Abstract
Amplification, overexpression, and elevated activation of Akt have been detected in many human malignancies making it an important target for cancer therapy. The Akt substrate-binding site offers a large number of potential interactions to an appropriately designed small molecule and can form the basis for the development of selective inhibitors. Here, we report the progression of GSK3beta substrate-mimetic inhibitors towards the development of a potent, small molecule substrate-mimetic inhibitor of Akt.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Binding Sites
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Cell Line, Tumor
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Chemistry, Pharmaceutical / methods*
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Crystallography, X-Ray
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Drug Design
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Drug Screening Assays, Antitumor
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology
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Glycogen Synthase Kinase 3 / chemistry*
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Glycogen Synthase Kinase 3 beta
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Humans
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Models, Chemical
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Neoplasms / drug therapy*
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Peptides / chemistry
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Proto-Oncogene Proteins c-akt / chemistry*
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Substrate Specificity
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Peptides
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GSK3B protein, human
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Glycogen Synthase Kinase 3 beta
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Proto-Oncogene Proteins c-akt
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Glycogen Synthase Kinase 3