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新型增强亲和力糖皮质激素激动剂糠酸氟替卡松在糖皮质激素受体-配体结合域中的X射线晶体结构

X-ray crystal structure of the novel enhanced-affinity glucocorticoid agonist fluticasone furoate in the glucocorticoid receptor-ligand binding domain.

作者信息

Biggadike Keith, Bledsoe Randy K, Hassell Anne M, Kirk Barrie E, McLay Iain M, Shewchuk Lisa M, Stewart Eugene L

出版信息

J Med Chem. 2008 Jun 26;51(12):3349-52. doi: 10.1021/jm800279t. Epub 2008 Jun 4.

DOI:10.1021/jm800279t
PMID:18522385
Abstract

An X-ray crystal structure is reported for the novel enhanced-affinity glucocorticoid agonist fluticasone furoate (FF) in the ligand binding domain of the glucocorticoid receptor. Comparison of this structure with those of dexamethasone and fluticasone propionate shows the 17 alpha furoate ester to occupy more fully the lipophilic 17 alpha pocket on the receptor, which may account for the enhanced glucocorticoid receptor binding of FF.

摘要

报道了新型增强亲和力的糖皮质激素激动剂糠酸氟替卡松（FF）在糖皮质激素受体配体结合域的X射线晶体结构。将该结构与地塞米松和丙酸氟替卡松的结构进行比较，结果显示17α-糠酸酯更充分地占据了受体上的亲脂性17α口袋，这可能是FF与糖皮质激素受体结合增强的原因。

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