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Cortistatin A is a High-Affinity Ligand of Protein Kinases ROCK, CDK8, and CDK11

Authors

  • Victor J. Cee Dr.,

    1. Departments of Medicinal Chemistry and Molecular Structure, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320 (USA), Fax: (+1) 805-480-1337
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  • David Y.-K. Chen Dr.,

    1. Chemical Synthesis Laboratory@Biopolis, Institute of Chemical Engineering Sciences (ICES), Agency for Science, Technology, and Research (A*STAR), 11 Biopolis Way, The Helios Block, no. 03-08, Singapore 138667 (Singapore)
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  • Matthew R. Lee Dr.,

    1. Departments of Medicinal Chemistry and Molecular Structure, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320 (USA), Fax: (+1) 805-480-1337
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  • K. C. Nicolaou Prof. Dr.

    1. Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037 (USA)
    2. Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093 (USA)
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  • We thank Dr. Randy Hungate, Dr. Andrew Tasker, and Dr. Yax Sun (Amgen Inc.) for their support.

Abstract

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Antiproliferatives Alkaloid: Cortistatin A ist ein hochaffiner Ligand für einen kleinen Satz von Proteinkinasen, einschließlich der Rho-assoziierten Proteinkinase (ROCK), der Cyclin-abhängigen Kinase 8 (CDK8) und der Cyclin-abhängigen Kinase 11 (CDK11). Modelle von Cortistatin A im Komplex mit einer kristallographischen Struktur von ROCK (siehe Bild) und ein Homologiemodell von CDK8 werden präsentiert.

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