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Curr Top Med Chem. 2016;16(25):2779-91.

Paralog Specific Hsp90 Inhibitors - A Brief History and a Bright Future.

Author information

1
Hauptman-Woodward Medical Research Institute, 700 Ellicott Street, Buffalo, NY, 14203, USA. gewirth@hwi.buffalo.edu.

Abstract

BACKGROUND:

The high sequence and structural homology among the hsp90 paralogs - Hsp90α, Hsp90β, Grp94, and Trap-1 - has made the development of paralog-specific inhibitors a challenging proposition.

OBJECTIVE:

This review surveys the state of developments in structural analysis, compound screening, and structure-based design that have been brought to bear on this problem.

RESULTS:

First generation compounds that selectively bind to Hsp90, Grp94, or Trap-1 have been identified.

CONCLUSION:

With the proof of principle firmly established, the prospects for further progress are bright.

PMID:
27072700
PMCID:
PMC4995118
[Indexed for MEDLINE]
Free PMC Article

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