TPP-1 hydrochloride

TPP-1, a peptide inhibitor, targets the interaction between programmed cell death protein 1 (PD-1) and its ligand (PD-L1), binding specifically to PD-L1 with a dissociation constant (Kd) of 94.67 nM. At a concentration of 20 µM, TPP-1 effectively counteracts the PD-L1-induced suppression of IFN-? production in anti-CD3-stimulated isolated human CD4+ T cells. Furthermore, TPP-1 demonstrates significant efficacy in reducing tumor volume in a mouse xenograft model of HL-60 leukemia. This model involved HL-60 cells co-cultured with anti-CD3-activated isolated human CD4+ T cells, with TPP-1 administration at a dosage of 4 mg/kg showing notable antitumor activity.

O=C(NCC(N[C@@H](CCC(N)=O)C(N[C@@H](CC1=CC=C(O)C=C1)C(N[C@H](C(N[C@@H](CO)C(N[C@@H](CC2=CC=C(O)C=C2)C(N[C@@H](CC3=CNC=N3)C(N[C@@H](CS[H])C(N[C@@H](CC4=CNC5=C4C=CC=C5)C(N[C@@H](CS[H])C(N[C@@H](CC6=CNC7=C6C=CC=C7)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(O)=O)C(N8CCC[C@H]8C(NCC(N[C@@H](CCCNC(N)=N)C(N[C@@H](CO)C(NCC(NCC(N[C@@H](CO)C(N[C@@H](CCCCN[H])C(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)C)=O)=O)=O)[C@H](CO)N[H].Cl