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Molecular Pharmacology, Vol 13, 948-955, Copyright © 1977 by the American Society for Pharmacology and Experimental Therapeutics

The Relationship between Glucocorticoid Structure and Effects upon Thymocytes

J. P. DAUSSE 1, D. DUVAL 1, P. MEYER 1, J. C. GAIGNAULT 2, C. MARCHANDEAU 2, and J. P. RAYNAUD 2

1 Physiologie et Pharmacologie, INSERM U7, Hôpital Necker, 75015 Paris, France
2 Centre de Recherches Roussel-Uclaf, 93230 Romainville, France

Glucocorticoid hormones inhibit uridine incorporation into ribonucleic acid of thymocytes. The relationship between this effect and the binding to glucocorticoid receptors in mouse thymocytes was studied in parallel. The 27 different steroids examined could be classified as either agonists (e.g., dexamethasone, hydrocortisone, corticosterone), which bind to thymocytes and have an inhibitory effect on uridine incorporation; antagonists (e.g., 6agr, 16agr-dimethylprogesterone, progesterone), which bind to receptors without significant effect on uridine incorporation and which inhibit the biochemical effect of agonists; or inactive steroids (e.g., estradiol, cortisone), which neither bind nor have any effect on uridine incorporation. Combined evaluation in mouse thymocytes thus appears to be a useful tool in screening of steroids for glucocorticoid activity.

Note:
ACKNOWLEDGMENTS The authors thank Mlle E. Goupy for typing the manuscript. They also thank Dr. J. W. Funder for helpful discussions and for critical reading of the manuscript.

Submitted on August 16, 1976
Accepted on April 22, 1977






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