Fig. 1.

NOTCH1 signaling pathway and drug targets. Agent categories and their targets: ADAM inhibitors prevent ADAM protease S2 site digestion; γ-secretase inhibitors (GSIs) prevent the cleavage of S3 site of γ-secretase; Monoclonal antibody prevent the conformational change of the negative regulatory region (NRR) from exposing the S2 and S3 cleavage sites; SERCA inhibitors include Ca²⁺ ATPase inhibitors prevent transportation process of NOTCH1 and the formation of heterodimerization domain (HD); SAHM1 prevent the formation of ICN1-CSL-MAML complex