Structure-function organization of ACTH: fragment ACTH 11-24--a functionally important site of the hormone molecule

The steroidogenic and lipolytic activities of ACTH fragments (ACTH11-24--I, ACTH11-19--II, ACTH11-16--III and ACTH 17-24--IV) were studied. Fragments I--IV exert a steroidogenic effect in isolated fasciculata rat adrenal cells at concentrations of 1--500 micrograms/ml. The inner activity (alpha) and...

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Published inBiokhimiia (Moscow, Russia) Vol. 47; no. 7; p. 1108
Main Authors Skuin'sh, A A, Ratkevich, M P, Kublis, G G, Porunkevich, E A, Syskov, I V
Format Journal Article
LanguageRussian
Published Russia (Federation) 01.07.1982
Subjects
Adipose Tissue - drug effects
Adipose Tissue - metabolism
Adrenal Glands - drug effects
Adrenal Glands - metabolism
Adrenocorticotropic Hormone - pharmacology
Adrenocorticotropic Hormone - physiology
Animals
Biological Assay
Cosyntropin
Lipolysis - drug effects
Peptide Fragments - pharmacology
Rats
Steroids - biosynthesis
Structure-Activity Relationship
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Summary:The steroidogenic and lipolytic activities of ACTH fragments (ACTH11-24--I, ACTH11-19--II, ACTH11-16--III and ACTH 17-24--IV) were studied. Fragments I--IV exert a steroidogenic effect in isolated fasciculata rat adrenal cells at concentrations of 1--500 micrograms/ml. The inner activity (alpha) and concentration at which a half-maximum effect is achieved (EC50) for fragments I and IV are 0.64+/-0.09 and 0.5--2.0 micrograms/ml, for fragment III--0.49+/-0.07 and 0.7 microgram/ml, respectively. Fragments I--IV have no effect on the lipolysis in isolated rat fat cells. The results obtained are indicative of the functional importance of fragment ACTH11-24 in manifestation of steroidogenic action of ACTH and suggest that the second active site of ACTH is enclosed within this amino acid sequence.
ISSN:0320-9725