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
Current Topics in Medicinal Chemistry
Title: Purine-Scaffold Hsp90 Inhibitors
Volume: 9 Issue: 15
Author(s): Tony Taldone and Gabriela Chiosis
Affiliation:
Keywords: Heat shock protein 90, purine, cancer, neurodegeneration
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.
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Cite this article as:
Taldone Tony and Chiosis Gabriela, Purine-Scaffold Hsp90 Inhibitors, Current Topics in Medicinal Chemistry 2009; 9 (15) . https://dx.doi.org/10.2174/156802609789895737
DOI https://dx.doi.org/10.2174/156802609789895737 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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