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Ruthenium Half-Sandwich Complexes Bound to Protein Kinase Pim-1

Authors


  • We gratefully acknowledge support for this work from the US National Institutes of Health through grant 1 R01 GM071695-01A1 (E.M.). The Structural Genomics Consortium is a registered charity (no. 1097737) funded by the Wellcome Trust, GlaxoSmithKline, Genome Canada, the Canadian Institutes of Health Research, the Ontario Innovation Trust, the Ontario Research and Development Challenge Fund, and the Canadian Foundation for Innovation.

Abstract

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Keeping in shape with half a sandwich: The structure of a picomolar organoruthenium inhibitor bound to the ATP-binding site of the protein kinase Pim-1 (see picture) demonstrates that the ruthenium center has solely a structural role in organizing the organic ligands in the three-dimensional receptor space, thus yielding a structure that is complementary in shape and functional group presentation to the active site of Pim-1.

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