文章基本信息

标题：Location of Two Photoaffinity-Labeled Sites on the Ligand-Binding Domain of Retinoic Acid Receptor α
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作者：Toru SASAKI ; Rumiko SHIMAZAWA ; Takayuki SAWADA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1996
卷号：19
期号：5
页码：659-664
DOI：10.1248/bpb.19.659
出版社：The Pharmaceutical Society of Japan
摘要：Retinoic acid receptors (RARs) consist of six domain structures. The C-terminal region (D/E/F-domains) is involved in ligand binding, dimerization, and ligand-dependent transactivation. Structural information about RARs is required for understanding its complex function. A photoreactive retinoid denoted as ADAM-3, which was designed as the result of comparison of two fluorescent retinoids (DAM-3 and DAM-15), was synthesized and used for photoaffinity labeling of recombinant protein MBP-RARα/E. The photoaffinity-labeled site was determined by an endoprotease combination method which utilizes four endoproteinases in a two-phase digestion procedure. Two major labeled fragments were detected in each digestion, and the results of two-phase digestion allowed identification of the labeled residues as being located within residues 492-510 and 585-594, which correspond to 288-306 and 381-390 in human RARα, respectively.
关键词：retinoic acid receptor;photoaffinity labeling;fluorescent probe;endoproteinase combination method;retinoid