• Open Access

Non-ATP-Mimetic Organometallic Protein Kinase Inhibitor

Authors

  • Kathrin Wähler,

    1. Fachbereich Chemie, Philipps-Universität Marburg, Hans-Meerwein-Straße, 35043 Marburg (Germany)
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  • Katja Kräling,

    1. Fachbereich Chemie, Philipps-Universität Marburg, Hans-Meerwein-Straße, 35043 Marburg (Germany)
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  • Dr. Holger Steuber,

    Corresponding author
    1. LOEWE-Zentrum für Synthetische Mikrobiologie, Philipps-Universität Marburg, Hans-Meerwein-Straße, 35043 Marburg (Germany)
    2. Present address: Bayer Pharma AG, Lead Discovery Berlin – Structural Biology, Müllerstraße 178, 13353 Berlin (Germany)
    • Holger Steuber, LOEWE-Zentrum für Synthetische Mikrobiologie, Philipps-Universität Marburg, Hans-Meerwein-Straße, 35043 Marburg (Germany)

      Eric Meggers, Fachbereich Chemie, Philipps-Universität Marburg, Hans-Meerwein-Straße, 35043 Marburg (Germany)

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  • Prof. Dr. Eric Meggers

    Corresponding author
    1. Fachbereich Chemie, Philipps-Universität Marburg, Hans-Meerwein-Straße, 35043 Marburg (Germany)
    2. College of Chemistry and Chemical Engineering, Xiamen University, Xiamen 361005 (P. R. China)
    • Holger Steuber, LOEWE-Zentrum für Synthetische Mikrobiologie, Philipps-Universität Marburg, Hans-Meerwein-Straße, 35043 Marburg (Germany)

      Eric Meggers, Fachbereich Chemie, Philipps-Universität Marburg, Hans-Meerwein-Straße, 35043 Marburg (Germany)

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Abstract

original image

Non-hinge binding: A novel organometallic protein kinase inhibitor scaffold based on a cyclometalated 1,8-phenanthrolin-7(8 H)-one ligand is reported, which binds to the ATP binding site of the protein kinase Pim1 in an unexpected, unusual non-ATP-mimetic fashion without mimicking the hydrogen-bonding interaction of the adenine nucleobase of ATP.

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