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TrkC-Targeted Kinase Inhibitors And PROTACs.

ABSTRACT: A small molecule motif (IY-IY), which binds the tropomyosin receptor kinase C (TrkC), was used to deliver the promiscuous kinase inhibitor (KI) dasatinib into breast cancer. Conjugates with noncleavable (1) and cleavable (2) linkers were compared in cellular assays and shown to have more impact on the cell viabilities of TrkC+ breast cancer cells over TrkC- epithelial cells. The IY-IY fragment was also used to recruit the E3 ligase cereblon, giving a potent proteolysis targeting chimeric (PROTAC) for TrkC degradation in metastatic breast cancer cells.

SUBMITTER: Zhao B 

PROVIDER: S-EPMC7034693 | biostudies-literature | 2019 Oct

REPOSITORIES: biostudies-literature

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TrkC-Targeted Kinase Inhibitors And PROTACs.

Zhao Bosheng B   Burgess Kevin K  

Molecular pharmaceutics 20190912 10

A small molecule motif (IY-IY), which binds the tropomyosin receptor kinase C (TrkC), was used to deliver the promiscuous kinase inhibitor (KI) dasatinib into breast cancer. Conjugates with noncleavable (<b>1</b>) and cleavable (<b>2</b>) linkers were compared in cellular assays and shown to have more impact on the cell viabilities of TrkC<sup>+</sup> breast cancer cells over TrkC<sup>-</sup> epithelial cells. The IY-IY fragment was also used to recruit the E3 ligase cereblon, giving a potent pr  ...[more]

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