Use of PROTACS as molecular probes of angiogenesis

被引：57

作者：

Bargagna-Mohan, P

Baek, SH

Lee, H

Kim, K

Mohan, R ^{[1
]}

机构：

[1] Univ Kentucky, Dept Ophthalmol & Visual Sci, Lexington, KY 40536 USA

[2] Univ Kentucky, Dept Pharmaceut Sci, Lexington, KY 40536 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 11期

关键词：

PROTACS; angiogenesis; estrogen; receptor; endothelial cell differentiation;

D O I：

10.1016/j.bmcl.2005.04.008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (c) 2005 Elsevier Ltd. All rights reserved.

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收藏

页码：2724 / 2727

页数：4

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