Abstract
The molecular chaperone heat shock protein 90 (HSP90) is essential for the folding stability, intracellular disposition and proteolytic turnover of many of the key regulators of cell growth, differentiation and survival. These essential functions are used by the cells during the oncogenesis process to allow the tumor transformation and facilitate the rapid somatic evolution. Inhibition of HSP90 would provide combinatorial blockade of a range of oncogenic pathways, antagonizing many of the hallmark traits of cancer. Several HSP90 inhibitors are currently under clinical trial investigation for the treatment of cancer. This review summarizes the current state and progress achieved in the development of HSP90 inhibitors targeting the N-terminal ATP pocket, C-terminal domain, different compartmentalized isoforms, and protein (cochaperones and/or client proteins)/HSP90 interactions. In the context of drug discovery, the most relevant patents which appeared recently in the literature are discussed as well.
Keywords: Anticancer therapeutics, development of antitumor agents, drug discovery, heat shock proteins (HSPs), HSP90 inhibitors, HSP90 modulators, heat shock response, molecular chaperones
Recent Patents on Anti-Cancer Drug Discovery
Title:Heat Shock Protein 90 Inhibitors as Therapeutic Agents
Volume: 7 Issue: 3
Author(s): Isabel Gomez-Monterrey, Marina Sala, Simona Musella and Pietro Campiglia
Affiliation:
Keywords: Anticancer therapeutics, development of antitumor agents, drug discovery, heat shock proteins (HSPs), HSP90 inhibitors, HSP90 modulators, heat shock response, molecular chaperones
Abstract: The molecular chaperone heat shock protein 90 (HSP90) is essential for the folding stability, intracellular disposition and proteolytic turnover of many of the key regulators of cell growth, differentiation and survival. These essential functions are used by the cells during the oncogenesis process to allow the tumor transformation and facilitate the rapid somatic evolution. Inhibition of HSP90 would provide combinatorial blockade of a range of oncogenic pathways, antagonizing many of the hallmark traits of cancer. Several HSP90 inhibitors are currently under clinical trial investigation for the treatment of cancer. This review summarizes the current state and progress achieved in the development of HSP90 inhibitors targeting the N-terminal ATP pocket, C-terminal domain, different compartmentalized isoforms, and protein (cochaperones and/or client proteins)/HSP90 interactions. In the context of drug discovery, the most relevant patents which appeared recently in the literature are discussed as well.
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Gomez-Monterrey Isabel, Sala Marina, Musella Simona and Campiglia Pietro, Heat Shock Protein 90 Inhibitors as Therapeutic Agents, Recent Patents on Anti-Cancer Drug Discovery 2012; 7 (3) . https://dx.doi.org/10.2174/157489212801820066
DOI https://dx.doi.org/10.2174/157489212801820066 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
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