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.



A multicenter, open-label, first-in-human study of TYRA-200 in advanced intrahepatic cholangiocarcinoma and other solid tumors with activating FGFR2 gene alterations (SURF201).

Jordi Rodon Ahnert ,  Sameek Roychowdhury ,  Haley Ellis ,  Fernando F. Blanco ,  Timothy Burn ,  Jennifer Michelle Davis ,  Alex Balcer ,  ...