002
Styrylquinazoline derivatives were prepared by Perkin condensation and evaluated for inhibitory activity against HIV-1 integrase. Among them, compound 5c containing a free catechol ring was the most potent (IC(50)=0.8 +/- 1.9 microM)and showed 6-fold more potency than the corresponding styrylquinoline compound (IC(50) = 130.7 +/- 8.6 microM).
Jae Yeol, Lee, Jang Hyun, Park, Sook Ja, Lee, Hokoon, Park, Yong Sup, Lee   +4 more
openaire   +2 more sources

HIV‐1 Integrase Inhibitors: Update and Perspectives

2008
Publisher Summary The chapter focuses on the recent advances in understanding the cellular mechanisms of human immunodeficiency virus (HIV) integration and the sites of actions of inhibitors. The chapter presents list of the known mutations that have been characterized for HIV‐1 integrase (IN) with their impact on IN activity, viral replication, and ...
Elena A, Semenova, Christophe, Marchand, Yves, Pommier   +2 more
openaire   +2 more sources

Patented HIV-1 Integrase Inhibitors (1998-2005)

Recent Patents on Anti-Infective Drug Discovery, 2006
Combination therapy, comprising at least three anti-human immunodeficiency virus (anti-HIV) drugs, has become the standard treatment of AIDS. Since 1996, highly active antiretroviral therapy (HAART) was designed to rapidly control HIV replication. It has had a significant impact on patient health and progression of AIDS in developed countries but its ...
openaire   +2 more sources

HIV Integrase Inhibitors

2014
Rajni Garg, Gene M. Ko
openaire   +2 more sources

Structure and function of retroviral integrase

Nature Reviews Microbiology, 2021
Goedele N Maertens, Alan N Engelman, Peter P Cherepanov   +2 more
exaly  

HIV Integrase Inhibitors and Entry Inhibitors

2021
Daniel Bradshaw, Ranjababu Kulasegaram
openaire   +1 more source

HIV-1 integrase inhibitor

Drug Discovery Today, 1996
openaire   +1 more source