Abstract
Histone deacetylases (HDACs), encompassing at least 18 members, are promising targets for anticancer drug discovery and development. To date, five histone deacetylase inhibitors (HDACis) have been approved for cancer treatment, and numerous others are undergoing clinical trials. It has been well validated that an agent that can simultaneously and effectively inhibit two or more targets may offer greater therapeutic benefits over single-acting agents in preventing resistance to treatment and in potentiating synergistic effects. A prime example of a bifunctional agent is the hybrid HDAC inhibitor. In this perspective, the authors review the majority of reported kinase/HDAC hybrid inhibitors.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Binding Sites
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Catalytic Domain
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Drug Design
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Erlotinib Hydrochloride / chemistry
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Erlotinib Hydrochloride / metabolism
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Erlotinib Hydrochloride / therapeutic use
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Histone Deacetylase Inhibitors / chemistry
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Histone Deacetylase Inhibitors / metabolism
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Histone Deacetylase Inhibitors / therapeutic use
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Histone Deacetylases / chemistry*
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Histone Deacetylases / metabolism
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Humans
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Neoplasms / drug therapy
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Protein Kinase Inhibitors / chemistry*
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Protein Kinase Inhibitors / metabolism
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Protein Kinase Inhibitors / therapeutic use
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Protein Kinases / chemistry*
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Protein Kinases / metabolism
Substances
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Histone Deacetylase Inhibitors
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Protein Kinase Inhibitors
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Erlotinib Hydrochloride
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Protein Kinases
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Histone Deacetylases