新型非甾体解离型糖皮质激素受体配体的设计与评估
Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands.
作者信息
Shah Nilesh, Scanlan Thomas S
机构信息
Graduate Group in Biophysics, University of California--San Francisco, San Francisco, CA 94143-2280, USA.
出版信息
Bioorg Med Chem Lett. 2004 Oct 18;14(20):5199-203. doi: 10.1016/j.bmcl.2004.07.052.
PMID:15380227
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-kappaB repression from each other.
摘要
一类新型的苯基吡唑稠合的维兰德-米舍尔酮衍生物在体外是糖皮质激素受体（GR）介导转录的高亲和力、受体特异性、选择性调节剂，可使反式激活、AP-1抑制和NF-κB抑制相互解离。
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