Results 241 to 250 of about 71,892 (273)

Coumarin-Based Inhibitors of HIV Integrase

Journal of Medicinal Chemistry, 1997
The structures of a large number of HIV-1 integrase inhibitors have in common two aryl units separated by a central linker. Frequently at least one of these aryl moieties must contain 1,2-dihydroxy substituents in order to exhibit high inhibitory potency.
Terrence R. Burke, Huixiao Hong, Sanjay Sunder, George W. A. Milne, He Zhao, Abhijit Mazumder, Yves Pommier, Nouri Neamati, Shaomeng Wang   +8 more
openaire   +3 more sources

The Hunt for HIV-1 Integrase Inhibitors

AIDS Patient Care and STDs, 2006
Currently, there are three distinct mechanistic classes of antiretrovirals: inhibitors of the HIV- 1 reverse transcriptase and protease enzymes and inhibitors of HIV entry, including receptor and coreceptor binding and cell fusion. A new drug class that inhibits the HIV-1 integrase enzyme (IN) is in development and may soon be available in the clinic ...
Michael J. Kozal, Max Lataillade
openaire   +2 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.
Abhijit Mazumder, Nouri Neamati, Yves Pommier, Terrence R. Burke, He Zhao, Sanjay Sunder   +5 more
openaire   +3 more sources

Raltegravir: The first HIV integrase inhibitor

Clinical Therapeutics, 2008
The availability of new classes of antiretroviral drugs has made it possible for HIV-infected individuals who are highly treatment experienced to achieve the goals of immunologic recovery and virologic suppression. Raltegravir is the first integrase inhibitor to be approved by the US Food and Drug Administration for use in antiretroviral treatment ...
Betty J. Dong, Jennifer Cocohoba
openaire   +3 more sources

The future of integrase inhibitors of HIV-1

Current Opinion in Virology, 2012
Integration of the HIV-1 DNA is required and essential to maintain the viral DNA in the infected cell. Integration process occurs in several events, mainly endonucleolytic processing of the 3' ends of the viral DNA and strand transfer or joining of the viral and cellular DNA.
Anne-Geneviève Marcelin, Isabelle Malet, Vincent Calvez   +2 more
openaire   +3 more sources

HIV Integrase Inhibitors

2013
This chapter presents the discovery, development and evolution of integrase strand transfer inhibitors. A brief overview of the first‐generation inhibitors raltegravir and elvitegravir serves to describe their landmark advancement of the field and also outline areas for further improvement.
Takashi Kawasuji, Brian A. Johns, Emile Johann Velthuisen   +2 more
openaire   +2 more sources

HIV pharmacotherapy

Journal of the American Academy of Physician Assistants, 2016
Integrase strand transfer inhibitors (INSTIs) are a class of antiretroviral agents used to treat HIV. These drugs--raltegravir, elvitegravir, and dolutegravir--are preferred options for treatment-naïve patients when used in combination with two nucleoside reverse transcriptase inhibitors.
Nathan Trustman, April Yalong, Elaine Wong   +2 more
openaire   +3 more sources

Dolutegravir, an HIV integrase inhibitor for the treatment of HIV infection

Drugs of Today, 2014
Dolutegravir, a next-generation integrase strand transfer inhibitor, was recently approved by the United States Food and Drug Administration to treat antiretroviral therapy-naive as well as treatment-experienced HIV-infected individuals, including those who have been treated with other integrase strand transfer inhibitors.
Zelalem Temesgen, Stacey A. Rizza, Rohit Talwani   +2 more
openaire   +3 more sources

A new mechanism of resistance of HIV-2 to integrase inhibitors: a 5 amino-acids insertion in the integrase C-terminal domain.

Clinical Infectious Diseases, 2018
Background Integrase strand-transfer inhibitors (INSTI) are crucial for treatment of HIV-2 infection, due to limited available therapeutic options. Recently, bictegravir has been approved for HIV-1-infected patients but no data are currently available ...
Q. Le Hingrat, G. Collin, M. Lê, G. Peytavin, B. Visseaux, M. Bertine, R. Tubiana, M. Karmochkine, N. Valin, F. Collin, A. Lemaignen, L. Bernard, F. Damond, S. Matheron, D. Descamps, C. Charpentier   +15 more
semanticscholar   +1 more source

Hydrazide-Containing Inhibitors of HIV-1 Integrase

Journal of Medicinal Chemistry, 1997
Inhibitors of HIV integrase are currently being sought as potential new therapeutics for the treatment of AIDS. A large number of inhibitors discovered to date contain the o-bis-hydroxy catechol structure. In an effort to discover structural leads for the development of new HIV integrase inhibitors which do not rely on this potentially cytotoxic ...
George W. A. Milne, Terrence R. Burke, Huixiao Hong, Shaomeng Wang, Yves Pommier, Sanjay Sunder, He Zhao, Nouri Neamati   +7 more
openaire   +3 more sources