Article
Insights into pralsetinib resistance to the non-gatekeeper RET kinase G810C mutation through molecular dynamics simulations.
Journal of molecular modeling - 28 Dec 2022
Cao Shu, Tan Changbin, Fei Anhua, Hu Gangqiang, Fu Ming, Lv Jun
Abstract excerpt
OBJECTIVE: RET (rearranged during transfection) kinase, as a transmembrane receptor tyrosine kinase, is a therapeutic target for several human cancer such as non-small cell lung cancer (NSCLC) and thyroid cancer. Pralsetinib is a recently approved drug for the treatment of RET-driven NSCLC and thyroid cancers. A single point mutation G810C at the C-lobe of the RET kinase causes pralsetinib resistance to this...
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