1. Academic Validation
  2. Antiangiogenic Activity of Alofanib, an Allosteric Inhibitor of Fibroblast Growth Factor Receptor 2

Antiangiogenic Activity of Alofanib, an Allosteric Inhibitor of Fibroblast Growth Factor Receptor 2

  • Bull Exp Biol Med. 2015 Nov;160(1):84-7. doi: 10.1007/s10517-015-3104-5.
D A Khochenkov 1 E Sch Solomko 2 N M Peretolchina 2 O O Ryabaya 2 3 E V Stepanova 2
Affiliations

Affiliations

  • 1 N. N. Blokhin Russian Cancer Research Center, Moscow, Russia. khochenkov@gmail.com.
  • 2 N. N. Blokhin Russian Cancer Research Center, Moscow, Russia.
  • 3 N. I. Pirogov Russian National Research Medical University, Ministry of Health of the Russian Federation, Moscow, Russia.
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.

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