Use of PROTACS as molecular probes of angiogenesis Article

Bargagna-Mohan, P, Baek, SH, Lee, H et al. (2005). Use of PROTACS as molecular probes of angiogenesis . BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 15(11), 2724-2727. 10.1016/j.bmcl.2005.04.008

cited authors

  • Bargagna-Mohan, P; Baek, SH; Lee, H; Kim, K; Mohan, R



  • Small molecules designed to specifically activate or inactivate protein functions have been useful to study biological processes. PROTACS are small molecule chimera which comprise a ligand and a peptide recognition motif for an E3 ligase. These novel reagents exploit the ubiquitin-mediated proteasome degradation pathway to target the ligand-bound protein for intracellular degradation. Here, we report that an estrogen receptor (ER)-targeting PROTACS that causes degradation of ER is able to potently inhibit endothelial cell differentiation in a three-dimensional angiogenic sprouting assay. These findings support the use of ER-targeting PROTACS as probes of angiogenesis. © 2005 Elsevier Ltd. All rights reserved.

publication date

  • June 2, 2005

Digital Object Identifier (DOI)

start page

  • 2724

end page

  • 2727


  • 15


  • 11