Article
Dasatinib Stimulates Its Own Mechanism of Resistance by Activating a CRTC3/MITF/Bcl-2 Pathway in Melanoma with Mutant or Amplified c-Kit.
Molecular cancer research : MCR - 1 Jul 2021
Sabbah Malak, Krayem Mohammad, Najem Ahmad, Sales François, Miller Wilson, Del Rincon Sonia, Awada Ahmad, Ghanem Ghanem E, Journe Fabrice
Abstract excerpt
Amplification or activating mutations of c-Kit are a frequent oncogenic alteration, which occurs commonly in acral and mucosal melanoma. Among c-Kit inhibitors, dasatinib is the most active due to its ability to bind both active and inactive conformations of the receptor. However, its use as a single agent in melanoma showed limited clinical benefit. We first found that sensitivity to dasatinib is restricted to...
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