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Current Topics in Medicinal Chemistry

Volume 9 Issue 15
ISSN: 1568-0266
eISSN: 1873-5294

 

   All Titles

  Purine-Scaffold Hsp90 Inhibitors
  pp.1436-1446 (11) Authors: Tony Taldone, Gabriela Chiosis
 
 
      Abstract

Hsp90 is a molecular chaperone with important roles in regulating the function of several proteins with potential pathogenic activity. Because many of these proteins are involved in cancer and neurodegenerative promoting pathways, Hsp90 has emerged as an attractive therapeutic target in these diseases. Molecules that bind to the N-terminal nucleotide pocket of Hsp90 inhibit its activity, and consequently, disrupt client protein function. A number of these inhibitors from several chemical classes are now known, and some are already in clinical trials. This review focuses on the purine class of Hsp90 inhibitors, their discovery through rational design, and on efforts aimed towards their optimization and development into clinically viable drugs for the treatment of cancer. Their potential towards neurodegenerative diseases will also be touched upon.

 
  Keywords: Heat shock protein 90, purine, cancer, neurodegeneration
  Affiliation: Program in Molecular Pharmacology and Chemistry and Department of Medicine, Memorial Sloan-Kettering Cancer Center, 1275 York Avenue, Box 482, New York, NY 10021, USA.
 
  Key: New Content Free Content Open Access Plus Subscribed Content

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