促黑素肽与克隆的人类外周黑素皮质素受体hMC1R的结合及环磷酸腺苷研究
Binding and cAMP studies of melanotropin peptides with the cloned human peripheral melanocortin receptor, hMC1R.
作者信息
Haskell-Luevano C, Miwa H, Dickinson C, Hruby V J, Yamada T, Gantz I
机构信息
Department of Chemistry, University of Arizona, Tucson 85721.
出版信息
Biochem Biophys Res Commun. 1994 Nov 15;204(3):1137-42. doi: 10.1006/bbrc.1994.2581.
Binding and stimulation of cAMP by the melanotropin peptides alpha-MSH (alpha-melanocyte-stimulating hormone) and its superpotent analogues [Nle4, DPhe7]alpha-MSH (MT-I) and Ac-[Nle4,[formula: see text]alpha-MSH4-10-NH2 (MT-II) were undertaken to examine their respective properties on the human peripheral melanocyte melanocortin receptor, hMC1R. alpha-MSH was found to possess a binding IC50 value of 6.5 +/- 0.9 x 10(-9) M and cAMP EC50 value of 2.0 +/- 0.6 x 10(-9) M. MT-I possesses a binding IC50 value of 1.2 +/- 0.3 x 10(-9) M and a cAMP EC50 of 0.5 +/- 0.03 x 10(-9) M. MT-II possesses a binding IC50 of 0.57 +/- 0.08 x 10(-9) M and cAMP EC50 value of 0.20 +/- 0.05 x 10(-9) M.
对促黑素肽α-MSH（α-黑素细胞刺激素）及其超强类似物[Nle4, DPhe7]α-MSH（MT-I）和Ac-[Nle4,[式：见正文]α-MSH4-10-NH2（MT-II）与cAMP的结合及刺激作用进行了研究，以考察它们对人外周黑素细胞黑素皮质素受体hMC1R的各自特性。发现α-MSH的结合IC50值为6.5±0.9×10(-9) M，cAMP EC50值为2.0±0.6×10(-9) M。MT-I的结合IC50值为1.2±0.3×10(-9) M，cAMP EC50为0.5±0.03×10(-9) M。MT-II的结合IC50为0.57±0.08×10(-9) M，cAMP EC50值为0.20±0.05×10(-9) M。
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