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Metal–Bis(2-picolyl)amine Complexes as State 1(T) Inhibitors of Activated Ras Protein

Rosnizeck, Ina C. and Spoerner, Michael and Harsch, Tobias and Kreitner, Sandra and Filchtinski, Daniel and Herrmann, Christian and Engel , Daniel and König, Burkhard and Kalbitzer, Hans Robert (2012) Metal–Bis(2-picolyl)amine Complexes as State 1(T) Inhibitors of Activated Ras Protein. Angewandte Chemie International Edition 51, pp. 10647-10651.

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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 Zn(2+) -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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Item type:Article
Institutions:Biology, Preclinical Medicine > Institut für Biophysik und physikalische Biochemie > Prof. Dr. Dr. Hans Robert Kalbitzer
Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König
Identification Number:
22996816PubMed ID
Keywords:conformational dynamics · drug design · Ras protein · signal transduction
Dewey Decimal Classification:500 Science > 540 Chemistry & allied sciences
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Deposited on:22 Oct 2012 12:05
Last modified:22 Oct 2012 12:05
Item ID:26541
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