Results 191 to 200 of about 26,857 (227)

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.
Z, Temesgen, R, Talwani, S A, Rizza
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.
H, Zhao, N, Neamati, A, Mazumder, S, Sunder, Y, Pommier, T R, Burke   +5 more
openaire   +2 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 ...
Jennifer, Cocohoba, Betty J, Dong
openaire   +2 more sources

Hiv integrase: a target for aids therapeutics

Trends in Biotechnology, 1997
HIV integrase catalyses the incorporation of virally derived DNA into the human genome. This unique step in the virus life cycle provides a variety of points for intervention and hence is an attractive target for the development of new therapeutics for the treatment of AIDS.
Thomas, Mark, Brady, Leo
openaire   +3 more sources

Raltegravir: an integrase inhibitor for HIV-1

Expert Opinion on Investigational Drugs, 2008
The need to develop antiretroviral agents with novel mechanisms of action persists for the treatment of both antiretroviral- experienced and antiretroviral-naive patients with HIV/AIDS. This is mandated, in part, by the perpetual advent of antiretroviral-resistant HIV-1 strains.
Teresa H, Evering, Martin, Markowitz
openaire   +2 more sources

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.
H, Zhao, N, Neamati, H, Hong, A, Mazumder, S, Wang, S, Sunder, G W, Milne, Y, Pommier, T R, Burke   +8 more
openaire   +2 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 ...
Max, Lataillade, Michael J, Kozal
openaire   +2 more sources

HIV integrase: a target for drug discovery

Genes and Function, 1997
Current antiviral strategies against HIV rely on structure–function analysis of HIV reverse transcriptase (RT) and protease (PR). The third viral pol gene product, HIV integrase (IN), is also a good target for drug discovery, since IN is essential for retroviral replication and, moreover, it has no obvious functional analogue in the host.
R A, Lutzke, R H, Plasterk
openaire   +2 more sources

Structure and Function of HIV-1 Integrase

Current Topics in Medicinal Chemistry, 2004
HIV-1 integrase is a multidomain enzyme which is required for the integration of viral DNA into the host genome. It is one of three enzymes of HIV, the others being the Reverse Transcriptase and the Protease. It is an attractive target for therapeutic drug design. The enzyme consists of three domains.
Thang K, Chiu, David R, Davies
openaire   +2 more sources

HIV integrase as a target for antiviral chemotherapy

Reviews in Medical Virology, 2002
AbstractOne of the three key enzymes encoded by the pol gene of HIV is a Mr 32 000 protein called HIV integrase. This viral enzyme is involved in the integration of HIV DNA into host chromosomal DNA. There appears to be no functional equivalent of the enzyme in human cells.
openaire   +2 more sources