BMS-1166 是 PD-1/PD-L1 相互作用的有效抑制劑,其 IC50 值為 1.4 nM。BMS-1166 可拮抗 PD-1/PD-L1 免疫檢查點(diǎn)對(duì) T 細(xì)胞活化的抑制作用。
[1]. Guzik K, et al. Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) Interaction via Transiently Induced Protein States and Dimerization of PD-L1. J Med Chem. 2017 Jul 13;60(13):5857-5867.
[2]. Skalniak L, et al. Small-molecule inhibitors of PD-1/PD-L1 immune checkpoint alleviate the PD-L1-induced exhaustion of T-cells. Oncotarget. 2017 Aug 7;8(42):72167-72181.
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