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