SYNTHESIS OF A FLUORESCENT STEROID DERIVATIVE WITH HIGH AFFINITIES FOR THE GLUCOCORTICOID AND PROGESTERONE RECEPTORS

Authors
TEUTSCH G KLICH M BOUCHOUX F CEREDE E PHILIBERT D
Citation
G. Teutsch et al., SYNTHESIS OF A FLUORESCENT STEROID DERIVATIVE WITH HIGH AFFINITIES FOR THE GLUCOCORTICOID AND PROGESTERONE RECEPTORS, Steroids, 59(1), 1994, pp. 22-26
Citations number
29
Categorie Soggetti
Biology,"Endocrynology & Metabolism
Journal title
Steroids → ACNP
ISSN journal
0039128X
Volume
59
Issue
1
Year of publication
1994
Pages
22 - 26
Database
ISI
SICI code
0039-128X(1994)59:1<22:SOAFSD>2.0.ZU;2-U
Abstract
The synthesis of RU 45196, an 11 beta-substituted 19-norsteroid of the estra-4,9-diene series, incorporating the nitrobenzoxadiazole (NBD) f luorophore, is reported. The highly fluorescent target compound displa yed remarkable affinity for both the progesterone and glucocorticoid r eceptors. The present work demonstrates for the first time that it is indeed possible to design fluorescent steroid conjugates which maintai n very high affinities for their cognate receptors and which are poten tially useful for mechanistic and diagnostic purposes.