Khalid P, Chaturvedi S, Khan M M, Rastogi A K, Kundu B, Ahmad F, Mathur K B, Kidwai J R
Division of Biochemistry, Central Drug Research Institute, Lucknow, India.
Acta Diabetol Lat. 1989 Jul-Sep;26(3):203-9. doi: 10.1007/BF02581386.
The biologic activities of three synthetic analogues of CCK-4 (Trp-Met-Asp-Phe-NH2) in which (i) the C-terminal residue Phe was N-methylated (peptide I); (ii) the C-terminal Phe residue was N-methylated and Ser is substituted for Met in position 2 (peptide II); (iii) Pro was substituted for Trp in position 1 and the C-terminal amino nitrogen was methylated (peptide III), have been described. Peptides I and II have been found to inhibit the release of both insulin and glucagon, while peptide III was found to be a potent releasing agent for insulin and an inhibitor for glucagon.
已对三种CCK-4(色氨酸-蛋氨酸-天冬氨酸-苯丙氨酸-氨基)合成类似物的生物活性进行了描述,其中:(i)C末端残基苯丙氨酸进行了N-甲基化(肽I);(ii)C末端苯丙氨酸残基进行了N-甲基化,且第2位的蛋氨酸被丝氨酸取代(肽II);(iii)第1位的色氨酸被脯氨酸取代,且C末端氨基氮进行了甲基化(肽III)。已发现肽I和肽II可抑制胰岛素和胰高血糖素的释放,而肽III被发现是胰岛素的强效释放剂和胰高血糖素的抑制剂。