Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RETV804M Kinase.
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ABSTRACT:
SUBMITTER: Newton R
PROVIDER: S-EPMC7153033 | biostudies-literature | 2020 Apr
REPOSITORIES: biostudies-literature
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Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RET<sup>V804M</sup> Kinase.
Newton Rebecca R Waszkowycz Bohdan B Seewooruthun Chitra C Burschowsky Daniel D Richards Mark M Hitchin Samantha S Begum Habiba H Watson Amanda A French Eleanor E Hamilton Niall N Jones Stuart S Lin Li-Ying LY Waddell Ian I Echalier Aude A Bayliss Richard R Jordan Allan M AM Ogilvie Donald D
ACS medicinal chemistry letters 20200228 4
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<sup>V804M</sup> 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. ...[more]
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