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Specific Blocking of CREB/DNA Binding by Cyclometalated Platinum(II) Complexes

Authors

  • Ping Wang,

    1. Department of Chemistry and Open Laboratory of Chemical Biology of the Institute of Molecular Technology for Drug Discovery and Synthesis, The University of Hong Kong, Pokfulam Road, Hong Kong (P.R. China), Fax: (+852) 2857-1586
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    • These authors contributed equally to this work.

  • Dr. Chung-Hang Leung,

    1. Department of Chemistry and Open Laboratory of Chemical Biology of the Institute of Molecular Technology for Drug Discovery and Synthesis, The University of Hong Kong, Pokfulam Road, Hong Kong (P.R. China), Fax: (+852) 2857-1586
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    • These authors contributed equally to this work.

  • Dr. Dik-Lung Ma,

    1. Department of Chemistry and Open Laboratory of Chemical Biology of the Institute of Molecular Technology for Drug Discovery and Synthesis, The University of Hong Kong, Pokfulam Road, Hong Kong (P.R. China), Fax: (+852) 2857-1586
    2. Present address: Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong (P.R. China)
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  • Dr. Raymond Wai-Yin Sun,

    1. Department of Chemistry and Open Laboratory of Chemical Biology of the Institute of Molecular Technology for Drug Discovery and Synthesis, The University of Hong Kong, Pokfulam Road, Hong Kong (P.R. China), Fax: (+852) 2857-1586
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  • Dr. Siu-Cheong Yan,

    1. Department of Chemistry and Open Laboratory of Chemical Biology of the Institute of Molecular Technology for Drug Discovery and Synthesis, The University of Hong Kong, Pokfulam Road, Hong Kong (P.R. China), Fax: (+852) 2857-1586
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  • Dr. Qing-Shou Chen,

    1. Department of Chemistry and Open Laboratory of Chemical Biology of the Institute of Molecular Technology for Drug Discovery and Synthesis, The University of Hong Kong, Pokfulam Road, Hong Kong (P.R. China), Fax: (+852) 2857-1586
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  • Prof. Dr. Chi-Ming Che

    Corresponding author
    1. Department of Chemistry and Open Laboratory of Chemical Biology of the Institute of Molecular Technology for Drug Discovery and Synthesis, The University of Hong Kong, Pokfulam Road, Hong Kong (P.R. China), Fax: (+852) 2857-1586
    • Department of Chemistry and Open Laboratory of Chemical Biology of the Institute of Molecular Technology for Drug Discovery and Synthesis, The University of Hong Kong, Pokfulam Road, Hong Kong (P.R. China), Fax: (+852) 2857-1586
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  • This work was supported by the Area of Excellence Scheme established under the University Grants Committee of the Hong Kong Special Administrative Region, China (AoE/P-10/01), The University of Hong Kong (University Development Fund), and the Innovation Technology Fund (ITS/134/09FP) administrated by the Innovation Technology Commission of the Hong Kong Special Administrative Region, China. CREB=cAMP response element binding protein.

Abstract

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In the groove: The unique major-groove-binding properties of a PtII complex can be used to block the interaction between the transcription factor CREB and DNA (see picture). Variation of the ligands around the PtII center changes the DNA binding mode and results in specific gene regulators with superior potency and selectivity.

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