Equisetin and a novel opposite stereochemical homolog phomasetin, two fungal metabolites as inhibitors of HIV-1 integrase

✍ Scribed by Sheo B. Singh; Deborah L. Zink; Michael A. Goetz; Anne W. Dombrowski; Jon D. Polishook; Daria J. Hazuda

• Publisher: Elsevier Science
• Year: 1998
• Tongue: French
• Weight: 383 KB
• Volume: 39
• Category: Article
• ISSN: 0040-4039
• DOI: 10.1016/s0040-4039(98)00269-x

✦ Synopsis

Integration is an essential step in HIV replication and is catalyzed by an enzyme caged integmse. We have isolated equisetin (la), and a novel opposite stere&tetnical homolog, phomasetin (2a), from Fusariun~ he~emsporum and a Phomu sp. respectively. They inhibit the invitro recombinant integrase enzyme with ICm values of 7-20 pM. Unlike known inhibitors, these compounds also inhibit the integration reactions catalyzed by preintegmtion complexes isolated from HIV-l infected cells.