Results 181 to 190 of about 30,382,849 (226)

Targeting HIV-1 integrase

Expert Opinion on Therapeutic Targets, 2001
Human immunodeficiency virus Type 1 (HIV-1) integrase is an essential enzyme for the obligatory integration of the viral DNA into the infected cell chromosome. As no cellular homologue of HIV integrase has been identified, this unique HIV-1 enzyme is an attractive target for the development of new therapeutics.
Khampoune, Sayasith, Gilles, Sauvé, Jocelyn, Yelle   +2 more
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

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: 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

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

Thiazolothiazepine Inhibitors of HIV-1 Integrase

Journal of Medicinal Chemistry, 1999
A series of thiazolothiazepines were prepared and tested against purified human immunodeficiency virus type-1 integrase (HIV-1 IN) and viral replication. Structure-activity studies reveal that the compounds possessing the pentatomic moiety SC(O)CNC(O) with two carbonyl groups are in general more potent against purified IN than those containing only one
NEAMATI N., TURPIN J. A, WINSLOW H. E., CHRISTENSEN J. L., WILLIAMSON K., ORR A., RICE W. G., POMMIER Y., GAROFALO A., BRIZZI A., CAMPIANI G., FIORINI I., NACCI V.   +12 more
openaire   +4 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.
Isabelle, Malet, Vincent, Calvez, Anne-Geneviève, Marcelin   +2 more
openaire   +2 more sources

QSAR studies of HIV-1 integrase inhibition

Bioorganic & Medicinal Chemistry, 2002
Compounds from a wide variety of structural classes inhibit HIV-1 integrase. However, a single unified understanding of the relationship between the structures and activities of these compounds still eludes researchers. We report herein the development of QSAR models for integrase inhibition.
Hongbin, Yuan, Abby L, Parrill
openaire   +2 more sources

Metal-Dependent Inhibition of HIV-1 Integrase

Journal of Medicinal Chemistry, 2002
Human immunodeficiency virus type 1 integrase (HIV-1 IN) is an essential enzyme for effective viral replication. Therefore, IN inhibitors are being sought for chemotherapy against AIDS. We had previously identified a series of salicylhydrazides as potent inhibitors of IN in vitro (Neamati, N.; et al. J. Med. Chem. 1998, 41, 3202-3209.).
Nouri, Neamati, Zhaiwei, Lin, Rajeshri G, Karki, Ann, Orr, Kiriana, Cowansage, Dirk, Strumberg, Godwin C G, Pais, Johannes H, Voigt, Marc C, Nicklaus, Heather E, Winslow, He, Zhao, Jim A, Turpin, Jizu, Yi, Anna Marie, Skalka, Terrence R, Burke, Yves, Pommier   +15 more
openaire   +2 more sources

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 ...
H, Zhao, N, Neamati, S, Sunder, H, Hong, S, Wang, G W, Milne, Y, Pommier, T R, Burke   +7 more
openaire   +2 more sources