Sphingosine-1-Phosphate and Its Receptors: Structure, Signaling, and Influence

Novel Selective Allosteric and Bitopic Ligands for the S1P3 Receptor

(2012) Euijung Jo et al.   ACS Chemical Biology

Sphingosine-1-Phosphate and Lymphocyte Egress from Lymphoid Organs

(2012) Jason G. Cyster et al.   Annual Review of Immunology

Impact of Fingolimod Therapy on Magnetic Resonance Imaging Outcomes in Patients With Multiple Sclerosis

(2012) Ernst-Wilhelm Radue   ARCHIVES OF NEUROLOGY

Insights into the activation mechanism of the visual receptor rhodopsin

(2012) Steven O. Smith   BIOCHEMICAL SOCIETY TRANSACTIONS

Dose titration of BAF312 attenuates the initial heart rate reducing effect in healthy subjects

(2012) Eric Legangneux et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

A Potent and Selective S1P1 Antagonist with Efficacy in Experimental Autoimmune Encephalomyelitis

(2012) Jean Quancard et al.   CHEMISTRY & BIOLOGY

Structure-Based Design in the GPCR Target Space

(2012) M. Kontoyianni et al.   CURRENT MEDICINAL CHEMISTRY

Action of Molecular Switches in GPCRs - Theoretical and Experimental Studies

(2012) B. Trzaskowski et al.   CURRENT MEDICINAL CHEMISTRY

Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators

(2012) Ralf Mueller et al.   JOURNAL OF MOLECULAR MODELING

Constitutively active mutant gives novel insights into the mechanism of bitter taste receptor activation

(2012) Sai Prasad Pydi et al.   JOURNAL OF NEUROCHEMISTRY

Relapse and disability outcomes in patients with multiple sclerosis treated with fingolimod: subgroup analyses of the double-blind, randomised, placebo-controlled FREEDOMS study

(2012) Virginia Devonshire et al.   LANCET NEUROLOGY

Into the Eye of the Cytokine Storm

(2012) J. R. Tisoncik et al.   MICROBIOLOGY AND MOLECULAR BIOLOGY REVIEWS

Structure of the human κ-opioid receptor in complex with JDTic

(2012) Huixian Wu et al.   NATURE

Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic

(2012) Aaron A. Thompson et al.   NATURE

A new era of GPCR structural and chemical biology

(2012) Sébastien Granier et al.   Nature Chemical Biology

Functional selectivity induced by mGlu4 receptor positive allosteric modulation and concomitant activation of Gq coupled receptors

(2012) Shen Yin et al.   NEUROPHARMACOLOGY

Crystal Structure of a Lipid G Protein-Coupled Receptor

(2012) M. A. Hanson et al.   SCIENCE

Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions

(2012) W. Liu et al.   SCIENCE

Fusion Partner Toolchest for the Stabilization and Crystallization of G Protein-Coupled Receptors

(2012) Eugene Chun et al.   STRUCTURE

Ligand-Dependent Conformations and Dynamics of the Serotonin 5-HT2A Receptor Determine Its Activation and Membrane-Driven Oligomerization Properties

(2012) Jufang Shan et al.   PLoS Computational Biology

Human Cannabinoid 1 GPCR C-Terminal Domain Interacts with Bilayer Phospholipids to Modulate the Structure of its Membrane Environment

(2011) Elvis K. Tiburu et al.   AAPS Journal

The Best of Both Worlds? Bitopic Orthosteric/Allosteric Ligands of G Protein–Coupled Receptors

(2011) Celine Valant et al.   Annual Review of Pharmacology and Toxicology

“Molecular Switches” on mGluR Allosteric Ligands That Modulate Modes of Pharmacology

(2011) Michael R. Wood et al.   BIOCHEMISTRY

Discovery, design and synthesis of the first reported potent and selective sphingosine-1-phosphate 4 (S1P4) receptor antagonists

(2011) Miguel Guerrero et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

SAR analysis of innovative selective small molecule antagonists of sphingosine-1-phosphate 4 (S1P4) receptor

(2011) Mariangela Urbano et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold

(2011) Richard Williams et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery, synthesis and SAR analysis of novel selective small molecule S1P4-R agonists based on a (2Z,5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype

(2011) Mariangela Urbano et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery, design and synthesis of novel potent and selective sphingosine-1-phosphate 4 receptor (S1P4-R) agonists

(2011) Miguel Guerrero et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Endocannabinoid tone versus constitutive activity of cannabinoid receptors

(2011) Allyn C. Howlett et al.   BRITISH JOURNAL OF PHARMACOLOGY

Insights into the pharmacological relevance of lysophospholipid receptors

(2011) Tetsuji Mutoh et al.   BRITISH JOURNAL OF PHARMACOLOGY

A New Shield for a Cytokine Storm

(2011) Akiko Iwasaki et al.   CELL

Endothelial Cells Are Central Orchestrators of Cytokine Amplification during Influenza Virus Infection

(2011) John R. Teijaro et al.   CELL

Dissecting the Conserved NPxxY Motif of the M3 Muscarinic Acetylcholine Receptor: Critical Role of Asp-7.49 for Receptor Signaling and Multiprotein Complex Formation

(2011) Dasiel O. Borroto-Escuela et al.   CELLULAR PHYSIOLOGY AND BIOCHEMISTRY

Development of an Automated High Throughput LCP-FRAP Assay to Guide Membrane Protein Crystallization in Lipid Mesophases

(2011) Fei Xu et al.   CRYSTAL GROWTH & DESIGN

Immunomodulatory therapy for severe influenza

(2011) Ilyse Darwish et al.   Expert Review of Anti-Infective Therapy

Quelling the storm: utilization of sphingosine-1-phosphate receptor signaling to ameliorate influenza virus-induced cytokine storm

(2011) Kevin B. Walsh et al.   IMMUNOLOGIC RESEARCH

The sphingosine-1-phosphate receptor-1 antagonist, W146, causes early and short-lasting peripheral blood lymphopenia in mice

(2011) Gema Tarrasón et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

FTY720 (Gilenya) Phosphate Selectivity of Sphingosine 1-Phosphate Receptor Subtype 1 (S1P1) G Protein-coupled Receptor Requires Motifs in Intracellular Loop 1 and Transmembrane Domain 2

(2011) William J. Valentine et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Engagement of S1P1-degradative mechanisms leads to vascular leak in mice

(2011) Myat Lin Oo et al.   JOURNAL OF CLINICAL INVESTIGATION

Amelioration of Collagen-Induced Arthritis by a Novel S1P1 Antagonist with Immunomodulatory Activities

(2011) Y. Fujii et al.   JOURNAL OF IMMUNOLOGY

Evaluation of Molecular Modeling of Agonist Binding in Light of the Crystallographic Structure of an Agonist-Bound A2A Adenosine Receptor

(2011) Francesca Deflorian et al.   JOURNAL OF MEDICINAL CHEMISTRY

Allosteric Modulation of Seven Transmembrane Spanning Receptors: Theory, Practice, and Opportunities for Central Nervous System Drug Discovery

(2011) Bruce J. Melancon et al.   JOURNAL OF MEDICINAL CHEMISTRY

Comparison of fingolimod with interferon beta-1a in relapsing-remitting multiple sclerosis: a randomised extension of the TRANSFORMS study

(2011) Bhupendra Khatri et al.   LANCET NEUROLOGY

Structure of a nanobody-stabilized active state of the β2 adrenoceptor

(2011) Søren G. F. Rasmussen et al.   NATURE

Crystal structure of the β2 adrenergic receptor–Gs protein complex

(2011) Søren G. F. Rasmussen et al.   NATURE

Actions of a picomolar short-acting S1P1 agonist in S1P1-eGFP knock-in mice

(2011) Stuart M Cahalan et al.   Nature Chemical Biology

Sphingosine 1-phosphate (S1P): Physiology and the effects of S1P receptor modulation

(2011) T. Hla et al.   NEUROLOGY

Suppression of cytokine storm with a sphingosine analog provides protection against pathogenic influenza virus

(2011) K. B. Walsh et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

GRK2-Dependent S1PR1 Desensitization Is Required for Lymphocytes to Overcome Their Attraction to Blood

(2011) T. I. Arnon et al.   SCIENCE

Structure of an Agonist-Bound Human A2A Adenosine Receptor

(2011) F. Xu et al.   SCIENCE

Structure of the Adenosine A2A Receptor in Complex with ZM241385 and the Xanthines XAC and Caffeine

(2011) Andrew S. Doré et al.   STRUCTURE

Status of GPCR Modeling and Docking as Reflected by Community-wide GPCR Dock 2010 Assessment

(2011) Irina Kufareva et al.   STRUCTURE

Allostery in GPCRs: ‘MWC’ revisited

(2011) Meritxell Canals et al.   TRENDS IN BIOCHEMICAL SCIENCES

Sphingosine-1-phosphate signaling and its role in disease

(2011) Michael Maceyka et al.   TRENDS IN CELL BIOLOGY

Diversity and modularity of G protein-coupled receptor structures

(2011) Vsevolod Katritch et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Differential Effects of Allosteric M1 Muscarinic Acetylcholine Receptor Agonists on Receptor Activation, Arrestin 3 Recruitment, and Receptor Downregulation

(2010) Albert A. Davis et al.   ACS Chemical Neuroscience

Structure and Activation of the Visual Pigment Rhodopsin

(2010) Steven O. Smith   Annual Review of Biophysics

Phenotypic interactions of spinster with the genes encoding proteins for cell death control in Drosophila melanogaster

(2010) Akira Sakurai et al.   ARCHIVES OF INSECT BIOCHEMISTRY AND PHYSIOLOGY

Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: Development of a potent and highly selective M1 PAM

(2010) Thomas M. Bridges et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators

(2010) Thomas M. Bridges et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): The development of ML169, an MLPCN probe

(2010) Paul R. Reid et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

(S)-FTY720-Vinylphosphonate, an analogue of the immunosuppressive agent FTY720, is a pan-antagonist of sphingosine 1-phosphate GPCR signaling and inhibits autotaxin activity

(2010) William J. Valentine et al.   CELLULAR SIGNALLING

Cell-surface residence of sphingosine 1-phosphate receptor 1 on lymphocytes determines lymphocyte egress kinetics

(2010) Shobha Thangada et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Influenza Virus–Cytokine‐Protease Cycle in the Pathogenesis of Vascular Hyperpermeability in Severe Influenza

(2010) Siye Wang et al.   JOURNAL OF INFECTIOUS DISEASES

Impact of the DRY Motif and the Missing "Ionic Lock" on Constitutive Activity and G-Protein Coupling of the Human Histamine H4 Receptor

(2010) E. H. Schneider et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Allosteric activators of muscarinic receptors as novel approaches for treatment of CNS disorders

(2010) Gregory J. Digby et al.   Molecular BioSystems

Modulation of Chemokines and Allergic Airway Inflammation by Selective Local Sphingosine-1-phosphate Receptor 1 Agonism in Lungs

(2010) D. Marsolais et al.   MOLECULAR PHARMACOLOGY

An update on sphingosine-1-phosphate and other sphingolipid mediators

(2010) Henrik Fyrst et al.   Nature Chemical Biology

Fingolimod (FTY720): discovery and development of an oral drug to treat multiple sclerosis

(2010) Volker Brinkmann et al.   NATURE REVIEWS DRUG DISCOVERY

A Placebo-Controlled Trial of Oral Fingolimod in Relapsing Multiple Sclerosis

(2010) Ludwig Kappos et al.   NEW ENGLAND JOURNAL OF MEDICINE

FTY720 (fingolimod) efficacy in an animal model of multiple sclerosis requires astrocyte sphingosine 1-phosphate receptor 1 (S1P1) modulation

(2010) J. W. Choi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Three fatal cases of pandemic 2009 influenza A virus infection in Shenzhen are associated with cytokine storm

(2010) Xiao-Wen Cheng et al.   RESPIRATORY PHYSIOLOGY & NEUROBIOLOGY

Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists

(2010) B. Wu et al.   SCIENCE

Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist

(2010) E. Y. T. Chien et al.   SCIENCE

Discovery and Characterization of Novel Subtype-Selective Allosteric Agonists for the Investigation of M1 Receptor Function in the Central Nervous System

(2009) Evan P Lebois et al.   ACS Chemical Neuroscience

Sphingosine 1-Phosphate Receptor Signaling

(2009) Hugh Rosen et al.   Annual Review of Biochemistry

X-ray structure breakthroughs in the GPCR transmembrane region

(2009) Sid Topiol et al.   BIOCHEMICAL PHARMACOLOGY

Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M5 PAM

(2009) Thomas M. Bridges et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Palmitoylation of the sphingosine 1-phosphate receptor S1P1is involved in its signaling functions and internalization

(2009) Yusuke Ohno et al.   GENES TO CELLS

Location of the Retinal Chromophore in the Activated State of Rhodopsin*

(2009) Shivani Ahuja et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Conserved Aromatic Lock for the Tryptophan Rotameric Switch in TM-VI of Seven-transmembrane Receptors

(2009) Birgitte Holst et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Lymphatic endothelial cell sphingosine kinase activity is required for lymphocyte egress and lymphatic patterning

(2009) Trung H.M. Pham et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Persistent signaling induced by FTY720-phosphate is mediated by internalized S1P1 receptors

(2009) Florian Mullershausen et al.   Nature Chemical Biology

Chemical modulators of sphingosine-1-phosphate receptors as barrier-oriented therapeutic molecules

(2009) David Marsolais et al.   NATURE REVIEWS DRUG DISCOVERY

A critical role for the sphingosine analog AAL-R in dampening the cytokine response during influenza virus infection

(2009) D. Marsolais et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Treatment with a sphingosine analog does not alter the outcome of a persistent virus infection

(2009) Kevin B. Walsh et al.   VIROLOGY

Ligand-Binding Pocket Shape Differences between Sphingosine 1-Phosphate (S1P) Receptors S1P1and S1P3Determine Efficiency of Chemical Probe Identification by Ultrahigh-Throughput Screening

(2008) Stephan C. Schürer et al.   ACS Chemical Biology

Sphingosine-1-Phosphate in the Regulation of Vascular Tone

(2008) Bodo Levkau   CIRCULATION RESEARCH

The Spinster Homolog, Two of Hearts, Is Required for Sphingosine 1-Phosphate Signaling in Zebrafish

(2008) Nick Osborne et al.   CURRENT BIOLOGY

S1P1 Receptor Signaling Overrides Retention Mediated by Gαi-Coupled Receptors to Promote T Cell Egress

(2008) Trung H.M. Pham et al.   IMMUNITY

Agonist-Induced Conformational Changes in Bovine Rhodopsin: Insight into Activation of G-Protein-Coupled Receptors

(2008) Supriyo Bhattacharya et al.   JOURNAL OF MOLECULAR BIOLOGY

Full Pharmacological Efficacy of a Novel S1P1 Agonist That Does Not Require S1P-Like Headgroup Interactions

(2008) P. J. Gonzalez-Cabrera et al.   MOLECULAR PHARMACOLOGY

Local Not Systemic Modulation of Dendritic Cell S1P Receptors in Lung Blunts Virus-Specific Immune Responses to Influenza

(2008) D. Marsolais et al.   MOLECULAR PHARMACOLOGY