title: Vascular endothelial growth factor and vascular endothelial growth factor receptor inhibitors as anti-angiogenic agents in cancer therapy.
abstract: New blood vessel formation (angiogenesis) is fundamental to the process of tumor growth, invasion, and metastatic dissemination. The vascular endothelial growth factor (VEGF) family of ligands and receptors are well established as key regulators of these processes. VEGF is a glycoprotein with mitogenic activity on vascular endothelial cells. Specifically, VEGF-receptor pathway activation results in signaling cascades that promote endothelial cell growth, migration, differentiation, and survival from pre-existing vasculature. Thus, the role of VEGF has been extensively studied in the pathogenesis and angiogenesis of human cancers. Recent identification of seven VEGF ligand variants (VEGF [A-F], PIGF) and three VEGF tyrosine kinase receptors (VEGFR- [1-3]) has led to the development of several novel inhibitory compounds. Clinical trials have shown inhibitors to this pathway (anti-VEGF therapies) are effective in reducing tumor size, metastasis and blood vessel formation. Clinically, this may result in increased progression free survival, overall patient survival rate and will expand the potential for combinatorial therapies. Having been first described in the 1980s, VEGF patenting activity since then has focused on anti-cancer therapeutics designed to inhibit tumoral vascular formation. This review will focus on patents which target VEGF-[A-F] and/or VEGFR-[1-3] for use in anti-cancer treatment.
authors.affiliation: Department of Neurosurgery, Stanford University School of Medicine, Stanford, CA 94305-5484, USA.
authors.forename: Anand
authors.initials: A
authors.lastname: Veeravagu
authors.forename: Andrew R
authors.initials: AR
authors.lastname: Hsu
authors.forename: Weibo
authors.initials: W
authors.lastname: Cai
authors.forename: Lewis C
authors.initials: LC
authors.lastname: Hou
authors.forename: Victor C K
authors.initials: VC
authors.lastname: Tse
authors.forename: Xiaoyuan
authors.initials: X
authors.lastname: Chen
mesh_terms: D020533:Angiogenesis Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D009369:Neoplasms / Q000150:complications / Q000188:drug therapy* / Q000473:pathology; D009389:Neovascularization, Pathologic / Q000150:complications / Q000188:drug therapy* / Q000473:pathology; D010330:Patents as Topic; D016337:RNA, Catalytic / Q000627:therapeutic use; D034741:RNA, Small Interfering / Q000627:therapeutic use; D040262:Receptors, Vascular Endothelial Growth Factor / Q000037:antagonists & inhibitors*; D042461:Vascular Endothelial Growth Factor A / Q000037:antagonists & inhibitors* / Q000502:physiology
chemical_list: D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D016337:RNA, Catalytic; D034741:RNA, Small Interfering; D042461:Vascular Endothelial Growth Factor A; D040262:Receptors, Vascular Endothelial Growth Factor