Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RET^V804M Kinase.

ABSTRACT: A combination of focused library and virtual screening, hit expansion, and rational design has resulted in the development of a series of inhibitors of RET^V804M kinase, the anticipated drug-resistant mutant of RET kinase. These agents do not inhibit the wild type (wt) isoforms of RET or KDR and therefore offer a potential adjunct to RET inhibitors currently undergoing clinical evaluation.

SUBMITTER: Newton R 

PROVIDER: S-EPMC7153033 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature