(D)-PPA 1

(D)-PPA 1 is a hydrolysisresistant d-peptide antagonist. (D)-PPA 1 serves as a potent PD-1/PD-L1 inhibitor. (D)-PPA 1 binds to PD-1 with the affinity 0f 0.51 μM with in vitro and in vivo efficacy[1].

Research Areas >> Cancer

Signaling Pathways >> Immunology/Inflammation >> PD-1/PD-L1

(D)-PPA 1 (0.2 mg/mL, 1.0 mg/mL) 在 1.0 mg/mL 时阻断 PD-1/PD-L1 之间的相互作用[1]。 (d) -ppa 1 (3.125-100 μM;24 h, 48 h) 不直接杀死肿瘤细胞，对 CT26 细胞生长无影响[1]。 Cell Viability Assay[1] Cell Line: CT26 cells Concentration: 3.125, 6.25, 12.5, 25, 50, and 100 μM Incubation Time: 24 hours, 48 hours Result: Left tumor cells growing normally.

(D)-PPA 1 (2 mg/kg; 皮下注射或腹腔注射; 每天 1 次, 共 7 天) 抑制小鼠体内 CT26 肿瘤的生长[1]。 (D)-PPA 1 (40 μg/mouse in 200 μL; i.v.; single dose) 具有靶向 CT26 荷瘤小鼠肿瘤组织的能力[1]。 Animal Model: CT26-tumor-bearing Balb/c mice[1] Dosage: 2 mg/kg Administration: 1) Subcutaneous injection, for around the tumor once every day for 7 days 2) Intraperitoneal injection, once every day for 7 days3) Intraperitoneal injection, once every day for 12 days; recorded the survival on day 13 Result: Inhibited tumor growth, and prolonged the survival in mice.

[1]. Chang HN, et al. Blocking of the PD-1/PD-L1 Interaction by a D-Peptide Antagonist for Cancer Immunotherapy. Angew Chem Int Ed Engl. 2015 Sep 28;54(40):11760-4.