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Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RETV804M Kinase
ACS Medicinal Chemistry Letters ( IF 4.2 ) Pub Date : 2020-02-28 , DOI: 10.1021/acsmedchemlett.9b00615 Rebecca Newton 1 , Bohdan Waszkowycz 1 , Chitra Seewooruthun 2 , Daniel Burschowsky 2 , Mark Richards 3 , Samantha Hitchin 1 , Habiba Begum 1 , Amanda Watson 1 , Eleanor French 1 , Niall Hamilton 1 , Stuart Jones 1 , Li-Ying Lin 4 , Ian Waddell 1 , Aude Echalier 2 , Richard Bayliss 3 , Allan M. Jordan 1 , Donald Ogilvie 1
ACS Medicinal Chemistry Letters ( IF 4.2 ) Pub Date : 2020-02-28 , DOI: 10.1021/acsmedchemlett.9b00615 Rebecca Newton 1 , Bohdan Waszkowycz 1 , Chitra Seewooruthun 2 , Daniel Burschowsky 2 , Mark Richards 3 , Samantha Hitchin 1 , Habiba Begum 1 , Amanda Watson 1 , Eleanor French 1 , Niall Hamilton 1 , Stuart Jones 1 , Li-Ying Lin 4 , Ian Waddell 1 , Aude Echalier 2 , Richard Bayliss 3 , Allan M. Jordan 1 , Donald Ogilvie 1
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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.
中文翻译：
发现和优化RET V804M激酶的wt-RET / KDR选择性抑制剂
聚焦库和虚拟筛选，命中扩展和合理设计的结合，导致了一系列RET V804M激酶抑制剂的开发，该抑制剂是预期的RET激酶耐药突变体。这些药物不抑制RET或KDR的野生型（wt）亚型，因此可为目前正在临床评估中的RET抑制剂提供潜在的辅助药物。
更新日期：2020-02-28
中文翻译：
发现和优化RET V804M激酶的wt-RET / KDR选择性抑制剂
聚焦库和虚拟筛选，命中扩展和合理设计的结合，导致了一系列RET V804M激酶抑制剂的开发，该抑制剂是预期的RET激酶耐药突变体。这些药物不抑制RET或KDR的野生型（wt）亚型，因此可为目前正在临床评估中的RET抑制剂提供潜在的辅助药物。
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