Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands

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Abstract

A novel class of phenylpyrazole fused Wieland–Miescher ketone derivatives are high affinity, receptor specific, selective modulators of glucocorticoid receptor (GR) mediated transcription in vitro, dissociating transactivation, AP-1 repression, and NF-κB repression from each other.

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A novel class of phenylpyrazole fused Wieland–Miescher ketone derivatives are high affinity, receptor specific, selective modulators of glucocorticoid receptor (GR) function.

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Acknowledgements

We are grateful to I. Rogatsky, B. Darimont, and H. Luecke for plasmids. Research support was from the National Institutes of Health (DK 57574).

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