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鸡体内的促黑素细胞激素受体亚型对促肾上腺皮质激素衍生肽具有高度偏好性。

The melanocortin receptor subtypes in chicken have high preference to ACTH-derived peptides.

作者信息

Ling Maria K, Hotta Eri, Kilianova Zuzana, Haitina Tatjana, Ringholm Aneta, Johansson Lisa, Gallo-Payet Nicole, Takeuchi Sakae, Schiöth Helgi B

机构信息

Department of Neuroscience, Uppsala University, BMC, Box 593, 751 24 Uppsala, Sweden.

出版信息

Br J Pharmacol. 2004 Nov;143(5):626-37. doi: 10.1038/sj.bjp.0705900. Epub 2004 Oct 4.

Abstract

1 Melanocortin (MC) receptors are widely distributed throughout the body of chicken, like in mammals, and participate in a wide range of physiological functions. 2 To clarify the pharmacological impact of ligands acting in the MC system, we expressed the chicken MC1, MC2, MC3, MC4 and MC5 (cMC1-5) receptors in eukaryotic cells and performed comprehensive pharmacological characterization of the potency of endogenous and synthetic melanocortin peptides. 3 Remarkably, the cMC receptors displayed high affinity for ACTH-derived peptides and in general low affinity for alpha-MSH. It is evident that not only the cMC2 receptor but also the other cMC receptors interact with ACTH-derived peptide through an epitope beyond the sequence of alpha-MSH. 4 The synthetic ligand MTII was found to be a potent agonist whereas HS024 was a potent antagonist at the cMC4 receptor, indicating that these ligands are suitable for physiological studies in chicken. 5 We also show the presence of prohormone convertase 1 (PC1) and PC2 genes in chicken, and that these peptides are coexpressed with proopiomelanocortin (POMC) in various tissues.

摘要
  1. 黑素皮质素(MC)受体像在哺乳动物中一样广泛分布于鸡的全身,并参与多种生理功能。2. 为了阐明作用于MC系统的配体的药理作用,我们在真核细胞中表达了鸡MC1、MC2、MC3、MC4和MC5(cMC1 - 5)受体,并对内源性和合成黑素皮质素肽的效力进行了全面的药理学表征。3. 值得注意的是,cMC受体对促肾上腺皮质激素衍生的肽表现出高亲和力,而对α - 黑素细胞刺激素一般表现出低亲和力。很明显,不仅cMC2受体,其他cMC受体也通过α - 黑素细胞刺激素序列之外的表位与促肾上腺皮质激素衍生的肽相互作用。4. 发现合成配体MTII是一种强效激动剂,而HS024是cMC4受体的强效拮抗剂,这表明这些配体适用于鸡的生理学研究。5. 我们还表明鸡中存在激素原转化酶1(PC1)和PC2基因,并且这些肽在各种组织中与阿黑皮素原(POMC)共表达。

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1
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