Tag: PD-1

Infigratinib (BGJ-398) is an Orally Active FGFR Inhibitor

The fibroblast growth factor receptor (FGFR) family of receptor tyrosine kinases (RTKs) comprises four members (FGFR1, FGFR2, FGFR3, and FGFR4) that share significant sequence homology. This family of RTKs serves as high-affinity receptors for the fibroblast growth factors (FGFs) that control cell proliferation, apoptosis, and differentiation and are involved...

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...