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[几种促甲状腺激素释放激素类似物的比活性比较评估]

[Comparative assessment of the specific activity of several thyrotropin-releasing-hormone analogs].

作者信息

Morozova L G, Smirnova A P, Shvachkin I P, Fedotov V P

出版信息

Biull Eksp Biol Med. 1976 Jun;81(6):745-7.

PMID:821571
Abstract

A study was made of the effect of replacement of the second and third amino acid residues of the thyrotropin-releasing hormone on the manifestation of the specific biological activity assessed by the radioimmune method of determination of the thyrotropic hormone in rats. Replacement of histidine by alanine caused a 100-fold and by phenylalanine - a 10-fold reduction of the activity. Glycine analogue proved to be inactive. The biological activity of TRH analogue (Glu-Phe-Pro CH3) was only 10 times less in comparison with the activity of the standard. The second double modified analogue of this hormone (Glu-Gly-Ser NH2) was incapable of influencing the release of the thyrotropic hormone by the hypophysis.

摘要

研究了促甲状腺激素释放激素第二和第三个氨基酸残基的替换对通过放射免疫法测定大鼠促甲状腺激素所评估的特定生物活性表现的影响。组氨酸被丙氨酸替换导致活性降低100倍,被苯丙氨酸替换导致活性降低10倍。甘氨酸类似物被证明无活性。促甲状腺激素释放激素类似物(Glu-Phe-Pro CH3)的生物活性与标准物活性相比仅低10倍。该激素的第二种双重修饰类似物(Glu-Gly-Ser NH2)无法影响垂体促甲状腺激素的释放。

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