Irreversible anti-glucocorticoids

Details Irreversible anti-glucocorticoids Irreversible anti-glucocorticoids

1980-04-30

1981-10-20

Kepplinger, Esther M.

Chemistry: molecular biology and microbiology

Spore forming or isolating process

424243, C12N 500

Patent

active

042962064

ABSTRACT:
The use of cortisol-21-mesylate and dexamethasone-21-mesylate as inhibitors of glucocorticoid steroid hormone action is disclosed. These compounds were found to be irreversible inhibitors of glucocorticoid action, for example, in both whole and broken rat hepatoma tissue culture cells. The compounds contain both the basic glucocorticoid structure and a reactive functional group capable of yielding a covalent receptor-steroid complex.

REFERENCES:
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Pifferi et al., Chemical Abstracts 90:23407k, 690 (1979).
Gopalakrishnan et al., J. Biol. Chem., 252(8), 2717-2725 (1977).
Simons et al., Biochemistry, 18(22), 4915-4922 (1979).
G. B. Cutler, et al., "11-Deoxycortisol; A. Glucocorticoid Antagonist in Vivo", The Endocrine Society, 104, No. 6, 1839 (1979).
G. G. Rousseau, et al., "17 B -Carboxamide Steroids are a new class of Glucocorticoid Antagonist", Nature, 279, 158-160 (1979).
H. H. Samuels and G. M. Tomkins, Journal of Molecular Biology 52, 57-74 (1970).
G. G. Rousseau, et al., "Glucocorticoid Receptors: Relations between Steriod Binding and Biological Effects", Journal of Molecular Biology, 67, 99-115 (1972).

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