Jump to main content
Jump to site search

All chapters
Previous chapter Next chapter

CHAPTER 10

Inhibitors of the Hsp90 C-terminus

Hsp90 is a promising therapeutic target for the treatment of cancer and neurodegenerative diseases. While current research focuses on drugging the N-terminal ATP-binding pocket, small molecules that disrupt the Hsp90 C-terminus manifest distinctive properties and may provide additional advantages over N-terminal inhibitors. Structural modifications to novobiocin, the first Hsp90 C-terminal inhibitor identified, have led to a set of analogues that either induce a strong heat shock response or manifest potent anti-proliferative activities. The development of these novobiocin-based analogues and their biological evaluation is summarized in this chapter. Additional small molecules that bind the Hsp90 C-terminus are also discussed.

Publication details


Print publication date
30 Oct 2013
Copyright year
2013
Print ISBN
978-1-84973-666-4
PDF eISBN
978-1-84973-968-9
From the book series:
Drug Discovery