Journal
CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 16, Issue 25, Pages 2779-2791Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026616666160413141154
Keywords
Hsp90; Grp94; Trap-1; Paralog-selective inhibitor; Structure-based design; Screening
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Funding
- NIH [R01CA095130, P01CA186866]
- Richard W. and Mae Stone Goode Foundation
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Background. The high sequence and structural homology among the hsp90 paralogs - Hsp90 alpha, Hsp90 beta, 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.
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