✦ LIBER ✦
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
✍ Scribed by Valentina Corradi; Manuela Mancini; Fabrizio Manetti; Sara Petta; Maria Alessandra Santucci; Maurizio Botta
- Publisher
- Elsevier Science
- Year
- 2010
- Tongue
- English
- Weight
- 679 KB
- Volume
- 20
- Category
- Article
- ISSN
- 0960-894X
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✦ Synopsis
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.