The programmed death-1/programmed death-ligand 1 (PD-1/PD-L1) interaction plays a dominant role in the suppression of T cell responses, especially in a tumor microenvironment, protecting tumor cells from lysis. PD-1/PD-L1 inhibitor 2 is reported to prevent the interaction of PD-L1 with PD-1 with an IC50 value of 18 nM.
BMS-202 is a Novel inhibitor of the PD-1/PD-L1 interaction by inducing PD-L1 dimerization through PD-1 interacting surface.
1) Zak?et al.?(2016),?Structural basis for small molecule targeting of the programmed death ligand 1 (PD-L1);?Oncotarget?7?30323
2) Guzik?et al.?(2017),?Small-molecule inhibitors of the programmed cell death -1/programmed cell death -ligand 1(PD-1/PD-L1) interaction via transiently induced protein states and dimerization of PD-L1;?J. Med. Chem.?60?5857
