Author/Authors :
Sheo B Singh، نويسنده , , Deborah L. Zink، نويسنده , , Anne W. Dombrowski، نويسنده , , Jon D. Polishook، نويسنده , , John G. Ondeyka، نويسنده , , Jorden Hirshfield، نويسنده , , Peter Felock، نويسنده , , Daria J. Hazuda، نويسنده ,
Abstract :
HIV-1 integrase is a critical enzyme in the replication of HIV-1. It is absent in the host cells and therefore is a good target for treatment of HIV-1 infections. Integracides are members of the tetracyclic triterpenoids family that were isolated from the fermentation broth of a Fusarium sp. Integracide A, a sulfated ester, exhibited significant inhibitory activity against strand transfer reaction of HIV-1 integrase. The discovery, structure elucidation including single crystal X-ray structure and HIV-1 inhibitory activity of these compounds are described.
