title: Antiangiogenic Activity of Alofanib, an Allosteric Inhibitor of Fibroblast Growth Factor Receptor 2.
abstract: Alofanib is a potential allosteric inhibitor of FGFR2 used in oncology. The inhibitor blocks the extracellular part of the receptor and prevents its binding with the ligand. Alofanib suppressed proliferation of endothelial cells, their migration activity, and ability to form vessellike structures in vitro and significantly decreased the number of microvessels in Matrigel implant and in ovarian cancer (SKOV-3) xenograft in vivo. The results indicate that Alofanib can inhibit angiogenesis.
authors.affiliation: N. N. Blokhin Russian Cancer Research Center, Moscow, Russia. khochenkov@gmail.com.
authors.forename: D A
authors.initials: DA
authors.lastname: Khochenkov
authors.affiliation: N. N. Blokhin Russian Cancer Research Center, Moscow, Russia.
authors.forename: E Sch
authors.initials: ES
authors.lastname: Solomko
authors.affiliation: N. N. Blokhin Russian Cancer Research Center, Moscow, Russia.
authors.forename: N M
authors.initials: NM
authors.lastname: Peretolchina
authors.affiliation: N. N. Blokhin Russian Cancer Research Center, Moscow, Russia.|N. I. Pirogov Russian National Research Medical University, Ministry of Health of the Russian Federation, Moscow, Russia.
authors.forename: O O
authors.initials: OO
authors.lastname: Ryabaya
authors.affiliation: N. N. Blokhin Russian Cancer Research Center, Moscow, Russia.
authors.forename: E V
authors.initials: EV
authors.lastname: Stepanova
mesh_terms: D000409:Alanine / Q000031:analogs & derivatives / Q000494:pharmacology / Q000627:therapeutic use; D000494:Allosteric Regulation; D020533:Angiogenesis Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D001565:Benzoates / Q000494:pharmacology / Q000627:therapeutic use*; D000068258:Bevacizumab / Q000494:pharmacology / Q000627:therapeutic use; D002460:Cell Line; D003094:Collagen; D004338:Drug Combinations; D042783:Endothelial Cells / Q000187:drug effects; D005260:Female; D016222:Fibroblast Growth Factor 2 / Q000037:antagonists & inhibitors / Q000494:pharmacology; D006493:Heparin / Q000494:pharmacology; D061307:Human Umbilical Vein Endothelial Cells; D006801:Humans; D007797:Laminin; D008297:Male; D051379:Mice; D008819:Mice, Nude; D009389:Neovascularization, Pathologic / Q000188:drug therapy*; D010051:Ovarian Neoplasms; D011509:Proteoglycans; D011897:Random Allocation; D051497:Receptor, Fibroblast Growth Factor, Type 2 / Q000037:antagonists & inhibitors*; D013449:Sulfonamides / Q000494:pharmacology / Q000627:therapeutic use*; D014227:Triazines / Q000494:pharmacology / Q000627:therapeutic use; D042461:Vascular Endothelial Growth Factor A / Q000494:pharmacology; D023041:Xenograft Model Antitumor Assays
chemical_list: D020533:Angiogenesis Inhibitors; D001565:Benzoates; D004338:Drug Combinations; D007797:Laminin; D011509:Proteoglycans; D013449:Sulfonamides; D014227:Triazines; D042461:Vascular Endothelial Growth Factor A; D016222:Fibroblast Growth Factor 2; C059485:matrigel; D000068258:Bevacizumab; D006493:Heparin; D003094:Collagen; C509922:brivanib; C496353:FGFR2 protein, human; D051497:Receptor, Fibroblast Growth Factor, Type 2; C000610985:alofanib; D000409:Alanine
keywords: allosteric inhibitor of FGFR2; alofanib; endothelial cells; tumor angiogenesis