Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases

  • Bioorg Med Chem Lett. 2006 Jan 1;16(1):129-33. doi: 10.1016/j.bmcl.2005.09.036.
Sun-Young Han  1 ,  Seok-Soon Park ,  Woo Ghil Lee ,  Yong Ki Min ,  Bum Tae Kim
Affiliations
  • 1. Bio-Organic Science Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea.
PMID: 16216503 DOI: 10.1016/j.bmcl.2005.09.036
Abstract

A novel biotin-tagged photoaffinity probe was synthesized and evaluated as a vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase inhibitor. The probe (2) is a potent VEGFR-2 inhibitor with an IC(50) value of 7.1 microM, and inhibits VEGF-induced proliferation in human umbilical vein endothelial cells (HUVEC), with an IC(50) value of 40.3 microM. This probe will be a useful reagent for investigating ligand-protein interactions.

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