Ziegler R, Cushing A S, Walpole P, Jasensky R D, Morimoto H
Department of Biochemistry and Center for Insect Science, University of Arizona, Tucson 85721, USA.
Peptides. 1998;19(3):481-6. doi: 10.1016/s0196-9781(97)00421-x.
Single amino acid replacement analogs of Manduca adipokinetic hormone (M-AKH) pGlu-Leu-Thr-Phe-Thr-Ser-Ser-Trp-GlyNH2 were tested for activity in bioassays as well as receptor binding assays. Amino acids were replaced by Ala and by D-analogs. In addition an extended M-AKH and analogs containing photo affinity labels were tested. All analogs had reduced activity. All the peptides which had enough activity to allow a full dose response curve reached the same maximal activity as native M-AKH. The use of analogs, in which L-Phe4 was replaced by Ala or by D-Phe and of L-Thr3 replaced by D-Thr, as competitors led to improved binding of M-AKH in our competitive receptor binding assay. In the bioassay an inactive concentration of Ala4 M-AKH increased the activity of a half optimal concentration of native M-AKH.
对烟草天蛾脂肪动激素（M-AKH）pGlu-Leu-Thr-Phe-Thr-Ser-Ser-Trp-GlyNH2的单氨基酸替换类似物进行了生物测定和受体结合测定的活性测试。氨基酸被丙氨酸和D-类似物取代。此外，还测试了一种延长的M-AKH和含有光亲和标记的类似物。所有类似物的活性均降低。所有具有足够活性以绘制完整剂量反应曲线的肽达到与天然M-AKH相同的最大活性。在我们的竞争性受体结合测定中，使用L-Phe4被丙氨酸或D-苯丙氨酸取代以及L-Thr3被D-苏氨酸取代的类似物作为竞争者导致M-AKH的结合得到改善。在生物测定中，无活性浓度的Ala4 M-AKH增加了天然M-AKH半最佳浓度的活性。
