Selectively Targeting Tropomyosin Receptor Kinase A (TRKA) via PROTACs.

Published in: Journal of medicinal chemistry (2020)

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.

Keyphrases

small molecule
cancer therapy
acute coronary syndrome
high throughput
squamous cell carcinoma
tyrosine kinase
binding protein
childhood cancer