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去亮氨酸16鲑鱼降钙素和去苯丙氨酸16人降钙素的生物活性及受体相互作用

Biological activities and receptor interactions of des-Leu16 salmon and des-Phe16 human calcitonin.

作者信息

Findlay D M, Michelangeli V P, Orlowski R C, Martin T J

出版信息

Endocrinology. 1983 Apr;112(4):1288-91. doi: 10.1210/endo-112-4-1288.

Abstract

Analogs of salmon (des-Leu16 sCT) and human (des-Phe16 hCT) calcitonin were prepared in which the amino acid from position 16 was omitted. The biological activities were assessed in vivo in the rat hypocalcemic assay and in vitro by studying competition for binding of [125I]sCT and adenylate cyclase stimulation in human breast cancer cells (T 47D). Deletion from position 16 resulted in substantial loss of biological activity in each system, indicating the importance for a hydrophobic residue at position 16 in the intact calcitonin molecule.

摘要

制备了鲑鱼(去亮氨酸16 降钙素)和人(去苯丙氨酸16 人降钙素)降钙素的类似物,其中第16位的氨基酸被省略。通过大鼠低血钙测定法在体内评估其生物活性,并通过研究在人乳腺癌细胞(T 47D)中[125I]降钙素的结合竞争和腺苷酸环化酶刺激在体外评估其生物活性。第16位的缺失导致每个系统中的生物活性大幅丧失,表明完整降钙素分子中第16位的疏水残基很重要。

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