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人降钙素的构效关系。III. 肽链缩短或末端修饰的合成类似物的生物活性（作者译）

[Structure-activity relationship of human calcitonin. III. Biological activity of synthetic analogues with shortened or terminally modified peptide chains (author's transl)].

作者信息

Rittel W, Maier R, Brugger M, Kamber B, Riniker B, Sieber P

出版信息

Experientia. 1976 Feb 15;32(2):246-8. doi: 10.1007/BF01937791.

DOI:10.1007/BF01937791
PMID:1269626
Abstract

Assays of 8 synthetic analogues of human calcitonin in rats showed that their hypocalcaemic activity was drastically reduced by deletion of the C-terminal amide group, chain-shortening or opening of the disulphide ring, but unaffected or enhanced by modification of the N-terminal amino group.

摘要

对8种人降钙素合成类似物在大鼠体内进行的分析表明，通过删除C末端酰胺基团、缩短链长或打开二硫键环，它们的降钙活性会大幅降低，但通过修饰N末端氨基，其活性不受影响或有所增强。

相似文献

1
[Structure-activity relationship of human calcitonin. III. Biological activity of synthetic analogues with shortened or terminally modified peptide chains (author's transl)].人降钙素的构效关系。III. 肽链缩短或末端修饰的合成类似物的生物活性（作者译）
Experientia. 1976 Feb 15;32(2):246-8. doi: 10.1007/BF01937791.
2
Analogues of human calcitonin.人降钙素类似物。
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3
Analogues of human calcitonin. IV. Influence of leucine substitutions in positions 12, 16 and 19 on hypocalcaemic activity in the rat.人降钙素类似物。IV. 第12、16和19位亮氨酸替代对大鼠降血钙活性的影响。
Clin Endocrinol (Oxf). 1976;5 Suppl:327S-332S. doi: 10.1111/j.1365-2265.1976.tb03841.x.
4
A novel biologically active eel calcitonin analogue with carboxyl terminal Hse32-amide: carboxyl terminal Pro32-amide in calcitonin is not essential for biological activity.一种具有羧基末端Hse32-酰胺的新型生物活性鳗鱼降钙素类似物：降钙素中的羧基末端Pro32-酰胺对生物活性并非必不可少。
Biochem Mol Biol Int. 1996 Nov;40(5):923-9. doi: 10.1080/15216549600201543.
5
Analogues of human calcitonin. I. Influence of modifications in amino acid positions 29 and 31 on hypocalcaemic activity in the rat.人降钙素类似物。I. 第29位和第31位氨基酸修饰对大鼠降钙活性的影响。
FEBS Lett. 1974 Nov 1;48(1):68-71. doi: 10.1016/0014-5793(74)81064-1.
6
Analogues of human calcitonin. V. Influence of basic amino acids in positions 11, 17 and 24 on hypocalcaemic activity in the rat.人降钙素类似物。V. 第11、17和24位碱性氨基酸对大鼠降血钙活性的影响。
Acta Endocrinol (Copenh). 1977 May;85(1):102-8.
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Deletion sequences of salmon calcitonin that retain the essential biological and conformational features of the intact molecule.保留完整分子基本生物学和构象特征的鲑鱼降钙素缺失序列。
J Med Chem. 1988 Aug;31(8):1595-8. doi: 10.1021/jm00403a019.
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Biologically potent analogues of salmon calcitonin which do not contain an N-terminal disulfide-bridged ring structure.不含N端二硫键桥接环结构的具有生物活性的鲑鱼降钙素类似物。
Eur J Biochem. 1987 Jan 15;162(2):399-402. doi: 10.1111/j.1432-1033.1987.tb10615.x.
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des-Ser2 salmon calcitonin: a biologically potent synthetic analog.去丝氨酸2鲑鱼降钙素：一种具有生物活性的合成类似物。
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N-terminal truncation of salmon calcitonin leads to calcitonin antagonists. Structure activity relationship of N-terminally truncated salmon calcitonin fragments in vitro and in vivo.鲑鱼降钙素的N端截短会产生降钙素拮抗剂。N端截短的鲑鱼降钙素片段在体外和体内的构效关系。
Biochem Biophys Res Commun. 1992 Aug 31;187(1):8-13. doi: 10.1016/s0006-291x(05)81450-0.

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A comparison of the effects of amide and acid groups at the C-terminus on the collision-induced dissociation of deprotonated peptides.比较 C 末端酰胺和羧酸基团对去质子化肽的碰撞诱导解离的影响。
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Conformational transitions and fibrillation mechanism of human calcitonin as studied by high-resolution solid-state 13C NMR.

本文引用的文献

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A biological assay for calcitonin.
J Endocrinol. 1965 Nov;33(3):469-75. doi: 10.1677/joe.0.0330469.
2
[Thyrocalcitonin. IV. The total synthesis of alpha-thyrocalcitonin].[甲状腺降钙素。IV。α-甲状腺降钙素的全合成]
Helv Chim Acta. 1969;52(4):1058-73. doi: 10.1002/hlca.19690520420.
3
[Human calcitonin. Structure of calcitonin M and D].[人降钙素。降钙素M和D的结构]
Helv Chim Acta. 1968;51(8):1900-5. doi: 10.1002/hlca.19680510811.
通过高分辨率固态13C核磁共振研究人降钙素的构象转变和纤维化机制
Protein Sci. 2000 May;9(5):867-77. doi: 10.1110/ps.9.5.867.
4
Pharmacology and therapeutic use of calcitonin.降钙素的药理学与治疗用途。
Drugs. 1981 Apr;21(4):257-72. doi: 10.2165/00003495-198121040-00002.
5
Human calcitonin gene-related peptide possesses weak inhibitory potency of bone resorption in vitro.人降钙素基因相关肽在体外对骨吸收具有较弱的抑制效力。
Calcif Tissue Int. 1986 Jun;38(6):339-41. doi: 10.1007/BF02555747.
6
Peptides from the calcitonin genes: molecular genetics, structure and function.来自降钙素基因的肽：分子遗传学、结构与功能。
Biochem J. 1988 Oct 15;255(2):377-90. doi: 10.1042/bj2550377.
7
Synthesis of eel-calcitonin and (asu1,7)-eel-calcitonin: contribution of the disulfide bond to the hormonal activity.
Experientia. 1976 Sep 15;32(9):1104-6. doi: 10.1007/BF01927568.
8
Characterization of the immunochemical forms of calcitonin released by a medullary thyroid carcinoma in tissue culture.甲状腺髓样癌在组织培养中释放的降钙素免疫化学形式的特征分析。
J Clin Invest. 1978 Feb;61(2):449-58. doi: 10.1172/JCI108956.
9
Calcitonin and calcium ionophores: cyclic AMP responses in cells of a human lymphoid line.
Proc Natl Acad Sci U S A. 1978 Aug;75(8):3984-88. doi: 10.1073/pnas.75.8.3984.
4
[Human calcitonin. VI. Synthesis of calcitonin M].
Helv Chim Acta. 1970;53(8):2135-50. doi: 10.1002/hlca.19700530826.
5
Immunochemical studies on human calcitonin M leading to information on the shape of the molecule.关于人降钙素M的免疫化学研究，以获取有关分子形状的信息。
Biochem J. 1972 Mar;127(1):199-206. doi: 10.1042/bj1270199.