International Union of Basic and Clinical Pharmacology CIII: Chemerin Receptors CMKLR1 (Chemerin(1)) and GPR1 (Chemerin(2)) Nomenclature, Pharmacology, and Function.
International Union of Basic and Clinical Pharmacology CIII: Chemerin Receptors CMKLR1 (Chemerin(1)) and GPR1 (Chemerin(2)) Nomenclature, Pharmacology, and Function.
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DOI：
10.1124/pr.116.013177
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发表时间：
2018-01
影响因子：
21.1
通讯作者：
Davenport AP
中科院分区：
文献类型：
--
作者：
Kennedy AJ;Davenport AP
Chemerin是一种化学引诱蛋白和脂肪因子，已被鉴定为由基因CMKLR 1（也称为ChemR 23）编码的G蛋白偶联受体的内源性配体，因此该受体蛋白在2013年被重命名为Chemerin受体。从那时起，chemerin已被确定为第二个G蛋白偶联受体的内源性配体，由基因GPR 1编码。因此，国际基础与临床药理学联合会受体命名和药物分类委员会建议，趋化因子样受体1（CMKLR 1）的受体蛋白的正式名称为chemerin receptor 1，G蛋白偶联受体1为chemerin receptor 2，以遵循受体蛋白以内源性配体命名的惯例。Chemerin受体1和Chemerin受体2可分别缩写为Chemerin 1和Chemerin 2。Chemerin需要C-末端加工以获得活性，据报道人chemerin 21 -157是最具活性的形式，其C-末端衍生的肽片段对两种受体都具有生物活性。小分子拮抗剂CCX 832选择性阻断CMKLR 1，并讨论了消退素E1对CMKLR 1的激活作用。chemerin通过与Gi/o偶联激活两种受体，导致腺苷酸环化酶抑制和Ca 2+通量增加。受体和配体在人类、大鼠和小鼠中广泛表达，并且这两种受体在这些物种中具有约80%的同一性。CMKLR 1基因敲除小鼠强调了该受体在炎症和肥胖中的作用，同样，GPR 1基因敲除小鼠也表现出葡萄糖耐受不良。此外，chemerin受体与心血管疾病、癌症、类固醇生成、人类免疫缺陷病毒复制和神经变性疾病有关。
Chemerin, a chemoattractant protein and adipokine, has been identified as the endogenous ligand for a G protein–coupled receptor encoded by the gene CMKLR1 (also known as ChemR23), and as a consequence the receptor protein was renamed the chemerin receptor in 2013. Since then, chemerin has been identified as the endogenous ligand for a second G protein–coupled receptor, encoded by the gene GPR1. Therefore, the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification recommends that the official name of the receptor protein for chemokine-like receptor 1 (CMKLR1) is chemerin receptor 1, and G protein–coupled receptor 1 is chemerin receptor 2 to follow the convention of naming the receptor protein after the endogenous ligand. Chemerin receptor 1 and chemerin receptor 2 can be abbreviated to Chemerin1 and Chemerin2, respectively. Chemerin requires C-terminal processing for activity, and human chemerin21–157 is reported to be the most active form, with peptide fragments derived from the C terminus biologically active at both receptors. Small-molecule antagonist, CCX832, selectively blocks CMKLR1, and resolvin E1 activation of CMKLR1 is discussed. Activation of both receptors by chemerin is via coupling to Gi/o, causing inhibition of adenylyl cyclase and increased Ca2+ flux. Receptors and ligand are widely expressed in humans, rats, and mice, and both receptors share ∼80% identity across these species. CMKLR1 knockout mice highlight the role of this receptor in inflammation and obesity, and similarly, GPR1 knockout mice exhibit glucose intolerance. In addition, the chemerin receptors have been implicated in cardiovascular disease, cancer, steroidogenesis, human immunodeficiency virus replication, and neurogenerative disease.
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DOI：
10.1084/jem.20080129
发表时间：
2009-01-16
期刊：
The Journal of experimental medicine
影响因子：
--
作者：
Albanesi C;Scarponi C;Pallotta S;Daniele R;Bosisio D;Madonna S;Fortugno P;Gonzalvo-Feo S;Franssen JD;Parmentier M;De Pità O;Girolomoni G;Sozzani S
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影响因子：
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影响因子：
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作者：
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影响因子：
4.4
作者：
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DOI：
10.1073/pnas.0710487105
发表时间：
2008-01-08
影响因子：
11.1
作者：
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