Paralog Specific Hsp90 Inhibitors – A Brief History and a Bright Future

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.

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