Abstract
In the last decade, the molecular chaperone HSP90 has emerged as an important target in cancer therapeutics and has subsequently become the focus of several drug discovery and development efforts. The first-in-class HSP90 inhibitor 17-AAG entered into Phase I clinical trial in 1999. Today 13 HSP90 inhibitors representing multiple drug classes, with different modes of action, are undergoing clinical evaluation. The present review will highlight the involvement of HSP90 in regulating and maintaining the transformed phenotype, provide an overview on current HSP90 inhibitors and further update on the most relevant patents which have recently appeared in the literature.
MeSH terms
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Adenine / analogs & derivatives
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Adenine / chemistry
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Adenine / metabolism
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Adenine / therapeutic use
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Animals
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / metabolism
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Antineoplastic Agents / therapeutic use
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Benzodioxoles / chemistry
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Benzodioxoles / metabolism
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Benzodioxoles / therapeutic use
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Cell Membrane / drug effects
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Cell Membrane / metabolism
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Clinical Trials as Topic / trends
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Drug Discovery / trends*
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HSP90 Heat-Shock Proteins / antagonists & inhibitors*
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HSP90 Heat-Shock Proteins / metabolism
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Humans
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Neoplasms / drug therapy*
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Neoplasms / metabolism
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Patents as Topic*
Substances
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1-(4-(2-(6-amino-8-((6-bromo-1,3-benzodioxol-5-yl)sulfanyl)-9H-purin-9-yl)ethyl)piperidin-1-yl)-2-hydroxypropan-1-one
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Antineoplastic Agents
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Benzodioxoles
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HSP90 Heat-Shock Proteins
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Adenine