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.
Keywords: Hsp90, Grp94, Trap-1, Paralog-selective inhibitor, Structure-based design, Screening.
Current Topics in Medicinal Chemistry
Title:Paralog Specific Hsp90 Inhibitors – A Brief History and a Bright Future
Volume: 16 Issue: 25
Author(s): Daniel T. Gewirth
Affiliation:
Keywords: Hsp90, Grp94, Trap-1, Paralog-selective inhibitor, Structure-based design, Screening.
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.
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Cite this article as:
Gewirth T. Daniel, Paralog Specific Hsp90 Inhibitors – A Brief History and a Bright Future, Current Topics in Medicinal Chemistry 2016; 16 (25) . https://dx.doi.org/10.2174/1568026616666160413141154
DOI https://dx.doi.org/10.2174/1568026616666160413141154 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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