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Dr. Ina C. Rosnizeck, Priv.-Doz. Dr. Michael Spoerner, Tobias Harsch, Dr. Sandra Kreitner, Dr. Daniel Filchtinski, Prof. Dr. Christian Herrmann, Dr. Daniel Engel, Prof. Dr. Burkhard König and Prof. Dr. Dr. Hans Robert Kalbitzer Metal–Bis(2-picolyl)amine Complexes as State 1(T) Inhibitors of Activated Ras Protein Angewandte Chemie International Edition 51

Version of Record online: 20 SEP 2012 | DOI: 10.1002/anie.201204148

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Allosteric interactions: Metal(II) cyclens inhibit Ras–effector interactions by stabilizing a weak effector-binding state of Ras, state 1(T), and binding directly in the active site. The novel state (1T) inhibitor Zn2+–BPA (BPA=bis(2-picolyl)amine) binds outside the nucleotide binding pocket but nevertheless allosterically stabilizes state 1(T) and thus inhibits the Ras–Raf interaction.

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