The human melanocyte stimulating hormone receptor has evolved to become “super-sensitive” to melanocortin peptides

The human melanocyte stimulating hormone receptor has evolved to become “super-sensitive” to melanocortin peptides
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人类黑素细胞刺激激素受体已进化为对黑皮质素肽“超级敏感”

DOI:
10.1016/0303-7207(94)90113-9
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发表时间:
1994
影响因子:
4.1
通讯作者:
K. Mountjoy
K. Mountjoy
中科院分区:
医学2区
文献类型:
--
作者:
K. Mountjoy

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促黑素细胞激素(MSH)通过激活黑素细胞上的特异性细胞表面MSH受体(MC 1-Rs)来刺激哺乳动物的色素沉着。正常人黑素细胞上的MC 1-R一直难以检测和定位。本文报道了克隆的人MC 1-R(hMC 1-R)的药理学特性,并与克隆的小鼠MC 1-R(mMC 1-R)的药理学特性进行了直接比较。人和小鼠MC 1-Rs对α-MSH的超强类似物NDP-MSH同样敏感(EC_(50)= 1-2pM)。与mMCl-R相比,hMCl-R对α-MSH(EC 50 = 2pM)、ACTH(EC 50 = 8 pM)和Lysγ3-MSH(EC 50 < 10− 10 M)也非常敏感。这表明,与啮齿类动物相比,在人类中,ACTH和Lysγ3-MSH可能在色素沉着中具有生理作用。
Melanocyte-stimulating hormone (MSH) stimulates pigmentation in mammals by activating specific cell surface MSH receptors (MC1-Rs) on melanocytes. MC1-Rs on normal human melanocytes have been difficult to detect and characterise. The pharmacological characterisation of a cloned human MC1-R (hMC1-R) is reported here, and directly compared with that of a cloned mouse MC1-R (mMC1-R). The human and mouse MC1-Rs are equally sensitive (EC50= 1–2pM) to the super potent analogue of α-MSH, NDP-MSH. In contrast with the mMCl-R, the hMCl-R is also very sensitive to α-MSH (EC50= 2pM), ACTH (EC50= 8pM), and Lysγ3-MSH (EC50< 10−10M). This suggests that in man, in contrast with rodents, both ACTH and Lysγ3-MSH may have physiological roles in pigmentation.
α-黑素细胞刺激激素-白喉毒素融合蛋白与人黑色素瘤转移中促黑素受体的相互作用。
DOI: --
发表时间: 1992
期刊: Cancer research
影响因子: 11.2
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DOI: 10.1126/science.1325670
发表时间: 1992-08-28
期刊: SCIENCE
影响因子: 56.9
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