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Potentiation of the antagonistic effect of ACTH 11–24 on steroidogenesis by synthesis of covalent dimeric conjugates
Author(s) -
Fauchère Jean-Luc,
Rossier Michel,
Capponi Alessandro,
Vallotton Michel B.
Publication year - 1985
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(85)80794-8
Subject(s) - long term potentiation , covalent bond , chemistry , receptor , conjugate , monomer , potency , stereochemistry , biochemistry , biophysics , in vitro , biology , polymer , mathematical analysis , mathematics , organic chemistry
Covalent dimerization of the adrenocorticotropin fragment ACTH 11–24 increases its antagonistic potency on the ACTH‐induced steroidogenesis in isolated bovine fasciculata/reticularis cells by 3 orders of magnitude when the C‐termini are linked via a 10 Å long spacer. This strong potentiation, probably mediated by cross‐linking of the receptors, was shown to be dependent on the point of attachment of the monomeric fragment to the spacer, thus providing information about the position of the binding site in the hormonal segment and about the distance of the receptors on the cell surface.