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 …
Bioorganic & medicinal chemistry letters, 2010•Elsevier
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.
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.
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.
Elsevier