Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RETV804M Kinase.
Basic Information
ID: ALA4342511
Journal: ACS Med Chem Lett
Title: Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RETV804M Kinase.
Authors: Newton R, Waszkowycz B, Seewooruthun C, Burschowsky D, Richards M, Hitchin S, Begum H, Watson A, French E, Hamilton N, Jones S, Lin LY, Waddell I, Echalier A, Bayliss R, Jordan AM, Ogilvie D.
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 RETV804M 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.
CiteXplore: 32292556
DOI: 10.1021/acsmedchemlett.9b00615
Patent ID: ┄