Melanin concentrating hormone exhibits both MSH and MCH activities on individual melanophores.
Melanin concentrating hormone exhibits both MSH and MCH activities on individual melanophores.
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黑色素浓缩激素对单个黑色素细胞表现出 MSH 和 MCH 活性。
DOI：
10.1016/0024-3205(87)90041-5
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发表时间：
1987
期刊：
影响因子：
6.1
通讯作者：
Hruby,VJ
中科院分区：
文献类型：
--
作者：
Castrucci,AM;Hadley,ME;Wilkes,BC;Zechel,C;Hruby,VJ
合成了黑色素浓集激素（MCH）的天冬氨酸苏氨酸蛋氨酸精氨酸半胱氨酸蛋氨酸瓦尔甘氨酸精氨酸瓦尔酪氨酸精氨酸脯氨酸半胱氨酸色氨酸谷氨酸瓦尔及其片段类似物（MCH 1 - 14，MCH 5 - 17，MCH 5 - 14），并在一种非常灵敏的鱼皮生物测定法中测定了它们的生物活性。肽的效力等级和最小有效剂量确定为：MCH 1− 17（10− 12 M）>< MCH 5− 17（10 − 12 M）> MCH 1− 14（10− 11 M）> MCH 5− 14（2× 10− 10 M）。MCH的黑素体聚集活性可被100倍浓度的α-MSH完全逆转. MCH以剂量相关的方式被更高浓度的肽自我拮抗，MCH 1− 14片段类似物的活性也是如此。MCH 5− 17和MCH 5− 14类似物的MCH活性甚至不受所用肽的最高浓度的影响。MCH的MSH样活性似乎与肽的N-末端相关，而MCH活性更多地是激素的C-末端的功能。MCH在高浓度下的自我拮抗作用似乎与N-末端四肽有关，这是该激素内在的类FSH活性的原因。
Abstract Asp Thr Met Arg Cys Met Val Gly Arg Val Tyr Arg Pro Cys Trp Glu Val (melanin concentrating hormone, MCH) and several fragment analogs (MCH 1− 14, MCH 5− 17, MCH 5− 14) were synthesized and their biological activities determined in a very sensitive fish skin bioassay. The potency ranking and minimum effective doses of the peptides were determined to be: MCH 1− 17 (10− 12 M)>< MCH 5− 17 (10− 12 M)> MCH 1− 14 (10− 11 M)> MCH 5− 14 (2× 10− 10 M). The melanosome aggregating activity of MCH could be completely reversed by a 100-fold higher concentration of≺-MSH. MCH was self-antagonized in a dose-related manner by higher concentrations of the peptide as was the activity of the MCH 1− 14 fragment analog. The MCH activities of the MCH 5− 17 and MCH 5− 14 analogs were not compromised by even the highest concentrations of the peptides employed. The MSH-like activity of MCH appears to relate to the N-terminus of the peptide whereas MCH activity is more a function of the C-terminus of the hormone. Self-antagonism of MCH at high concentrations appears to relate to the N-terminal tetrapeptide, which is responsible for the intrinsic MSH-like activity of the hormone.