GP369, an FGFR2-IIIb Specific Antibody, Exhibits Potent Antitumor Activity against Human Cancers Driven by Activated FGFR2 Signaling

Bai, A., et al., 70 19), 7630-7639, Cancer Research, 2010

Aberrant activation of FGF receptor 2 (FGFR2) signaling, through overexpression of FGFR2 and/or its ligands, mutations, and receptor amplification, has been found in a variety of human tumors. The authors generated monoclonal antibodies against the extracellular ligand-binding domain of FGFR2 to address the role of FGFR2 in tumorigenesis and to explore the potential of FGFR2 as a novel therapeutic target. Octet QK system analysis revealed specific binding of a highly potent antibody called GP369 to human and mouse FGFR2-IIIb. Further epitope mapping studies were performed on the Octet system with Streptavidin biosensors by binding GP369 to 10 overlapping peptides covering the COOH-terminal half of the third Ig domain of human FGFR2-IIIb. Peptides 4, 5 and 6 showed strong binding, consistent with crystallographic data.

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