An in silico structure-based ligand design approach resulted in the identification of the first non-peptidic small molecule able to inhibit protein-protein interactions between 14-3-3 and c-Abl. This compound shows an anti-proliferative effect on human leukemia cells either sensitive or resistant to Imatinib, in consequence of the T315I mutation. It also mediates c-Abl release from 14-3-3 in a way similar to that found in response to Imatinib treatment.
Corradi, V., Mancini, M., Manetti, F., Petta, S., Santucci, M.A., Botta, M. (2010). Identification of the First Non-Peptidic Small Molecule Inhibitor of the c-Abl/14-3-3 Protein-Protein Interactions Able to Drive Sensitive and Imatinib-Resistant Leukemia Cells to Apoptosis. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 20(20), 6133-6137 [10.1016/j.bmcl.2010.08.019].
Identification of the First Non-Peptidic Small Molecule Inhibitor of the c-Abl/14-3-3 Protein-Protein Interactions Able to Drive Sensitive and Imatinib-Resistant Leukemia Cells to Apoptosis
Manetti, Fabrizio;Botta, Maurizio
2010-01-01
Abstract
An in silico structure-based ligand design approach resulted in the identification of the first non-peptidic small molecule able to inhibit protein-protein interactions between 14-3-3 and c-Abl. This compound shows an anti-proliferative effect on human leukemia cells either sensitive or resistant to Imatinib, in consequence of the T315I mutation. It also mediates c-Abl release from 14-3-3 in a way similar to that found in response to Imatinib treatment.
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https://hdl.handle.net/11365/10915
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