CONSTRAINED ANALOGS OF THE CALCITONIN-GENE-RELATED PEPTIDE

被引：13

作者：

HAKALA, JML

VALO, T

VIHAVAINEN, S

HERMONEN, J

HEINO, P

HALME, M

KOSKINEN, AM

机构：

[1] UNIV OULU,DEPT CHEM,SF-90570 OULU,FINLAND

[2] LEIRAS OY,SF-33721 TAMPERE,FINLAND

[3] UNIV TURKU,DEPT PHARMACOL,SF-20520 TURKU,FINLAND

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1994年 / 202卷 / 01期

关键词：

D O I：

10.1006/bbrc.1994.1956

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The calcitonin gene-related peptide, CGRP, has potential medicinal use for instance as a vasodilator or in the regulation of bone metabolism. In this study new analogues of CGRP based on molecular modelling of active fragments were synthesised and tested. The analogues were found to have affinities for the receptor comparable to those seen for native CGRP. Two analogues were found to be agonists. The analogues give an insight to the bioactive conformation of CGRP as they were constrained by disulphide, bridges. (C) 1994 Academic Press, Inc.

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收藏

页码：497 / 503

页数：7

相关论文

共 14 条

[1] DISULFIDE BOND FORMATION USING THE SILYL CHLORIDE SULFOXIDE SYSTEM FOR THE SYNTHESIS OF A CYSTINE PEPTIDE [J].

AKAJI, K ;

TATSUMI, T ;

YOSHIDA, M ;

KIMURA, T ;

FUJIWARA, Y ;

KISO, Y .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1992, 114 (11) :4137-4143

[2] ALTERNATIVE RNA PROCESSING IN CALCITONIN GENE-EXPRESSION GENERATES MESSENGER-RNAS ENCODING DIFFERENT POLYPEPTIDE PRODUCTS [J].

AMARA, SG ;

JONAS, V ;

ROSENFELD, MG ;

ONG, ES ;

EVANS, RM .

NATURE, 1982, 298 (5871) :240-244

[3]

Atherton E, 1989, SOLID PHASE PEPTIDE

[4] HUMAN SYNTHETIC CALCITONIN GENE-RELATED PEPTIDE INHIBITS BONE-RESORPTION INVITRO [J].

DSOUZA, SM ;

MACINTYRE, I ;

GIRGIS, SI ;

MUNDY, GR .

ENDOCRINOLOGY, 1986, 119 (01) :58-61

[5] SOLID-PHASE PEPTIDE-SYNTHESIS UTILIZING 9-FLUORENYLMETHOXYCARBONYL AMINO-ACIDS [J].

FIELDS, GB ;

NOBLE, RL .

INTERNATIONAL JOURNAL OF PEPTIDE AND PROTEIN RESEARCH, 1990, 35 (03) :161-214

[6] CARDIOVASCULAR ACTION OF CALCITONIN GENE-RELATED PEPTIDE IN HUMANS [J].

GENNARI, C ;

FISCHER, JA .

CALCIFIED TISSUE INTERNATIONAL, 1985, 37 (06) :581-584

[7] BIOLOGICAL-ACTIVITY OF N-TERMINAL FRAGMENTS OF CALCITONIN GENE-RELATED PEPTIDE [J].

MAGGI, CA ;

ROVERO, P ;

GIULIANI, S ;

EVANGELISTA, S ;

REGOLI, D ;

MELI, A .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1990, 179 (1-2) :217-219

[8] ACTIVITIES OF CALCITONIN GENE-RELATED PEPTIDE (CGRP) AND RELATED PEPTIDES AT THE CGRP RECEPTOR [J].

MATON, PN ;

PRADHAN, T ;

ZHOU, ZC ;

GARDNER, JD ;

JENSEN, RT .

PEPTIDES, 1990, 11 (03) :485-489

[9] CONFORMATIONAL CHARACTERIZATION BY CIRCULAR-DICHROISM SPECTROSCOPY OF VARIOUS FRAGMENTS AND ANALOGS OF CALCITONIN-GENE-RELATED PEPTIDE [J].

MIMEAULT, M ;

STPIERRE, S ;

FOURNIER, A .

EUROPEAN JOURNAL OF BIOCHEMISTRY, 1993, 213 (03) :927-934

[10] ISOLATION AND CHARACTERIZATION OF HUMAN CALCITONIN GENE-RELATED PEPTIDE [J].

MORRIS, HR ;

PANICO, M ;

ETIENNE, T ;

TIPPINS, J ;

GIRGIS, SI ;

MACINTYRE, I .

NATURE, 1984, 308 (5961) :746-748