کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1375979 | 981948 | 2005 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Use of PROTACS as molecular probes of angiogenesis Use of PROTACS as molecular probes of angiogenesis](/preview/png/1375979.png)
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.
E2-penta is an estradiol-peptide chemical chimera (ER-PROTAC) that binds to the estrogen receptor and targets it for proteolysis via the ubiquitin-mediated proteasome pathway. We show that E2-penta is a novel chemical genetic probe of angiogenesis as it blocks differentiation of vascular endothelial cells and potently inhibits angiogenic sprouting in vivo.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 11, 2 June 2005, Pages 2724–2727