Deutsch
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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Abstract
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
| 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 | ||||
| Projects: | DFG | ||||
| Identification Number: |
| ||||
| Keywords: | conformational dynamics · drug design · Ras protein · signal transduction | ||||
| Subjects: | 500 Science > 540 Chemistry & allied sciences | ||||
| Status: | Published | ||||
| Refereed: | Yes, this version has been refereed | ||||
| Created at the University of Regensburg: | Yes | ||||
| Owner: | Regina Hoheisel | ||||
| Deposited On: | 22 Oct 2012 14:05 | ||||
| Last Modified: | 22 Oct 2012 14:05 | ||||
| Item ID: | 26541 |
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