Title:Targeting Hsp90-Cdc37: A Promising Therapeutic Strategy by Inhibiting Hsp90 Chaperone Function
Volume: 18
Issue: 13
关键词:
Hsp90 / Cdc37,蛋白质 - 蛋白质相互作用,PPI抑制剂,靶向策略,蛋白激酶。
摘要: Background & Objective: The Hsp90 chaperone protein regulates the folding, maturation
and stability of a wide variety of oncoproteins. In recent years, many Hsp90 inhibitors have entered
into the clinical trials while all of them target ATPase showing similar binding capacity and kinds of
side-effects so that none have reached to the market. During the regulation progress, numerous protein-
protein interactions (PPI) such as Hsp90 and client proteins or cochaperones are involved. With
the Hsp90-cochaperones PPI networks being more and more clear, many cancerous proteins have
been reported to be tightly correlated to Hsp90-cochaperones PPI. Among them, Hsp90-Cdc37 PPI
has been widely reported to associate with numerous protein kinases, making it a novel target for the
treatment of cancers.
Results and Conclusion: In this paper, we briefly review the strategies and modulators targeting
Hsp90-Cdc37 complex including direct and indirect regulation mechanism. Through these discussions
we expect to present inspirations for new insights into an alternative way to inhibit Hsp90 chaperone
function.