Selectively Targeting Tropomyosin Receptor Kinase A (TRKA) via PROTACs
| Autor: | Weiguo Xiang, Shaomeng Wang |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Proteomics
Chemistry Kinase Tropomyosin receptor kinase B Tropomyosin receptor kinase A Tropomyosin receptor kinase C Tropomyosin In vitro Cell biology Cell Line Mice nervous system In vivo Drug Discovery Proteolysis Molecular Medicine Animals Humans Receptor trkA Receptor Protein Kinase Inhibitors Cell Proliferation |
| Zdroj: | Journal of medicinal chemistry. 63(23) |
| ISSN: | 1520-4804 |
| Popis: | Tropomyosin receptor kinases (TRKs) are promising cancer therapeutic targets. Chen ( J. Med. Chem. 2020, DOI: 10.1021/acs.jmedchem.0c01342) report the discovery of CG416 and CG428 as two potent small-molecule proteolysis-targeting chimera (PROTAC) degraders selective for TRKA over TRKB and TRKC. CG416 and CG428 are valuable research tool compounds for in vitro and in vivo studies and promising lead compounds for further optimization. |
| Databáze: | OpenAIRE |
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