Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands

被引:74
作者
Shah, N
Scanlan, TS [1 ]
机构
[1] Univ Calif San Francisco, Dept Pharmaceut Chem, San Francisco, CA 94143 USA
[2] Univ Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USA
[3] Univ Calif San Francisco, Grad Grp Biophys, San Francisco, CA 94143 USA
关键词
glucocorticoid; nuclear receptor; ligand;
D O I
10.1016/j.bmcl.2004.07.052
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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-kappaB repression from each other. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:5199 / 5203
页数:5
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