Regeneron Pharmaceuticals, Inc.

George Brian Whitaker

David R Jones

Jan Susan Rosenbaum

Peptides that specifically interfere with the ability of VEGFto interact with the NP-1 receptor or with a VEGFR-2/NP-1 co-receptor complex are disclosed. The inventive peptides are useful to control pathological angiogenesis, such as occurs in cancer and other diseases. The peptides are based on a combination of basic residues contained within Exon 6 of human placental growth factor (PIGF), coupled at the carboxyl terminus to either Exon 8 of VEGFor Exon 7 of PIGF. The peptides behave as antagonists of VEGFsignaling through a mechanism that involves competition for VEGFbinding at either the VEGFR-2/NP-1 complex or NP-1, without affecting VEGF signaling through other pathways. This binding is sufficient to attenuate pathological angiogenesis such as occurs in tumor growth.

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West Chester, OH, United States of America

George Brian Whitaker