Development of withaferin A analogs as probes of angiogenesis Article

Yokota, Y, Bargagna-Mohan, P, Ravindranath, PP et al. (2006). Development of withaferin A analogs as probes of angiogenesis . BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 16(10), 2603-2607. 10.1016/j.bmcl.2006.02.039

cited authors

  • Yokota, Y; Bargagna-Mohan, P; Ravindranath, PP; Kim, KB; Mohan, R

authors

abstract

  • The natural product withaferin A (WFA) is a potent angiogenesis inhibitor and it targets the ubiquitin-proteasome pathway in vascular endothelial cells. We generated a biotinylated affinity analog WFA-LC2B for use as a probe to study angiogenesis. WFA-LC2B inhibits angiogenic sprouting in vitro and it causes levels of ubiquitinated proteins to increase in tumor necrosis factor-α-treated human umbilical vein endothelial cells, confirming the retention of WFA's biological activity. We show that WFA-LC2B forms protein adducts in endothelial cells which are competed by free WFA in vivo. This WFA-LC2B analog will be useful to isolate the biological target of WFA. © 2006 Elsevier Ltd. All rights reserved.

publication date

  • May 15, 2006

published in

Digital Object Identifier (DOI)

start page

  • 2603

end page

  • 2607

volume

  • 16

issue

  • 10