Novel small-molecule inhibitors of the vascular endothelial growth factor receptor.
Sustained angiogenesis is one of the hallmarks of carcinogenesis. Vascular endothelial growth factor (VEGF) is a critical molecule mediating pro-angiogenic signals against which a number of therapeutic approaches have been designed. The 2 predominant approaches to inhibiting VEGF signalling are the use of monoclonal antibodies to block the receptor or ligand and small molecule receptor kinase inhibitors. There are several small-molecule inhibitors of tyrosine kinase activity of VEGF receptors in clinical trials. These are discussed in this review.
Adjei
Alex A
AA
Roswell Park Cancer Institute, Buffalo, NY 14263, USA. alex.adjei@roswellpark.org
D020533:Angiogenesis Inhibitors / Q000627:therapeutic use*; D000818:Animals; D000911:Antibodies, Monoclonal / Q000627:therapeutic use; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000503:physiopathology; D009389:Neovascularization, Pathologic / Q000188:drug therapy; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use; D040262:Receptors, Vascular Endothelial Growth Factor / Q000037:antagonists & inhibitors*; D015398:Signal Transduction / Q000502:physiology
D020533:Angiogenesis Inhibitors; D000911:Antibodies, Monoclonal; D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D040262:Receptors, Vascular Endothelial Growth Factor