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

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.

journal_name

Curr Top Med Chem

authors

Gewirth DT

doi

10.2174/1568026616666160413141154

subject

Has Abstract

pub_date

2016-01-01 00:00:00

pages

2779-91

issue

25

eissn

1568-0266

issn

1873-4294

pii

CTMC-EPUB-74964

journal_volume

16

pub_type

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