MOLECULAR-CLONING AND CHARACTERIZATION OF THE RAT 5TH MELANOCORTIN RECEPTOR
MOLECULAR-CLONING AND CHARACTERIZATION OF THE RAT 5TH MELANOCORTIN RECEPTOR
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DOI：
10.1006/bbrc.1994.1550
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发表时间：
1994-04-29
影响因子：
3.1
通讯作者：
SOKOLOFF, P
中科院分区：
文献类型：
--
作者：
GRIFFON, N;MIGNON, V;SOKOLOFF, P
促肾上腺皮质激素（ACTH）和黑皮质素肽（α、β和γ MSH）在中枢神经系统和外周组织（即肾上腺）中具有许多活性。最近，五黑皮质素受体被克隆和表征。我们在这里报告的克隆，药理学特性和表达的大鼠第五黑皮质素受体（MC 5），从多巴胺D-3受体序列筛选基因组DNA文库。MC 5包含325个氨基酸的序列，与其他黑皮质素受体具有45-62%的同一性，与我们随后克隆的人类对应物具有82%的同一性。后者的序列与所谓的“MC 2”受体的序列相同（Chhajlani等人，1993，生物化学，生物物理学。Res，Comm.195，866-873）。在CHO细胞中稳定表达的MC 5介导cAMP蓄积增加，具有特征药理学：α MSH的效力是NDP α MSH的两倍，是ACTH的10倍，是γ MSH的100倍。在脑中检测到非常低的表达水平，而在肾上腺、胃、肺和脾中发现高水平。此外，br原位杂交研究表明，MC 5表达在肾上腺皮质的三层，主要是在醛固酮产生的肾小球细胞。(C)1994年出版社出版。
Adrenocorticotropic hormone (ACTH) and melanocortin peptides (alpha, beta and gamma MSH) have numerous activities in both central nervous system and peripheral tissues, namely the adrenals. Recently, five melanocortin receptors were cloned and characterized. We report here the cloning, pharmacological characterization and expression of the rat fifth melanocortin receptor (MC5), starting from the dopamine D-3 receptor sequence to screen a genomic DNA library. The MC5 comprises a sequence of 325 aminoacids, displaying 45-62% identity with other melanocortin receptors and 82% identity with its human counterpart that we cloned thereafter. The sequence of the latter is identical to that of a so-called 'MC2' receptor (Chhajlani et al., 1993, Biochem. Biophys. Res, Comm. 195, 866-873). The MC5, stably expressed in CHO cells, mediates increase in cAMP accumulation with a characteristic pharmacology: alpha MSH is twice as potent as NDP alpha MSH, 10 times as ACTH and 100 times as gamma MSH. Very low expression levels were detected in brain, while high levels were found in adrenals, stomach, lung and spleen. In addition, br situ hybridization studies show the MC5 expressed in the three layers of the adrenal cortex,predominantly in the aldosterone-producing zona glomerulosa cells. (C) 1994 Academic Press, Inc.