Tag: PD-1

Sitravatinib (MGCD516) is an Orally Bioavailable RTK Inhibitor with PD-1 Blockade Activity

Sarcomas are rare but highly aggressive mesenchymal tumors. Mutation and overexpression of many receptor tyrosine kinases (RTKs) including c-Met, PDGFR, c-Kit and IGF1-R drive defective signaling pathways in sarcomas. Sitravatinib is a small molecule inhibitor targeting multiple receptor tyrosine kinases involved in driving sarcoma cell growth. Moreover, Sitravatinib significantly...

BMSpep-57 is a Competitive Peptide Inhibitor of PD-1/PD-L1 Interaction

Programmed cell death 1 (PD-1) is a cell surface receptor. PD-1 is highly expressed on tumor-specific T cells. It is a T cell checkpoint and plays a central role in regulating T cell exhaustion. Programmed cell death ligand 1 (PD-L1) is a trans-membrane protein.  PD-L1 is a co-inhibitory factor...

TPP-1 is a Potent Inhibitor of the PD-1/PD-L1 Interaction

PD-L1 is expressed in many types of cancers. And its high expression in tumor cells or presence in TME can be indicative of tumor-infiltrating lymphocytes (TILs). Blockade of PD-1/PD-L1 can strengthen the function of effector T cells. Blockade of PD-1/PD-L1 can strengthen the function of effector T cells. Additionally,...

MSA-2 is an Orally Available STING Agonist with Anti-tumor Activity

Stimulator of interferons genes (STING) is an adaptor protein. It plays a critical role in the secretion of type I interferons and pro-inflammatory cytokines in response to cytosolic nucleic acid. STING is also an endoplasmic reticulum-associated homodimeric protein. It is the receptor for cGAMP. The cGAMP is a second...