Journal of medicinal chemistryHumansProtein Kinase InhibitorsAnimalsReceptortrkA
Discovery of Novel Bifunctional Agents as Potent TRK Inhibitors and Degraders against xDFG Mutation Resistance.
Jian Song, Jingjie Zhu, Wenjian Zhu, Jinwei Feng, Jiarong Fan, Yi Mei, Qiren Shi, Yuzhuo Yang, Zhijie Feng, Peng Wang, Tianduanyi Wang, Shengtao Xu, Jinyi Xu, Huajian Zhu
Published: 202510.1021/acs.jmedchem.5c02491
Abstract
Despite the clinical success of tropomyosin receptor kinases (TRKs) inhibitors in NTRK fusion-positive cancers, prolonged administration has resulted in acquired resistance, particularly xDFG mutations, for which no approved therapies are available.…
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