Differential structural requirements for the MSH and MCH activities of melanin concentrating hormone.

Differential structural requirements for the MSH and MCH activities of melanin concentrating hormone.
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黑色素浓缩激素的 MSH 和 MCH 活性的不同结构要求。

DOI:
10.1016/0024-3205(87)90231-1
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发表时间:
1987
期刊:
影响因子:
6.1
通讯作者:
Hruby,VJ
Hruby,VJ
中科院分区:
医学2区
文献类型:
--
作者:
Hadley,ME;Zechel,C;Wilkes,BC;Castrucci,AM;Visconti,MA;Pozo-Alonso,M;Hruby,VJ

文献摘要

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摘要黑色素浓缩激素(melanin concentration hormone, MCH)具有黑色素颗粒浓缩和分散(MSH-like)活性。本文合成了MCH的片段类似物,并测定了其致黑活性。在青蛙(Rana pipiens)和蜥蜴(Anolis carolinensis)的皮肤生物测定中,5 - 17和5 - 14片段的MCH(在浓度为10−5 M或更低的情况下)是无活性的,而1-14序列的MCH与MCH相比表现出最小的(约10%)msh样活性,据先前报道,MCH的活性比α-MSH低约600倍。在硬骨鱼(鱼)皮肤生物测定中,mch5 - 17类似物与MCH的活性相当,而1-14类似物的活性是MCH的10-30倍,环n - c端截断类似物mch5 - 14的活性比MCH低约300倍。这些结果表明,在研究的四足动物物种中,n端序列对msh样活性特别关键,而MCH的其他结构区域,特别是c端,与硬骨鱼的MCH活性更相关。
Abstract melanin concentrating hormone (MCH), exhibits both melanin granule concentrating and dispersing (MSH-like) activities. Fragment analogues of MCH were synthesized as described herein and the melanotropic activities of the peptides were determined. In the frog (Rana pipiens) and lizard (Anolis carolinensis) skin bioassays, the 5–17 and 5–14 fragments of MCH were inactive (at concentrations of 10− 5 M or less), whereas the 1–14 sequence exhibited minimal (about 10%) MSH-like activity compared to MCH, which, as reported previously, was about 600 times less active than α-MSH. In the teleost (fish) skin bioassay, the MCH 5–17 analogue was equipotent to MCH, whereas the 1–14 analogue was 10–30 times and the cyclic N-and C-terminal truncated analogue, MCH 5–14, was about 300 times less active than MCH. These results suggest that the N-terminal sequence is particularly critical to MSH-like activity in the tetrapod species studied, whereas other structural regions of MCH, particularly in the C-terminal, are more related to MCH activity in teleosts.