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PMID: 6275834 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

Cyclic nucleotide phosphodiesterase of rat pancreatic islets. Effects of Ca2+, calmodulin and trifluoperazine.

The Biochemical journal ·Vol. 197 ·No. 2 ·1981-08-01 ·Pages 459-64

Sugden MC, Ashcroft SJ

Abstract

Cyclic nucleotide phosphodiesterase activity towards cyclic AMP and cyclic GMP was studied in extracts of rat islets of Langerhans. Biphasic Eadie plots [Eadie (1942) J. Biol. Chem. 146, 85-93] were obtained with either substrate suggesting the presence of both 'high'- and 'low'-Km components. The apparent Km values were 6.2 +/- 0.5 (n = 8) microM and 103.4 +/- 13.5 (6) microM for cyclic AMP and 3.6 +/- 0.3 (12) microM and 61.4 +/- 7.5 (13) microM for cyclic GMP. With cyclic AMP as substrate, phosphodeisterase activity was increased by calmodulin and Ca2+ and decreased by trifluoperazine, a specific inhibitor of calmodulin. With cyclic GMP as substrate, phosphodiesterase activity was decreased by omission of Ca2+ or addition of trifluoperazine. Addition of exogenous calmodulin had no effect on activity. The data suggest that Ca2+ may influence the islet content of cyclic AMP and cyclic GMP via effects on calmodulin-dependent cyclic nucleotide phosphodiesterase(s).

MeSH Terms
2',3'-Cyclic-Nucleotide Phosphodiesterases/antagonists & inhibitors,metabolism Animals Calcium/pharmacology Calcium-Binding Proteins/pharmacology Calmodulin/pharmacology Cyclic AMP/metabolism Cyclic GMP/metabolism Enzyme Activation/drug effects In Vitro Techniques Islets of Langerhans/drug effects,enzymology Kinetics Male Phosphoric Diester Hydrolases/metabolism Rats Rats, Inbred Strains Trifluoperazine/pharmacology
Chemicals
Calcium-Binding Proteins Calmodulin Trifluoperazine Cyclic AMP 2',3'-Cyclic-Nucleotide Phosphodiesterases Phosphoric Diester Hydrolases Cyclic GMP Calcium
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Sugden M C
Ashcroft S J
References (18)
18 references, click to expand
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Article Info
Journal
The Biochemical journal
Abbr.
Biochem J
ISSN
0264-6021
DOI
10.1042/bj1970459
Published
1981-08-01
Pages
459-64
Language
English
Region
England
NLM ID
2984726R
PMCID
PMC1163146
Subset
IM
External Links
PubMed source DOI: 10.1042/bj1970459 PMC Full Text View journal details
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