| Secretin and VIP-stimulated adenylate cyclase from rat heart. I. General properties and structural requirements for enzyme activation. | |
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MedLine Citation:
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PMID: 7193463 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Membrane adenylate cyclase from rat heart was activated by the two gut peptides secretin and vasoactive intestinal peptide (VIP), glucagon, and the beta-adrenergic drug isoproterenol, in the presence of guanosine 5'-triphosphate (GTP). With all the stimuli tested, the optimal magnesium concentration was 5 mM, i.e. in excess over the 0.5 mM ATP substrate concentration and 0.01 mM GTP used as cofactor. Under these conditions, half-maximal adenylate cyclase activation with glucagon, secretin, and VIP was achieved at concentrations of 0.5, 0.5 and 1.0 microM, respectively. Data obtained with the secretin (7--27) fragment, a secretin antagonist, indicate that secretin and VIP acted on the same binding sites, which differed from glucagon binding sites. Structural requirements for secretin activation of cardiac adenylate cyclase were evaluated by comparing the potency and efficacy of parent peptides and synthetic analogs. The gastric inhibitory peptide GIP was inactive. When using 13 mono-or bi-substituted analogs, it appeared that amino acids in positions 1, 2, 3, 4 and 6 were of major importance while those in position 5 and 11 played a relatively minor role. |
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Authors:
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P Chatelain; P Robberecht; P De Neef; M Deschodt-Lanckman; W König; J Christophe |
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Publication Detail:
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Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S. |
Journal Detail:
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Title: Pflügers Archiv : European journal of physiology Volume: 389 ISSN: 0031-6768 ISO Abbreviation: Pflugers Arch. Publication Date: 1980 Dec |
Date Detail:
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Created Date: 1981-05-28 Completed Date: 1981-05-28 Revised Date: 2007-11-14 |
Medline Journal Info:
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Nlm Unique ID: 0154720 Medline TA: Pflugers Arch Country: GERMANY, WEST |
Other Details:
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Languages: eng Pagination: 21-7 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Adenosine Triphosphate Adenylate Cyclase / metabolism* Animals Dose-Response Relationship, Drug Enzyme Activation Gastrointestinal Hormones / pharmacology* Glucagon / pharmacology Guanosine Triphosphate Isoproterenol / pharmacology Magnesium / pharmacology Male Myocardium / enzymology* Rats Secretin / pharmacology* Structure-Activity Relationship Vasoactive Intestinal Peptide / pharmacology* |
| Grant Support | |
ID/Acronym/Agency:
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R0-IAM-17010/AM/NIADDK NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Gastrointestinal Hormones; 1393-25-5/Secretin; 37221-79-7/Vasoactive Intestinal Peptide; 56-65-5/Adenosine Triphosphate; 7439-95-4/Magnesium; 7683-59-2/Isoproterenol; 86-01-1/Guanosine Triphosphate; 9007-92-5/Glucagon; EC 4.6.1.1/Adenylate Cyclase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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