A potent and orally active HIV-1 integrase inhibitor

…, MM Zrada, AR Cortes, A Wallace, Y Leonard…

Index: Egbertson, Melissa S.; Moritz, H. Marie; Melamed, Jeffrey Y.; Han, Wei; Perlow, Debra S.; Kuo, Michelle S.; Embrey, Mark; Vacca, Joseph P.; Zrada, Matthew M.; Cortes, Amanda R.; Wallace, Audrey; Leonard, Yvonne; Hazuda, Daria J.; Miller, Michael D.; Felock, Peter J.; Stillmock, Kara A.; Witmer, Marc V.; Schleif, William; Gabryelski, Lori J.; Moyer, Gregory; Ellis, Joan D.; Jin, Lixia; Xu, Wei; Braun, Matthew P.; Kassahun, Kellem; Tsou, Nancy N.; Young, Steven D. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 5 p. 1392 - 1398

Full Text: HTML

Citation Number: 28

Abstract

Replication of the human immunodeficiency virus (HIV) is dependent upon the enzyme HIV Integrase (IN), one of three essential enzymes encoded in the viral genome. HIV IN catalyzes the insertion of the viral genome into the host genome. HIV IN subunits assemble onto double stranded viral DNA and process the 3′ ends to prepare the strand for integration. The pre-integration complex then enters the nucleus where it catalyzes the DNA insertion (strand transfer) step. ...