Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors

被引:0
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作者
Jie Yin
Kerim Babaoglu
Chad A Brautigam
Lindsay Clark
Zhenhua Shao
Thomas H Scheuermann
Charles M Harrell
Anthony L Gotter
Anthony J Roecker
Christopher J Winrow
John J Renger
Paul J Coleman
Daniel M Rosenbaum
机构
[1] University of Texas Southwestern Medical Center,Department of Biophysics
[2] Merck Research Laboratories,Department of Structural Chemistry
[3] Merck Research Laboratories,Department of Neuroscience
[4] Merck Research Laboratories,Department of Medicinal Chemistry
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摘要
Human orexin receptors (hOX1R and hOX2R) are GPCRs involved in sleep regulation. Structures of hOX1R bound to a selective antagonist or to a dual antagonist, functional assays and computational analyses reveal the basis for subtype selectivity.
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页码:293 / 299
页数:6
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