(PROTAC)

PROTAC.png

PROTAC: Heterobifunctional Proteolysis-Targeting Chimeric molecules (PROTACs). Signet Tx will be also developing the degrader to overcome the potential drug resistance of target inhibitor and enhance the efficacy of elimination of target function.

Advantages of this approach include:

(i)that PROTACs can act catalytically;

(ii)that the pharmacodynamic effect of a PROTAC persists until the target can reaccumulate

(iii) that all functions of a target are eliminated simultaneously;

(iv) that all one needs to assemble a PROTAC is a small molecule that binds the target specifically—it is not necessary that the small molecule modulates target function.

 

Raymond, et al, Nature, 2020