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olaratumab

Ligand Summary
Description
Olaratumab is a human IgG1 antibody that binds platelet-derived growth factor receptor alpha (PDGFR-alpha). PDGFR-alpha is a receptor tyrosine kinase expressed on cells of mesenchymal origin. Signaling through this receptor plays a role in cell growth, chemotaxis, and mesenchymal stem cell differentiation. The receptor has also been detected on some tumor and stromal cells, including sarcomas, where signaling can contribute to cancer cell proliferation, metastasis, and maintenance of the tumor microenvironment. The interaction between olaratumab and PDGFR-alpha prevents binding of the receptor by the PDGF-AA and -BB ligands as well as PDGF-AA, -BB, and -CC-induced receptor activation and downstream PDGFR-alpha pathway signaling. Olaratumab exhibits in vitro and in vivo anti-tumor activity against selected sarcoma cell lines and disrupted the PDGFR-alpha signaling pathway in in vivo tumor implant models.
Synonyms & Links
DrugCentral: 5183
LyCHI:  olaratumab


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Target Activities