Characterization of human circulating TIG2 as a ligand for the orphan receptor ChemR23

Characterization of human circulating TIG2 as a ligand for the orphan receptor ChemR23
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DOI:
10.1016/s0014-5793(03)01312-7
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发表时间:
2003-12-18
期刊:
影响因子:
3.5
通讯作者:
Forssmann, WG
Forssmann, WG
中科院分区:
生物学3区
文献类型:
--
作者:
Meder, W;Wendland, M;Forssmann, WG

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孤儿受体ChemR23是一种与神经肽和化学引诱剂受体同源的g蛋白偶联受体(GPCR)。他zarotene是一种合成的类维甲酸,可激活维甲酸受体(RAR),上调他zarotene-induced gene-2 (TIG2)。现在描述了该蛋白的功能和分子靶点。通过使用从人血液滤过液中生成的肽库进行反向药理学筛选,我们分离并鉴定了TIG2作为ChemR23的天然配体,并报道了具有生物活性的循环TIG2的特定分子形式,代表163个氨基酸的前肽中的氨基酸残基21至154。基于ChemR23和TIG2的表达模式,目前正在研究其在骨骼发育、免疫和炎症反应以及皮肤维持中的生理作用。(C) 2003年欧洲生化学会联合会。Elsevier B.V.版权所有。
The orphan receptor ChemR23 is a G-protein coupled receptor (GPCR) with homology to neuropeptide and chemoattractant receptors. Tazarotene, a synthetic retinoid activating retinoic acid receptor (RAR), up-regulates tazarotene-induced gene-2 (TIG2). The function and molecular target of this protein are now described. By means of reverse pharmacology screening using a peptide library generated from human hemofiltrate, we have isolated and identified TIG2 as the natural ligand of ChemR23 and report the specific molecular form of the bioactive, circulating TIG2, representing the amino-acid residues 21 to 154 of the 163 amino acid-containing prepropeptide. Based on the expression pattern of ChemR23 and TIG2, the physiological role in bone development, immune and inflammatory responses and the maintenance of skin is now being investigated. (C) 2003 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.