Article
Molecular mechanism of D816X mutation-induced c-Kit activation and -mediated inhibitor resistance in gastrointestinal stromal tumor.
Journal of molecular graphics & modelling - 1 Sept 2018
Jiang Haohai, Shao Weiwei, Wang Yuanjin, Xu Ronghui, Zhou Linsen, Mu Xiangming
Abstract excerpt
The D816X (X = V, H, Y or F) missense mutation constitutively activates c-Kit kinase in gastrointestinal stromal tumor (GIST) and has been observed to cause acquired resistance against first-line and second-line kinase inhibitors. In the present study, the allosteric mechanism of D816X-induced c-Kit conformational change is investigated at molecular level. The Asp816 residue is located at the activation loop...
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