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

被引：0

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

来源：

Nature Structural & Molecular Biology | 2016年 / 23卷

关键词：

D O I：

暂无

中图分类号：

学科分类号：

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.

引用

页码：293 / 299

页数：6

共 50 条

[41] RESPECTIVE ROLE OF OREXIN-1 AND OREXIN-2 RECEPTORS IN THE EFFECTS OF A DUAL OX1/2R ANTAGONIST ON SLEEP
Dugovic, C.
Yun, S.
Shelton, J.
Bonaventure, P.
Shireman, B.
Lovenberg, T.
SLEEP, 2012, 35 : A32 - A32
[42] Involvement of TRPC3 channels in calcium oscillations mediated by OX1 orexin receptors
Peltonen, Hanna M.
Magga, Johanna M.
Bart, Genevieve
Turunen, Pauli M.
Antikainen, Miia S. H.
Kukkonen, Jyrki P.
Akerman, Karl E.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2009, 385 (03) : 408 - 412
[43] Toward the Development of Bivalent Ligand Probes of Cannabinoid CB1 and Orexin OX1 Receptor Heterodimers
Perrey, David A.
Gilmour, Brian P.
Thomas, Brian F.
Zhang, Yanan
ACS MEDICINAL CHEMISTRY LETTERS, 2014, 5 (06): : 634 - 638
[44] Calcium affects OX1 orexin (hypocretin) receptor responses by modifying both orexin binding and the signal transduction machinery
Putula, Jaana
Pihlajamaa, Tero
Kukkonen, Jyrki P.
BRITISH JOURNAL OF PHARMACOLOGY, 2014, 171 (24) : 5816 - 5828
[45] IP3-independent signalling of OX1 orexin/hypocretin receptors to Ca2+ influx and ERK
Ekholm, Marie E.
Johansson, Lisa
Kukkonen, Jyrki P.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2007, 353 (02) : 475 - 480
[46] Gonadal steroids differentially regulate orexin OX2 receptors in the adrenal gland of male and female rats
Brüggemann, N
Jöhren, O
Dendorfer, A
Dominiak, P
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 2003, 367 : R73 - R73
[47] Autocrine Endocannabinoid Signaling through CB1 Receptors Potentiates OX1 Orexin Receptor Signaling
Jantti, Maria H.
Putula, Jaana
Turunen, Pauli M.
Nasman, Johnny
Reijonen, Sami
Lindqvist, Christer
Kukkonen, Jyrki P.
MOLECULAR PHARMACOLOGY, 2013, 83 (03) : 621 - 632
[48] Characterization of a minimal promoter for human OX2
Chen, ZQ
Marsden, P
Gorczynski, R
FASEB JOURNAL, 2001, 15 (04): : A698 - A698
[49] OX1 orexin receptors activate extracellular signal-regulated kinase in Chinese hamster ovary cells via multiple mechanisms:: The role of Ca2+ influx in OX1 receptor signaling
Ammoun, S
Johansson, L
Ekholm, ME
Holmqvist, T
Danis, AS
Korhonen, L
Sergeeva, OA
Haas, HL
Åkerman, KEO
Kukkonen, JP
MOLECULAR ENDOCRINOLOGY, 2006, 20 (01) : 80 - 99
[50] Kinetic properties of "dual" orexin receptor antagonists at OX1R and OX2R orexin receptors
Callander, Gabrielle E.
Olorunda, Morenike
Monna, Dominique
Schuepbach, Edi
Langenegger, Daniel
Betschart, Claudia
Hintermann, Samuel
Behnke, Dirk
Cotesta, Simona
Fendt, Markus
Laue, Grit
Ofner, Silvio
Briard, Emmanuelle
Gee, Christine E.
Jacobson, Laura H.
Hoyer, Daniel
FRONTIERS IN NEUROSCIENCE, 2013, 7

← 1 2 3 4 5 →