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鲑鱼降钙素活性的构象要求

Conformational requirements for activity of salmon calcitonin.

作者信息

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

出版信息

Endocrinology. 1985 Sep;117(3):801-5. doi: 10.1210/endo-117-3-801.

Abstract

A series of deletion-substitution analogs of salmon calcitonin (SCT) have been prepared containing combinations of a glycine substitution in position 8 and deletions of serine-2 and tyrosine-22. Biological activity of the analogs with respect to native SCT were determined in the rat hypocalcemic assay and by studying stimulation of cAMP formation and competition for binding of 125I-labeled SCT in T47 D human breast cancer cells. It was found that each of the analogs retained full potency, irrespective of the means of assessment. It is suggested that conservation of the alpha-helical region of SCT, along with the overall tertiary structure, are more important for peptide potency than chain length per se.

摘要

已制备了一系列鲑鱼降钙素(SCT)的缺失-取代类似物,其中包含8位甘氨酸取代以及丝氨酸-2和酪氨酸-22缺失的组合。通过大鼠低血钙测定法、研究cAMP形成的刺激作用以及在T47 D人乳腺癌细胞中竞争125I标记的SCT结合,测定了这些类似物相对于天然SCT的生物活性。结果发现,无论评估方式如何,每种类似物都保留了全部效力。有人提出,SCT的α-螺旋区域以及整体三级结构的保守性对肽的效力比链长本身更为重要。

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