BMS-1166-N-piperidine-COOH, a derivative of the potent PD-1/PD-L1 interaction inhibitor BMS-1166, serves as a key component in the design of PROTAC PD-1/PD-L1 degrader-1 (HY-131183). By binding to an E3 ligase ligand via a linker, this moiety facilitates the targeted degradation of PD-1/PD-L1, offering a novel approach to modulate immune checkpoint pathways. BMS-1166 itself is a highly effective inhibitor of the PD-1/PD-L1 interaction, with an IC50 of 1.4 nM, and it counteracts the immune-suppressive effects of the PD-1/PD-L1 checkpoint on T cell activation. This innovative strategy combines the inhibitory potency of BMS-1166 with the degradation capability of PROTAC technology, providing a promising tool for advancing cancer immunotherapy and immune-related research.
