کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1362772 | 981495 | 2010 | 5 صفحه PDF | دانلود رایگان |

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.
The first non-peptidic small molecule able to bind 14-3-3 and to disrupt the c-Abl/14-3-3 complex was discovered by an in silico structure-based drug design approach. Its activity induces wild type and T315I Ba/F3 leukemia cells to apoptosis via cytoplasm-to-nucleus shuttling of c-Abl.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 20, 15 October 2010, Pages 6133–6137