A possible improvement for structure-based drug design illustrated by the discovery of a Tat HIV-1 inhibitor
✍ Scribed by Mickaël Montembault; Giang Vo-Thanh; Abdallah Deyine; Valérie Fargeas; Monique Villiéras; Ané Adjou; Didier Dubreuil; Didier Esquieu; Catherine Grégoire; Sandrine Opi; Jean-Marie Péloponèse; Grant Campbell; Jennifer Watkins; Jean de Mareuil; Anne-Marie Aubertin; Christian Bailly; Erwann Loret; Jacques Lebreton
- Book ID
- 108073209
- Publisher
- Elsevier Science
- Year
- 2004
- Tongue
- English
- Weight
- 194 KB
- Volume
- 14
- Category
- Article
- ISSN
- 0960-894X
No coin nor oath required. For personal study only.
📜 SIMILAR VOLUMES
The cocrystal structures of LY289612 and LY297135 were used as a starting point in the design of nonpeptidic HIV-1 protease inhibitors. This report details the discovery of a series of novel aromatic P2 replacement groups. The 3-hydroxy-2-methyl benzoic acid group, discovered in AG1254, was incorpor
A combination of structure-activity studies, kinetic analysis, X-ray crystallographic analysis, and modeling were employed in the design of a novel series of HIV-1 protease (HIV PR) inhibitors. The crystal structure of a complex of HIV PR with SRSS-2,5-bis[N-(tert-butyloxycarbonyl)amino]-3,4-dihydro