Literature DB >> 18522385

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

Keith Biggadike1, Randy K Bledsoe, Anne M Hassell, Barrie E Kirk, Iain M McLay, Lisa M Shewchuk, Eugene L Stewart.   

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.

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Year:  2008        PMID： 18522385     DOI： 10.1021/jm800279t

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  30 in total

1.  An analysis of glucocorticoid receptor-mediated gene expression in BEAS-2B human airway epithelial cells identifies distinct, ligand-directed, transcription profiles with implications for asthma therapeutics.

Authors:  T Joshi; M Johnson; R Newton; M Giembycz
Journal:  Br J Pharmacol       Date:  2015-01-08       Impact factor: 8.739

2.  Deciphering modern glucocorticoid cross-pharmacology using ancestral corticosteroid receptors.

Authors:  Jeffrey A Kohn; Kirti Deshpande; Eric A Ortlund
Journal:  J Biol Chem       Date:  2012-03-21       Impact factor: 5.157

3.  Hormone binding and co-regulator binding to the glucocorticoid receptor are allosterically coupled.

Authors:  Samuel J Pfaff; Robert J Fletterick
Journal:  J Biol Chem       Date:  2010-03-24       Impact factor: 5.157

Review 4.  Fluticasone furoate/vilanterol: a review of its use in patients with asthma.

Authors:  Yahiya Y Syed
Journal:  Drugs       Date:  2015-03       Impact factor: 9.546

5.  Structures and mechanism for the design of highly potent glucocorticoids.

Authors:  Yuanzheng He; Wei Yi; Kelly Suino-Powell; X Edward Zhou; W David Tolbert; Xiaobo Tang; Jing Yang; Huaiyu Yang; Jingjing Shi; Li Hou; Hualiang Jiang; Karsten Melcher; H Eric Xu
Journal:  Cell Res       Date:  2014-04-25       Impact factor: 25.617

6.  Discovery of GW870086: a potent anti-inflammatory steroid with a unique pharmacological profile.

Authors:  I J Uings; D Needham; J Matthews; M Haase; R Austin; D Angell; K Leavens; J Holt; K Biggadike; S N Farrow
Journal:  Br J Pharmacol       Date:  2013-07       Impact factor: 8.739

Review 7.  Structural overview of the nuclear receptor superfamily: insights into physiology and therapeutics.

Authors:  Pengxiang Huang; Vikas Chandra; Fraydoon Rastinejad
Journal:  Annu Rev Physiol       Date:  2010       Impact factor: 19.318

8.  The role of the CCR1 receptor in the inflammatory response to tobacco smoke in a mouse model.

Authors:  Per-Ola Onnervik; Maria Lindahl; Naila Svitacheva; Martin Stämpfli; Kerstin Thim; Amir Smailagic; Robert Virtala; John D Taylor
Journal:  Inflamm Res       Date:  2010-04-13       Impact factor: 4.575

9.  Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor.

Authors:  Keith Biggadike; Randy K Bledsoe; Diane M Coe; Tony W J Cooper; David House; Marie A Iannone; Simon J F Macdonald; Kevin P Madauss; Iain M McLay; Tracy J Shipley; Simon J Taylor; Thuy B Tran; Iain J Uings; Victoria Weller; Shawn P Williams
Journal:  Proc Natl Acad Sci U S A       Date:  2009-10-12       Impact factor: 11.205

Review 10.  Understanding nuclear receptor form and function using structural biology.

Authors:  Fraydoon Rastinejad; Pengxiang Huang; Vikas Chandra; Sepideh Khorasanizadeh
Journal:  J Mol Endocrinol       Date:  2013-11-07       Impact factor: 5.098
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