Paralog Specific Hsp90 Inhibitors - A Brief History and a Bright Future.
Paralog Specific Hsp90 Inhibitors - A Brief History and a Bright Future.
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DOI:
10.2174/1568026616666160413141154
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发表时间:
2016
影响因子:
3.4
通讯作者:
Gewirth DT
中科院分区:
文献类型:
--
作者:
Gewirth DT
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. 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. First generation compounds that selectively bind to Hsp90, Grp94, or Trap-1 have been identified. With the proof of principle firmly established, the prospects for further progress are bright.