Work

Mechanistic Studies of Sansalvamide A-Amide: An Allosteric Modulator of Hsp90

Year: 2010

Type: article

Abstract: Herein we show that San A-amide, a structurally unique molecule, influences a subset of cancer-related pathways involving Hsp90. We show that San A-amide specifically binds to the N-middle domain of Hsp90 allosterically disrupts the binding of proteins thought to interact with the Hsp90 C-terminal domain, while having no effect on an N-terminal domain client protein. This unique mechanism suggests that San A-amide is a potential tool for studying C-terminal binding proteins of Hsp90 as well as a promising lead in the development of new cancer therapeutics.

Source: ACS Medicinal Chemistry Letters

DOI: 10.1021/ml900003t

Authors: Robert C. Vasko, Rodrigo A. Rodriguez, Christian N. Cunningham, Veronica C. Ardi, David A. Agard, Shelli R. McAlpine

Institutions: Howard Hughes Medical Institute, University of California, San Francisco, San Diego State University

Language: English

Topic: Heat shock proteins research

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

Funders: National Cancer Institute, National Institute of General Medical Sciences, Fogarty International Center