一种源自人αS1酪蛋白的新型阿片肽（酪氨酸-缬氨酸-脯氨酸-苯丙氨酸-脯氨酸）的鉴定（αS1-酪蛋白吗啡样肽及αS1-酪蛋白吗啡样肽酰胺）。
Identification of a novel opioid peptide (Tyr-Val-Pro-Phe-Pro) derived from human alpha S1 casein (alpha S1-casomorphin, and alpha S1-casomorphin amide).
作者信息
Kampa M, Loukas S, Hatzoglou A, Martin P, Martin P M, Castanas E
机构信息
Laboratory of Experimental Endocrinology, University of Crete School of Medicine and University Hospital, Heraklion, Greece.
出版信息
Biochem J. 1996 Nov 1;319 ( Pt 3)(Pt 3):903-8. doi: 10.1042/bj3190903.
Abstract
A new casomorphin pentapeptide (alpha S1-casomorphin) has been isolated from the sequence of human alpha S1-casein [alpha S1-casein-(158-162)], with the sequence Tyr-Val-Pro-Phe-Pro. This peptide was found to bind with high affinity to all three subtypes of the kappa-opioid receptor (kappa 1-kappa 2). When amidated at the C-terminus, alpha S1-casomorphin amide binds to the delta- and kappa 3-opioid sites. Both alpha S1-casomorphin and its amide inhibit in a dose-dependent and reversible manner the proliferation of T47D human breast cancer cells. This anti-proliferative activity was greater for alpha S1-casomorphin, which was the most potent opioid in inhibiting T47D cell proliferation. In T47D breast cancer cells, other casomorphins have been found to bind to somatostatin receptors in addition to opioid sites. In contrast, alpha S1-casomorphin and its amide do not interact with somatostatin receptors in our system.
摘要
一种新的酪蛋白吗啡五肽（αS1-酪蛋白吗啡）已从人αS1-酪蛋白序列[αS1-酪蛋白-(158 - 162)]中分离出来，其序列为Tyr-Val-Pro-Phe-Pro。发现该肽与κ-阿片受体的所有三种亚型（κ1 - κ2）具有高亲和力结合。当在C末端酰胺化时，αS1-酪蛋白吗啡酰胺与δ-和κ3-阿片位点结合。αS1-酪蛋白吗啡及其酰胺均以剂量依赖性和可逆方式抑制T47D人乳腺癌细胞的增殖。对于αS1-酪蛋白吗啡，这种抗增殖活性更强，它是抑制T47D细胞增殖中最有效的阿片类物质。在T47D乳腺癌细胞中，已发现其他酪蛋白吗啡除了与阿片位点结合外，还与生长抑素受体结合。相比之下，在我们的系统中，αS1-酪蛋白吗啡及其酰胺不与生长抑素受体相互作用。
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Identification of a novel opioid peptide (Tyr-Val-Pro-Phe-Pro) derived from human alpha S1 casein (alpha S1-casomorphin, and alpha S1-casomorphin amide).一种源自人αS1酪蛋白的新型阿片肽（酪氨酸-缬氨酸-脯氨酸-苯丙氨酸-脯氨酸）的鉴定（αS1-酪蛋白吗啡样肽及αS1-酪蛋白吗啡样肽酰胺）。
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本文引用的文献
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Antiproliferative and receptor binding properties of alpha- and beta-casomorphins in the T47D human breast cancer cell line.α-和β-酪蛋白吗啡在T47D人乳腺癌细胞系中的抗增殖及受体结合特性
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The antiproliferative effect of opioid receptor agonists on the T47D human breast cancer cell line, is partially mediated through opioid receptors.阿片受体激动剂对T47D人乳腺癌细胞系的抗增殖作用部分是通过阿片受体介导的。
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