Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 11, Issue 4, Pages 497-505Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00615
Keywords
RET; KDR; kinase inhibitor; virtual screening
Categories
Funding
- Cancer Research UK [C480/A11411, C5759/A17098]
- CRT Pioneer Fund
- CRUK Centre Network Structural Biology Accelerator Award [C1362/A20263]
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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.
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