Use of PROTACS as molecular probes of angiogenesis

Paola Bargagna-Mohan, Sun Hee Baek, Hyosung Lee, Kyungbo Kim, Royce Mohan

Research output: Contribution to journalArticlepeer-review

55 Scopus citations


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.

Original languageEnglish
Pages (from-to)2724-2727
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number11
StatePublished - Jun 2 2005

Bibliographical note

Funding Information:
We are grateful to the Department of Ophthalmology and Visual Sciences (University of Kentucky) for generous start-up funds to R.M. and the Kentucky Lung Cancer Research Program for financial support to K.K.


  • Angiogenesis
  • Endothelial cell differentiation
  • Estrogen
  • Receptor

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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