Intercellular Lipid Mediators and GPCR Drug Discovery

Regulation of inflammation by extracellular acidification and proton-sensing GPCRs

(2013) Fumikazu Okajima   CELLULAR SIGNALLING

UDP-glucose enhances outward K+currents necessary for cell differentiation and stimulates cell migration by activating the GPR17 receptor in oligodendrocyte precursors

(2013) Elisabetta Coppi et al.   GLIA

Medium-chain Fatty Acid-sensing Receptor, GPR84, Is a Proinflammatory Receptor

(2013) Masakatsu Suzuki et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Neutrophils Regulate Tissue Neutrophilia in Inflammation via the Oxidant-modified Lipid Lysophosphatidylserine

(2013) S. Courtney Frasch et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

5-Oxo-ETE Receptor Antagonists

(2013) Vivek Gore et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Adhesion-GPCR BAI1 Regulates Synaptogenesis by Controlling the Recruitment of the Par3/Tiam1 Polarity Complex to Synaptic Sites

(2013) J. G. Duman et al.   JOURNAL OF NEUROSCIENCE

Phosphatidylserine receptor BAI1 and apoptotic cells as new promoters of myoblast fusion

(2013) Amelia E. Hochreiter-Hufford et al.   NATURE

Conformational biosensors reveal GPCR signalling from endosomes

(2013) Roshanak Irannejad et al.   NATURE

Sterols and oxysterols in immune cell function

(2013) Nathanael J Spann et al.   NATURE IMMUNOLOGY

The eosinophil chemoattractant 5-oxo-ETE and the OXE receptor

(2013) William S. Powell et al.   PROGRESS IN LIPID RESEARCH

Estrogen receptor GPR30 exerts anxiolytic effects by maintaining the balance between GABAergic and glutamatergic transmission in the basolateral amygdala of ovariectomized mice after stress

(2013) Zhen Tian et al.   PSYCHONEUROENDOCRINOLOGY

Changes of the GPR17 receptor, a new target for neurorepair, in neurons and glial cells in patients with traumatic brain injury

(2013) Heike Franke et al.   Purinergic Signalling

Tools for GPCR drug discovery

(2012) Ru Zhang et al.   ACTA PHARMACOLOGICA SINICA

Sphingosine-1-Phosphate and Lymphocyte Egress from Lymphoid Organs

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

The ligand specificity of the G-protein-coupled receptor GPR34

(2012) Lars Ritscher et al.   BIOCHEMICAL JOURNAL

Lysophosphatidylinositol signalling: New wine from an old bottle

(2012) Roberto Piñeiro et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Lysophospholipids and their receptors in the central nervous system

(2012) Ji Woong Choi et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Current progress in non-Edg family LPA receptor research

(2012) Keisuke Yanagida et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Novel bioactive glycerol-based lysophospholipids: New data – New insight into their function

(2012) Anna Grzelczyk et al.   BIOCHIMIE

The orphan receptor GPR3 modulates the early phases of cocaine reinforcement

(2012) Clara Tourino et al.   BRITISH JOURNAL OF PHARMACOLOGY

FoxO1 Target Gpr17 Activates AgRP Neurons to Regulate Food Intake

(2012) Hongxia Ren et al.   CELL

Fine-Tuning S1P Therapeutics

(2012) Hideru Obinata et al.   CHEMISTRY & BIOLOGY

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

(2012) Jean Quancard et al.   CHEMISTRY & BIOLOGY

Novel Anti-Inflammatory-Pro-Resolving Mediators and Their Receptors

(2012) Charles N. Serhan et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

The therapeutic potential of GPR119 agonists for type 2 diabetes

(2012) Takahide Ohishi et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

GPR34 is a receptor for lysophosphatidylserine with a fatty acid at the sn-2 position

(2012) Hajime Kitamura et al.   JOURNAL OF BIOCHEMISTRY

Sphingosine 1-phosphate acts as an activator for the porcine Gpr3 of constitutively active G protein-coupled receptors

(2012) Bao-le Zhang et al.   Journal of Zhejiang University-SCIENCE B

GPR55 and GPR35 and their relationship to cannabinoid and lysophospholipid receptors

(2012) Pingwei Zhao et al.   LIFE SCIENCES

TGFα shedding assay: an accurate and versatile method for detecting GPCR activation

(2012) Asuka Inoue et al.   NATURE METHODS

The G Protein Coupled Receptor 3 Is Involved in cAMP and cGMP Signaling and Maintenance of Meiotic Arrest in Porcine Oocytes

(2012) Cai-Rong Yang et al.   PLoS One

Emerging roles for lysophosphatidylserine in resolution of inflammation

(2012) S. Courtney Frasch et al.   PROGRESS IN LIPID RESEARCH

Amelioration of dermal fibrosis by genetic deletion or pharmacologic antagonism of lysophosphatidic acid receptor 1 in a mouse model of scleroderma

(2011) Flavia V. Castelino et al.   ARTHRITIS AND RHEUMATISM

Δ9-Tetrahydrocannabinol and N-arachidonyl glycine are full agonists at GPR18 receptors and induce migration in human endometrial HEC-1B cells

(2011) Douglas McHugh et al.   BRITISH JOURNAL OF PHARMACOLOGY

Identification of the Orphan G Protein-coupled Receptor GPR31 as a Receptor for 12-(S)-Hydroxyeicosatetraenoic Acid

(2011) Yande Guo et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

2-Oleoyl Glycerol Is a GPR119 Agonist and Signals GLP-1 Release in Humans

(2011) Katrine B. Hansen et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Emerging roles for the BAI1 protein family in the regulation of phagocytosis, synaptogenesis, neurovasculature, and tumor development

(2011) Sarah M. Cork et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

Oxysterols direct B-cell migration through EBI2

(2011) Changlu Liu et al.   NATURE

Oxysterols direct immune cell migration via EBI2

(2011) Sébastien Hannedouche et al.   NATURE

The G-protein-coupled estrogen receptor GPER in health and disease

(2011) Eric R. Prossnitz et al.   Nature Reviews Endocrinology

GPR3 orphan receptor is involved in neuropathic pain after peripheral nerve injury and regulates morphine-induced antinociception

(2011) Jessica Ruiz-Medina et al.   NEUROPHARMACOLOGY

Brain angiogenesis inhibitor 1 (BAI1) is a pattern recognition receptor that mediates macrophage binding and engulfment of Gram-negative bacteria

(2011) Soumita Das et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Emerging paradigms of β-arrestin-dependent seven transmembrane receptor signaling

(2011) Arun K. Shukla et al.   TRENDS IN BIOCHEMICAL SCIENCES

Targeting GPR120 and other fatty acid-sensing GPCRs ameliorates insulin resistance and inflammatory diseases

(2011) Saswata Talukdar et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

GPR35 is a novel lysophosphatidic acid receptor

(2010) Saori Oka et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

N-arachidonoyl glycine, an abundant endogenous lipid, potently drives directed cellular migration through GPR18, the putative abnormal cannabidiol receptor

(2010) Douglas McHugh et al.   BMC NEUROSCIENCE

Distinct expression and ligand-binding profiles of two constitutively active GPR17 splice variants

(2010) T Benned-Jensen et al.   BRITISH JOURNAL OF PHARMACOLOGY

Agonist activation of the G protein-coupled receptor GPR35 involves transmembrane domain III and is transduced via Gα13 and β-arrestin-2

(2010) Laura Jenkins et al.   BRITISH JOURNAL OF PHARMACOLOGY

Altered Immune Response in Mice Deficient for the G Protein-coupled Receptor GPR34

(2010) Ines Liebscher et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Pharmacokinetic and Pharmacodynamic Characterization of an Oral Lysophosphatidic Acid Type 1 Receptor-Selective Antagonist

(2010) J. S. Swaney et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Teaching old receptors new tricks: biasing seven-transmembrane receptors

(2010) Sudarshan Rajagopal et al.   NATURE REVIEWS DRUG DISCOVERY

IUPHAR-DB: new receptors and tools for easy searching and visualization of pharmacological data

(2010) Joanna L. Sharman et al.   NUCLEIC ACIDS RESEARCH

International Union of Basic and Clinical Pharmacology. LXXVIII. Lysophospholipid Receptor Nomenclature

(2010) J. Chun et al.   PHARMACOLOGICAL REVIEWS

International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid Receptors and Their Ligands: Beyond CB1 and CB2

(2010) R. G. Pertwee et al.   PHARMACOLOGICAL REVIEWS

Quantitative expression profiling of G-protein-coupled receptors (GPCRs) in metastatic melanoma: the constitutively active orphan GPCR GPR18 as novel drug target

(2010) Y. Qin et al.   Pigment Cell & Melanoma Research

Vasculostatin Inhibits Intracranial Glioma Growth and Negatively Regulates In vivo Angiogenesis through a CD36-Dependent Mechanism

(2009) B. Kaur et al.   CANCER RESEARCH

Discovery of Selective Probes and Antagonists for G Protein-Coupled Receptors FPR/FPRL1 and GPR30

(2009) Jeffrey Arterburn et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Lipid G Protein-coupled Receptor Ligand Identification Using β-Arrestin PathHunter™ Assay

(2009) Hong Yin et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Synthesis and Evaluation of Lysophosphatidylserine Analogues as Inducers of Mast Cell Degranulation. Potent Activities of Lysophosphatidylthreonine and Its 2-Deoxy Derivative

(2009) Masazumi Iwashita et al.   JOURNAL OF MEDICINAL CHEMISTRY

N-Oleoyldopamine Enhances Glucose Homeostasis through the Activation of GPR119

(2009) Zhi-Liang Chu et al.   MOLECULAR ENDOCRINOLOGY

GPR3 Receptor, a Novel Actor in the Emotional-Like Responses

(2009) Olga Valverde et al.   PLoS One

The Gs-Linked Receptor GPR3 Inhibits the Proliferation of Cerebellar Granule Cells during Postnatal Development

(2009) Shigeru Tanaka et al.   PLoS One

GPR17 is a negative regulator of the cysteinyl leukotriene 1 receptor response to leukotriene D4

(2009) Akiko Maekawa et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

New intercellular lipid mediators and their GPCRs: An update

(2009) Dong-Soon Im   PROSTAGLANDINS & OTHER LIPID MEDIATORS

Signaling, physiological functions and clinical relevance of the G protein-coupled estrogen receptor GPER

(2009) Eric R. Prossnitz et al.   PROSTAGLANDINS & OTHER LIPID MEDIATORS

G2A and LPC: Regulatory functions in immunity

(2009) Janusz H. Kabarowski   PROSTAGLANDINS & OTHER LIPID MEDIATORS

5-Oxo-ETE and the OXE receptor

(2009) Gail E. Grant et al.   PROSTAGLANDINS & OTHER LIPID MEDIATORS

The Orphan G Protein-Coupled Receptor 3 Modulates Amyloid-Beta Peptide Generation in Neurons

(2009) A. Thathiah et al.   SCIENCE

Bile-acid-activated receptors: targeting TGR5 and farnesoid-X-receptor in lipid and glucose disorders

(2009) Stefano Fiorucci et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Identification of the orphan GPCR, P2Y10 receptor as the sphingosine-1-phosphate and lysophosphatidic acid receptor

(2008) Masanori Murakami et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Meiotic Arrest in Human Oocytes Is Maintained by a Gs Signaling Pathway1

(2008) Andrea DiLuigi et al.   BIOLOGY OF REPRODUCTION

Apoptotic Cell Recognition: Will the Real Phosphatidylserine Receptor(s) Please Stand up?

(2008) Donna L. Bratton et al.   CURRENT BIOLOGY

Constitutively active GPR6 is located in the intracellular compartments

(2008) Shalini Padmanabhan et al.   FEBS LETTERS

The G protein-coupled receptor G2A: Involvement in hepatic lipid metabolism and gallstone formation in mice

(2008) Laura E. Johnson et al.   HEPATOLOGY

Identification of Farnesyl Pyrophosphate andN-Arachidonylglycine as Endogenous Ligands for GPR92

(2008) Da Young Oh et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeting bile-acid signalling for metabolic diseases

(2008) Charles Thomas et al.   NATURE REVIEWS DRUG DISCOVERY

GPR55 is a cannabinoid receptor that increases intracellular calcium and inhibits M current

(2008) J. E. Lauckner et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

G2A as a receptor for oxidized free fatty acids

(2008) Hideru Obinata et al.   PROSTAGLANDINS & OTHER LIPID MEDIATORS

The use of controlled ovarian hyperstimulation (COH) in clinical in vitro fertilization: the role of Georgeanna Seegar Jones

(2007) Howard W. Jones   FERTILITY AND STERILITY