X-ray Crystal Structure of the Novel Enhanced-Affinity Glucocorticoid Agonist Fluticasone Furoate in the Glucocorticoid Receptor−Ligand Binding Domain
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- 作者：Keith Biggadike ; Randy K. Bledsoe ; Anne M. Hassell ; Barrie E. Kirk ; Iain M. McLay ; Lisa M. Shewchuk ; Eugene L. Stewart
- 刊名：Journal of Medicinal Chemistry
- 出版年：2008
- 出版时间：June 26, 2008
- 年：2008
- 卷：51
- 期：12
- 页码：3349 - 3352
- 全文大小：1459K
- 年卷期：v.51,no.12(June 26, 2008)
- ISSN：1520-4804
文摘
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 17α furoate ester to occupy more fully the lipophilic 17α pocket on the receptor, which may account for the enhanced glucocorticoid receptor binding of FF.