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Open AccessStructural basis of ligand recognition and design of antihistamines targeting histamine H4 receptor
The histamine H4 receptor (H4R) plays key role in immune cell function and is a highly valued target for treating allergic and inflammatory diseases. However, structural information of H4R remains elusive. Here, ...
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Article
Open AccessIdentification of oleic acid as an endogenous ligand of GPR3
Although GPR3 plays pivotal roles in both the nervous system and metabolic processes, such as cold-induced thermogenesis, its endogenous ligand remains elusive. Here, by combining structural approach (includin...
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Open AccessStructural basis of Sphingosine-1-phosphate transport via human SPNS2
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Structural basis of omega-3 fatty acid receptor FFAR4 activation and G protein coupling selectivity
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Effects of warming and precipitation reduction on physiological characters of dominant psammophytes’ seeds in Horqin sandy land, northeast China
Seeds are generally sensitive to environmental change and the reactive oxygen species (ROS) generated during their development cause oxidative stress leading to oxidative damage in seeds. Therefore, it is esse...
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Article
Open AccessStructural basis of lysophosphatidylserine receptor GPR174 ligand recognition and activation
Lysophosphatidylserine (LysoPS) is a lipid mediator that induces multiple cellular responses through binding to GPR174. Here, we present the cryo-electron microscopy (cryo-EM) structure of LysoPS-bound human G...
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Open AccessStructural basis of adhesion GPCR GPR110 activation by stalk peptide and G-proteins coupling
Adhesion G protein-coupled receptors (aGPCRs) are keys of many physiological events and attractive targets for various diseases. aGPCRs are also known to be capable of self-activation via an autoproteolysis pr...
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Article
Open AccessStructural basis of leukotriene B4 receptor 1 activation
Leukotriene B4 receptor 1 (BLT1) plays crucial roles in the acute inflammatory responses and is a valuable target for anti-inflammation treatment, however, the mechanism by which leukotriene B4 (LTB4) activate...
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Author Correction: Structural basis of sphingosine-1-phosphate receptor 1 activation and biased agonism
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Structural basis of sphingosine-1-phosphate receptor 1 activation and biased agonism
Sphingosine-1-phosphate receptor 1 (S1PR1) is a master regulator of lymphocyte egress from the lymph node and an established drug target for multiple sclerosis (MS). Mechanistically, therapeutic S1PR1 modulato...
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Open AccessCryo-EM structure of the human histamine H1 receptor/Gq complex
Histamine receptors play important roles in various pathophysiological conditions and are effective targets for anti-allergy treatment, however the mechanism of receptor activation remain elusive. Here, we pre...
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Article
Open AccessCrystal structure of heliorhodopsin 48C12
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A complex structure of arrestin-2 bound to a G protein-coupled receptor
Arrestins comprise a family of signal regulators of G-protein-coupled receptors (GPCRs), which include arrestins 1 to 4. While arrestins 1 and 4 are visual arrestins dedicated to rhodopsin, arrestins 2 and 3 (...
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Article
Crystal structure of the Frizzled 4 receptor in a ligand-free state
Frizzled receptors (FZDs) are class-F G-protein-coupled receptors (GPCRs) that function in Wnt signalling and are essential for develo** and adult organisms1,2. As central mediators in this complex signalling p...
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Open AccessGinkgolic acid, a sumoylation inhibitor, promotes adipocyte commitment but suppresses adipocyte terminal differentiation of mouse bone marrow stromal cells
Sumoylation is a post-translational modification process having an important influence in mesenchymal stem cell (MSC) differentiation. Thus, sumoylation-modulating chemicals might be used to control MSC differ...
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Open AccessMolecular assembly of rhodopsin with G protein-coupled receptor kinases
G protein-coupled receptor kinases (GRKs) play pivotal roles in desensitizing GPCR signaling but little is known about how GRKs recognize and phosphorylate GPCRs due to the technical difficulties in detecting ...
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Open AccessX-ray laser diffraction for structure determination of the rhodopsin-arrestin complex
Serial femtosecond X-ray crystallography (SFX) using an X-ray free electron laser (XFEL) is a recent advancement in structural biology for solving crystal structures of challenging membrane proteins, including...
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Erratum: Discovery of a highly potent glucocorticoid for asthma treatment
Correction to: Cell Discovery (2015) 1, 15035; doi:10.1038/celldisc.2015.35; published online 15 December 2015 In the initial published version of this article, an error was made when we drew the chemical stru...
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Open AccessDiscovery of a highly potent glucocorticoid for asthma treatment
Glucocorticoids are the most effective treatment for asthma. However, their clinical applications are limited by low efficacy in severe asthma and by undesired side effects associated with high dose or prolong...
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Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser
G-protein-coupled receptors (GPCRs) signal primarily through G proteins or arrestins. Arrestin binding to GPCRs blocks G protein interaction and redirects signalling to numerous G-protein-independent pathways....