E3 ligand-linker conjugate 3 is a building block in the synthesis of proteolysis-targeting chimera (PROTAC) technologies containing thalidomide , which is a ligand for the E3 ubiquitin ligase cereblon.1,2 It has been used in the synthesis of PROTACs for the degradation of several proteins, including anaplastic lymphoma kinase (ALK) and the bromodomain and extra terminal domain (BET) family of proteins, with anticancer activity.
1.Yan, G., Zhong, X., Yue, L., et al.Discovery of a PROTAC targeting ALK with in vivo activityEur. J. Med. Chem.212(1)113150(2021) 2.Zhou, B., Hu, J., Xu, F., et al.Discovery of a small-molecule degrader of bromodomain and extra-terminal (BET) proteins with picomolar cellular potencies and capable of achieving tumor regressionJ. Med. Chem.61(2)462-481(2018)