Inhibition of Steroidogenesis in Cultured Leydig Tumor Cells by 22-Amino-23,24-Bisnor-5-Cholen-3β-Ol and (20R)20-Phenyl-5-Pregnene-3β,20-Diol*
- 1 July 1983
- journal article
- research article
- Published by The Endocrine Society in Endocrinology
- Vol. 113 (1) , 127-132
- https://doi.org/10.1210/endo-113-1-127
Abstract
Using the cholesterol side-chain cleavage enzyme purified from bovine adrenals, 22-amino-23,24-bisnor-5-cholen-3-.beta.-ol (22-ABC) and (20R)20-phenyl-5-pregnene-3.beta.,20-diol (20-PPD) are potent competitive inhibitors of this enzyme. The effects of these new inhibitors on steroid production by intact cells were characterized. Using cultured Leydig tumor cells, the effects of 22-ABC, 20-PPD and aminoglutethimide (a well known inhibitor of the cholesterol side-chain cleavage enzyme) on hormone-stimulated steroidogenesis were compared. These compounds inhibit steroid production in a dose-dependent manner and 20-PPD and 22-ABC are about 100 and 4 times more active, respectively, than aminoglutethimide. In these cells, the inhibitory effects of the new compounds seem to be localized exclusively at the conversion of cholesterol to pregnenolone.This publication has 14 references indexed in Scilit:
- Studies on the source of cholesterol used for steroid biosynthesis in cultured Leydig tumor cells.Journal of Biological Chemistry, 1982
- Proximity of the substrate binding site and the heme-iron catalytic site in cytochrome P-450scc.Proceedings of the National Academy of Sciences, 1982
- Desensitization to gonadotropins in cultured Leydig tumor cells involves loss of gonadotropin receptors and decreased capacity for steroidogenesis.Proceedings of the National Academy of Sciences, 1981
- Inhibition of bovine adrenocortical cytochrome P-450scc by 3,3'-dimethoxybenzidineSteroids, 1981
- Characterization of Several Clonal Lines of Cultured Ley dig Tumor Cells: Gonadotropin Receptors and Steroidogenic Responses*Endocrinology, 1981
- Stereoselective Inhibition of Aromatase by Enantiomers of Aminoglutethimide*Endocrinology, 1979
- Enzymatic side chain cleavage of C-20 alkyl and aryl analogs of (20-S)-20-hydroxycholesterol. Implications for the biosynthesis of pregnenoloneJournal of Biological Chemistry, 1979
- Cholesterol side-chain cleavage, cytochrome P450, and the control of steroidogenesisMolecular and Cellular Endocrinology, 1979
- Stereoselective Inhibition of Cholesterol Side Chain Cleavage by Enantiomers of Aminoglutethimide12Endocrinology, 1977
- Inhibition of Adrenal Corticosteroid Synthesis by Aminoglutethimide: Studies of the Mechanism of Action1Journal of Clinical Endocrinology & Metabolism, 1967