MOLECULAR-CLONING OF A NOVEL HUMAN MELANOCORTIN RECEPTOR

MOLECULAR-CLONING OF A NOVEL HUMAN MELANOCORTIN RECEPTOR
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DOI:
10.1006/bbrc.1993.2125
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发表时间:
1993-09-15
影响因子:
3.1
通讯作者:
WIKBERG, JES
WIKBERG, JES
中科院分区:
生物学4区
文献类型:
--
作者:
CHHAJLANI, V;MUCENIECE, R;WIKBERG, JES

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分离命名为MC-2的人基因组克隆。克隆的DNA编码325个氨基酸的蛋白质,其具有7个疏水片段,这是G蛋白偶联受体的特征。MC-2受体在脑组织中表达,但在黑色素瘤细胞中不表达。当MC-2 DNA在COS-7细胞中表达时,它与[125 I]标记的[Nle 4,D-Phe 7]- α黑素细胞刺激素(NDP-MSH)结合,然后可被促黑素肽α-MSH、β-MSH、γ-MSH和促肾上腺皮质激素取代,但不被非促黑素肽β-内啡肽取代。5.18 nM的最高亲和力是针对NDP-MSH肽。我们先前描述的新MG-2受体和MC-1受体(8)显示出对黑皮质素肽的相同的亲和力顺序,但是与先前描述的MG-1受体相比,对黑皮质素肽的亲和力和亲和力的倍数差异是不同的。结果表明,MC-2 DNA编码一种新的黑皮质素受体。
A human genomic clone designated MC-2 is isolated. The cloned DNA codes for a protein of 325 amino acids which possesses seven hydrophobic segments, a characteristic of G-protein coupled receptors. The MC-2 receptor is expressed in brain tissue but not in the melanoma cells. When the MC-2 DNA is expressed in COS-7 cells, it binds [125I]-labelled [Nle4, D-Phe7]- α melanocyte stimulating hormone (NDP-MSH) which then could be displaced by melanotropic peptides α-MSH, β-MSH, γ-MSH and adrenocorticotropic hormone, but not by non-melanotropic peptide β-endorphine. The highest affinity of 5.18 nM was for the NDP-MSH peptide. The novel MG-2 receptor and the MC-1 receptor, described earlier by us (8) showed identical order of affinity for the melanocortin peptides, but the affinities and the fold differences in the affinities to the melanocortin peptides were different when compared to the earlier described MG-1 receptor. The results suggest that the MC-2 DNA codes for a novel melanocortin receptor.