MOLECULAR-CLONING, EXPRESSION, AND CHARACTERIZATION OF A 5TH MELANOCORTIN RECEPTOR

MOLECULAR-CLONING, EXPRESSION, AND CHARACTERIZATION OF A 5TH MELANOCORTIN RECEPTOR
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DOI:
10.1006/bbrc.1994.1580
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发表时间:
1994-05-16
影响因子:
3.1
通讯作者:
YAMADA, T
YAMADA, T
中科院分区:
生物学4区
文献类型:
--
作者:
GANTZ, I;SHIMOTO, Y;YAMADA, T

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我们报告的基因编码的黑皮质素受体家族的新成员的分离。小鼠黑皮质素-5受体(mMC 5 R)对黑皮质素的反应是细胞内环3 ',5'-腺苷酸(cAMP)浓度增加。黑皮质素对mMC 5 R的刺激揭示了效力等级,其中α-黑素细胞刺激激素(α-MSH)> β-黑素细胞刺激激素(β-MSH)>促肾上腺皮质激素(ACTH)> γ-黑素细胞刺激激素(γ-MSH)。进一步的结构-活性研究表明,α-MSH的氨基和羧基末端部分似乎是mMC 5 R活化的关键决定因素,而黑皮质素核心七肽序列缺乏药理学活性。北方印迹分析显示小鼠骨骼肌中有mMC 5 R mRNA的表达。肌肉肺脾和大脑(C)1994年出版社出版。
We report the isolation of a gene encoding a novel member of the family of melanocortin receptors. The mouse melanocortin-5 receptor (mMC5R) responds to melanocortins with an increase in intracellular cyclic 3', 5'-adenosine monophosphate (cAMP) concentrations. Stimulation of the mMC5R by the melanocortins revealed a hierarchy of potency in which alpha-melanocyte stimulating hormone (alpha-MSH) > beta-melanocyte stimulating hormone (beta-MSH) > adrenocorticotropic hormone (ACTH) > gamma-melanocyte stimulating hormone (gamma-MSH). Further structure-activity studies indicated that amino- and carboxyl-terminal portions of alpha-MSH appear to be key determinants in the activation of mMC5R whereas the melanocortin core heptapeptide sequence is devoid of pharmacological activity. Northern blot analysis demonstrated the expression of mMC5R mRNA in mouse skeletal. muscle, lung, spleen, and brain. (C) 1994 Academic Press, Inc.