β-内啡肽：羧基末端修饰的类似物的合成及其活性增强
beta-Endorphin: synthesis of analogs modified at the carboxyl terminus with increased activites.
作者信息
Li C H, Yamashiro D, Tseng L F, Chang W C, Ferrara P
出版信息
Proc Natl Acad Sci U S A. 1979 Jul;76(7):3276-8. doi: 10.1073/pnas.76.7.3276.
Abstract
Three analogs of human beta-endorphin (beta h-EP) have been synthesized: [Gly31]beta h-EP, [Gly31]beta h-endorphinamide, and [Gly31]beta h-endorphinylglycine. All are more active than beta h-EP in both the guinea pig ileum bioassay and the opiate receptor binding assay. The last two analogs are about twice as active as beta h-EP in an assay for analgesia. Modification at position 31 and extension at the COOH terminus may afford a route toward analogs with even greater biological activity.
摘要
已合成了三种人β-内啡肽（βh-EP）类似物：[甘氨酸31]βh-EP、[甘氨酸31]βh-内啡肽酰胺和[甘氨酸31]βh-内啡肽基甘氨酸。在豚鼠回肠生物测定和阿片受体结合测定中，所有这些类似物的活性均高于βh-EP。在镇痛测定中，后两种类似物的活性约为βh-EP的两倍。31位的修饰和COOH末端的延伸可能为获得具有更高生物活性的类似物提供一条途径。
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本文引用的文献
1
The effects of adrenaline, noradrenaline and isoprenaline on inhibitory alpha- and beta-adrenoceptors in the longitudinal muscle of the guinea-pig ileum.肾上腺素、去甲肾上腺素和异丙肾上腺素对豚鼠回肠纵肌中抑制性α和β肾上腺素能受体的作用。
Br J Pharmacol. 1970 Jun;39(2):398-413. doi: 10.1111/j.1476-5381.1970.tb12903.x.
2
Isolation and amino-acid sequence of beta-LPH from sheep pituitary glands.从绵羊脑垂体中分离β-促脂解素及其氨基酸序列
Nature. 1965 Dec 11;208(5015):1093-4. doi: 10.1038/2081093b0.
3
Primary structure of human beta-lipotropin.
Nature. 1976 Apr 15;260(5552):622-4. doi: 10.1038/260622a0.
4
Identification of two related pentapeptides from the brain with potent opiate agonist activity.从大脑中鉴定出两种具有强效阿片激动剂活性的相关五肽。
Nature. 1975 Dec 18;258(5536):577-80. doi: 10.1038/258577a0.
5
Morphinomimetic activity of synthetic fragments of beta-lipotropin and analogs.β-促脂素合成片段及类似物的拟吗啡活性
Proc Natl Acad Sci U S A. 1976 Sep;73(9):3308-10. doi: 10.1073/pnas.73.9.3308.
6
Beta-Endorphin as a potent analgesic by intravenous injection.β-内啡肽通过静脉注射可作为一种强效镇痛药。
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7
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Biochem Biophys Res Commun. 1977 Oct 10;78(3):1124-9. doi: 10.1016/0006-291x(77)90537-x.
8
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9
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FEBS Lett. 1977 Apr 1;76(1):91-2. doi: 10.1016/0014-5793(77)80127-0.
10
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J Med Chem. 1977 Mar;20(3):325-8. doi: 10.1021/jm00213a001.
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