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Photoaffinity labeling of gonadotropin releasing hormone receptors in control and desensitized pituitary cells.

Abstract：

:Gonadotropin releasing hormone (GnRH), preincubated with cultured rat pituitary cells, induced down regulation of GnRH receptors in a time- and dose-dependent manner. The specific binding was inhibited by 50% after 30 min and maximal inhibition (70%) was obtained after 75 min preincubation with 1 microM GnRH. Preincubation of the cells for 2 h with 10 nM GnRH inhibited the specific binding by 20%, reaching a plateau of 70% inhibition with 0.1 microM GnRH. Concomitantly, exposure of the cells to GnRH caused a time- and dose-dependent desensitization of LH release. The responsiveness of the desensitized cells was not parallel to the binding capacity and was inhibited to a greater extent (93%). Photoactivation of GnRH receptors with iodinated [azidobenzoyl-D-Lys6]GnRH in control and desensitized cells resulted in the identification of a single specific band with the same apparent molecular weight of 60K daltons. These results indicate that structural alterations of GnRH receptors are not associated with GnRH-induced desensitization. Therefore, desensitization may involve conformational changes in the receptor or more likely a post-receptor mechanism.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Hazum E,Schvartz I

doi

10.1016/0006-291x(84)90572-2

subject

Has Abstract

pub_date

1984-12-14 00:00:00

pages

532-8

issue

2

eissn

0006-291X

issn

1090-2104

pii

0006-291X(84)90572-2

journal_volume

125

pub_type

杂志文章

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