Heat shock protein (HSP) drug discovery and development: Targeting heat shock proteins in disease Journal Article


Authors: Shrestha, L.; Bolaender, A.; Patel, H. J.; Taldone, T.
Article Title: Heat shock protein (HSP) drug discovery and development: Targeting heat shock proteins in disease
Abstract: Heat shock proteins (HSPs) present as a double edged sword. While they play an important role in maintaining protein homeostasis in a normal cell, cancer cells have evolved to co-opt HSP function to promote their own survival. As a result, HSPs such as HSP90 have attracted a great deal of interest as a potential anticancer target. These efforts have resulted in over 20 distinct compounds entering clinical evaluation for the treatment of cancer. However, despite the potent anticancer activity demonstrated in preclinical models, to date no HSP90 inhibitor has obtained regulatory approval. In this review we discuss the unique challenges faced in targeting HSPs that have likely contributed to their lack of progress in the clinic and suggest ways to overcome these so that the enormous potential of these compounds to benefit patients can finally be realized. We also provide a guideline for the future development of HSP-targeted agents based on the many lessons learned during the last two decades in developing HSP90 inhibitors. © 2016 Bentham Science Publishers.
Keywords: inhibitor; n-terminal; hsp90; chaperone; cancer
Journal Title: Current Topics in Medicinal Chemistry
Volume: 16
Issue: 25
ISSN: 1568-0266
Publisher: Bentham Science Publishers  
Date Published: 2016-01-01
Start Page: 2753
End Page: 2764
Language: English
PROVIDER: scopus
PMCID: PMC4995156
PUBMED: 27072696
DOI: 10.2174/1568026616666160413141911
DOI/URL:
Notes: Review -- Export Date: 3 October 2016 -- Source: Scopus
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MSK Authors
  1. Hardik Jitendra Patel
    24 Patel
  2. Tony Taldone
    74 Taldone