Progress in the discovery and development of heat shock protein 90 (Hsp90) inhibitors

Rohit Bhat; Sreedhar R Tummalapalli; David P Rotella

doi:10.1021/jm500823a

Progress in the discovery and development of heat shock protein 90 (Hsp90) inhibitors

J Med Chem. 2014 Nov 13;57(21):8718-28. doi: 10.1021/jm500823a. Epub 2014 Aug 29.

Authors

Rohit Bhat¹, Sreedhar R Tummalapalli, David P Rotella

Affiliation

¹ Department of Chemistry and Biochemistry, Sokol Institute for Pharmaceutical Life Sciences, Montclair State University , Montclair, New Jersey 07043, United States.

PMID: 25141341
DOI: 10.1021/jm500823a

Abstract

The discovery and clinical development of heat shock protein 90 (Hsp90) inhibitors continue to progress. A number of Hsp90 inhibitors are in clinical trials, and preclinical discoveries of new chemotypes that bind to distinct regions in the protein as well as isoform selective compounds are active areas of research. This review will highlight progress in the field since 2010.

Publication types

Review

MeSH terms

Animals
Antineoplastic Agents / pharmacology
Benzoquinones / pharmacology
Drug Design
HSP90 Heat-Shock Proteins / antagonists & inhibitors*
HSP90 Heat-Shock Proteins / metabolism
Humans
Lactams, Macrocyclic / pharmacology
Neoplasms / drug therapy
Neuroprotective Agents / pharmacology
Protein Isoforms / metabolism
Protein Isoforms / physiology
Rats
tau Proteins / metabolism

Substances

Antineoplastic Agents
Benzoquinones
HSP90 Heat-Shock Proteins
Lactams, Macrocyclic
Neuroprotective Agents
Protein Isoforms
tau Proteins
geldanamycin