Mechanistic Studies of Sansalvamide A-Amide: An Allosteric Modulator of Hsp90
ACS Medicinal Chemistry Letters2010Vol. 1(1), pp. 4–8
Citations Over TimeTop 10% of 2010 papers
Robert C. Vasko, Rodrigo A. Rodriguez, Christian N. Cunningham, Veronica C. Ardi, David A. Agard, Shelli R. McAlpine
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.
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