title: Discovery and development of purine-scaffold Hsp90 inhibitors.
abstract: The heat-shock protein 90 (Hsp90), an important target in cancer and other diseases, has become recently the focus of several drug discovery and development efforts. The initially identified natural-product inhibitors of Hsp90, such as geldanamycin, played a major role in elucidating its biological function and in determining its clinical relevance. Upcoming synthetic inhibitors, such as the purine-scaffold class, furthered our understanding on Hsp90 in cancer and neurodegenerative diseases and delivered what are promised to be clinical candidates with favorable pharmacologic profiles. This review intends to inform the reader on efforts ranging from the discovery of purine-scaffold Hsp90 inhibitors to their clinical translation as well as on their use as chemical tools to dissect the roles of Hsp90 in pathogenic systems.
authors.affiliation: Memorial Sloan-Kettering Cancer Center, Department of Medicine and Program in Molecular Pharmacology and Chemistry, 1275 York Avenue, Box 482, New York, NY10021, USA +1 646 888 2235 ; +1 646 422 0416 ; chiosisg@mskcc.org.
authors.forename: Gabriela
authors.initials: G
authors.lastname: Chiosis
authors.forename: Yanlong
authors.initials: Y
authors.lastname: Kang
authors.forename: Weilin
authors.initials: W
authors.lastname: Sun