Results 241 to 250 of about 45,597 (259)

Tolerability of HIV integrase inhibitors

Current Opinion in HIV and AIDS, 2012
This review discusses the available safety data for three integrase strand transfer inhibitors (INSTIs)--raltegravir, elvitegravir and dolutegravir--derived from studies in both HIV-infected and HIV-uninfected cohorts.Phase 2 and 3 clinical trials show that all three INSTIs are well tolerated in treatment-naive and treatment-experienced patients with ...
Frederick J, Lee, Andrew, Carr
openaire   +2 more sources

HIV Integrase Structure and Function

1999
HIV integrase consists of three domains, the structures of which have been individually determined by X-ray crystallography or NMR spectroscopy. The core domain, spanning residues 50-212, is responsible for the catalytic activity of the enzyme.
D, Esposito, R, Craigie
openaire   +2 more sources

Integrase inhibitors to treat HIV/Aids

Nature Reviews Drug Discovery, 2005
HIV integrase is a rational target for treating HIV infection and preventing AIDS. It took approximately 12 years to develop clinically usable inhibitors of integrase, and Phase I clinical trials of integrase inhibitors have just begun. This review focuses on the molecular basis and rationale for developing integrase inhibitors.
Yves, Pommier, Allison A, Johnson, Christophe, Marchand   +2 more
openaire   +2 more sources

Quinoline-based HIV Integrase Inhibitors

Current Pharmaceutical Design, 2013
HIV integrase became an important target for drug development more than twenty years ago. However, progress has been hampered by the lack of assays suitable for high throughput screening, a reliable crystal structure or pharmacophore. Thus, a real breakthrough was only observed in 2007 with the introduction of the first integrase inhibitor, raltegravir,
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

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

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 INHIBITORS

2022
HIV infection is incredibly detrimental and fatal to people. Unfortunately, despite recent advancements and medications, it has not yet been completely eradicated. Opportunistic infections are added to the list of disorders in AIDS (Acquired Immune Deficiency Syndrome), an infectious disease that develops as a result of an impaired immune system.
openaire   +1 more source

HIV integrase inhibitory activity ofAgastache rugosa

Archives of Pharmacal Research, 1999
We have been screening anti-HIV integrase compounds from Korean medicinal plants by using an in vitro assay system which is mainly composed of recombinant human immunodeficiency virus type 1 integrase and radiolabeled oligonucleotides. From the above screening, the aqueous methanolic extract of the roots of Agastache rugosa exhibited a significant ...
H K, Kim, H K, Lee, C G, Shin, H, Huh
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