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.
Keywords:
allosteric inhibitor of FGFR2; alofanib; endothelial cells; tumor angiogenesis.
MeSH terms
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Alanine / analogs & derivatives
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Alanine / pharmacology
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Alanine / therapeutic use
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Allosteric Regulation
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Angiogenesis Inhibitors / pharmacology
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Angiogenesis Inhibitors / therapeutic use*
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Animals
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Benzoates / pharmacology
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Benzoates / therapeutic use*
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Bevacizumab / pharmacology
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Bevacizumab / therapeutic use
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Cell Line
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Collagen
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Drug Combinations
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Endothelial Cells / drug effects
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Female
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Fibroblast Growth Factor 2 / antagonists & inhibitors
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Fibroblast Growth Factor 2 / pharmacology
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Heparin / pharmacology
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Human Umbilical Vein Endothelial Cells
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Humans
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Laminin
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Male
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Mice
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Mice, Nude
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Neovascularization, Pathologic / drug therapy*
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Ovarian Neoplasms
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Proteoglycans
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Random Allocation
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Receptor, Fibroblast Growth Factor, Type 2 / antagonists & inhibitors*
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Sulfonamides / pharmacology
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Sulfonamides / therapeutic use*
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Triazines / pharmacology
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Triazines / therapeutic use
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Vascular Endothelial Growth Factor A / pharmacology
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Xenograft Model Antitumor Assays
Substances
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Angiogenesis Inhibitors
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Benzoates
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Drug Combinations
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Laminin
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Proteoglycans
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Sulfonamides
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Triazines
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Vascular Endothelial Growth Factor A
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Fibroblast Growth Factor 2
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matrigel
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Bevacizumab
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Heparin
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Collagen
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brivanib
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FGFR2 protein, human
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Receptor, Fibroblast Growth Factor, Type 2
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alofanib
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Alanine