title: Use of PROTACS as molecular probes of angiogenesis.
abstract: 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.
authors.affiliation: Department of Ophthalmology and Visual Sciences, University of Kentucky, Lexington, 40536, USA.
authors.forename: Paola
authors.initials: P
authors.lastname: Bargagna-Mohan
authors.forename: Sun-Hee
authors.initials: SH
authors.lastname: Baek
authors.forename: Hyosung
authors.initials: H
authors.lastname: Lee
authors.forename: Kyungbo
authors.initials: K
authors.lastname: Kim
authors.forename: Royce
authors.initials: R
authors.lastname: Mohan
mesh_terms: D018919:Neovascularization, Physiologic; D046988:Proteasome Endopeptidase Complex / Q000378:metabolism; D011960:Receptors, Estrogen / Q000378:metabolism; D025801:Ubiquitin / Q000378:metabolism
chemical_list: D011960:Receptors, Estrogen; D025801:Ubiquitin; D046988:Proteasome Endopeptidase Complex