Thursday, July 15, 2021

Covalent PROTACs: the best of both worlds?

Neil P. Grimster

RSC Med. Chem., 2021

https://doi.org/10.1039/D1MD00191D

Covalent PROTACs combine the cutting edge research areas of targeted covalent inhibitors (TCIs) and proteolysis targeting chimeras (PROTACs). This nascent field of research has already demonstrated several interesting findings, and holds an immense amount of potential to expand the druggable proteome. In this opinion, we present some of these intriguing early findings and discuss the potential advantages and disadvantages of this approach.



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Glecirasib, a potent and selective covalent KRAS G12C inhibitor exhibiting synergism 2 with cetuximab or SHP2 inhibitor JAB-3312

Wang, P., Sun, X., He, X., Kang, D., Liu, X., Liu, D., Li, A., Yang, G., Lin, Y., Li, S., Wang, Y., & Wang, Y. Cancer research communica...