Murphy J, Zhang W J, Macaulay W, Fasman G, Merrifield R B
Rockefeller University, New York, New York 10021.
J Biol Chem. 1987 Dec 25;262(36):17304-12.
Six new analogs of glucagon have been synthesized containing replacements at positions 19, 22, and 23. They were designed to study the correlation between predicted conformation in the 19-27 segment of the hormone and the conformation calculated from circular dichroism measurements and the observed activation of adenylate cyclase in the liver membrane. The analogs were [Val19]glucagon, [Val22]glucagon, [Glu23]glucagon, [Val19,Glu23]glucagon, [Glu22,Glu23]glucagon, and [Ala22,Ala23]glucagon. The structures predicted for the 19-27 segment ranged from strongly alpha helical to weakly beta sheet. The observed conformations varied as functions of amino acid composition, solvent, concentration, pH, and temperature but did not correlate well with prediction. There was, however, a correlation between predicted structure and activation of adenylate cyclase in rat liver membranes.
已合成了六种胰高血糖素新类似物,它们在第19、22和23位上有取代。设计这些类似物是为了研究该激素19 - 27片段的预测构象与通过圆二色性测量计算出的构象以及在肝细胞膜中观察到的腺苷酸环化酶激活之间的相关性。这些类似物分别是[缬氨酸19]胰高血糖素、[缬氨酸22]胰高血糖素、[谷氨酸23]胰高血糖素、[缬氨酸19,谷氨酸23]胰高血糖素、[谷氨酸22,谷氨酸23]胰高血糖素和[丙氨酸22,丙氨酸23]胰高血糖素。预测的19 - 27片段结构从强α螺旋到弱β折叠不等。观察到的构象随氨基酸组成、溶剂、浓度、pH值和温度而变化,但与预测结果相关性不佳。然而,在大鼠肝细胞膜中,预测结构与腺苷酸环化酶的激活之间存在相关性。