Targeting proteinase-activated receptors: therapeutic potential and challenges

Kallikrein-Related Peptidase 14 Acts on Proteinase-Activated Receptor 2 to Induce Signaling Pathway in Colon Cancer Cells

(2011) Valérie Gratio et al.   AMERICAN JOURNAL OF PATHOLOGY

Protease-Activated Receptor-2 Modulates Protease-Activated Receptor-1–Driven Neointimal Hyperplasia

(2011) Leila M. Sevigny et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Proteinase-activated receptor-1 mediates dorsal root ganglion neuronal degeneration in HIV/AIDS

(2011) Shaona Acharjee et al.   BRAIN

Preserved arterial vasodilatation via endothelial protease-activated receptor-2 in obese type 2 diabetic mice

(2011) Satomi Kagota et al.   BRITISH JOURNAL OF PHARMACOLOGY

Indirect modulation of neuronal excitability and synaptic transmission in the hippocampus by activation of proteinase-activated receptor-2

(2011) J Gan et al.   BRITISH JOURNAL OF PHARMACOLOGY

Randomized Trial of Atopaxar in the Treatment of Patients With Coronary Artery Disease

(2011) Stephen D. Wiviott et al.   CIRCULATION

Safety and Tolerability of Atopaxar in the Treatment of Patients With Acute Coronary Syndromes

(2011) Michelle L. O'Donoghue et al.   CIRCULATION

PAR1 plays a role in epithelial malignancies: Transcriptional regulation and novel signaling pathway

(2011) Rachel Bar-Shavit et al.   IUBMB LIFE

Adaptor Protein Complex-2 (AP-2) and Epsin-1 Mediate Protease-activated Receptor-1 Internalization via Phosphorylation- and Ubiquitination-dependent Sorting Signals

(2011) Buxin Chen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Neutrophil Elastase Acts as a Biased Agonist for Proteinase-activated Receptor-2 (PAR2)

(2011) Rithwik Ramachandran et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Mucosal Allergic Sensitization to Cockroach Allergens Is Dependent on Proteinase Activity and Proteinase-Activated Receptor-2 Activation

(2011) N. G. Arizmendi et al.   JOURNAL OF IMMUNOLOGY

Expression and Function of the Kallikrein-Related Peptidase 6 in the Human Melanoma Microenvironment

(2011) Stefanie Krenzer et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Structure, function and pathophysiology of protease activated receptors

(2011) Mark N. Adams et al.   PHARMACOLOGY & THERAPEUTICS

Interdicting protease-activated receptor-2-driven inflammation with cell-penetrating pepducins

(2011) L. M. Sevigny et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of an antithrombotic allosteric modulator that acts through helix 8 of PAR1

(2011) L. Dowal et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Distinct Roles of Two GPCRs, MrgprC11 and PAR2, in Itch and Hyperalgesia

(2011) Q. Liu et al.   Science Signaling

Kallikrein-Related Peptidase 4

(2010) Valérie Gratio et al.   AMERICAN JOURNAL OF PATHOLOGY

Apical and basolateral pools of proteinase-activated receptor-2 direct distinct signaling events in the intestinal epithelium

(2010) Chang Lau et al.   AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY

Exploration of a new series of PAR1 antagonists

(2010) Bruno Planty et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Double-blind, placebo-controlled Phase II studies of the protease-activated receptor 1 antagonist E5555 (atopaxar) in Japanese patients with acute coronary syndrome or high-risk coronary artery disease

(2010) S. Goto et al.   EUROPEAN HEART JOURNAL

Contribution of bone marrow-derived cells to the pro-inflammatory effects of protease-activated receptor-2 in colitis

(2010) Eric Hyun et al.   INFLAMMATION RESEARCH

Activation of Protease Activated Receptor 2 by Exogenous Agonist Exacerbates Early Radiation Injury in Rat Intestine

(2010) Junru Wang et al.   INTERNATIONAL JOURNAL OF RADIATION ONCOLOGY BIOLOGY PHYSICS

A Novel Protease-activated Receptor-1 Interactor, Bicaudal D1, Regulates G Protein Signaling and Internalization

(2010) Steven Swift et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Arrestin-2 Differentially Regulates PAR4 and ADP Receptor Signaling in Platelets

(2010) Dongjun Li et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Deficiency of PAR4 Attenuates Cerebral Ischemia/Reperfusion Injury in Mice

(2010) Yingying Mao et al.   JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM

 -Synuclein Activates Microglia by Inducing the Expressions of Matrix Metalloproteinases and the Subsequent Activation of Protease-Activated Receptor-1

(2010) E.-J. Lee et al.   JOURNAL OF IMMUNOLOGY

Novel Agonists and Antagonists for Human Protease Activated Receptor 2

(2010) Grant D. Barry et al.   JOURNAL OF MEDICINAL CHEMISTRY

Current Perspective on the Role of the Thrombin Receptor in Cerebral Vasospasm After Subarachnoid Hemorrhage

(2010) Katsuya Hirano et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

Functional Selectivity and Biased Receptor Signaling

(2010) T. Kenakin   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Protease-Activated Receptor-1 Antagonist F 16618 Reduces Arterial Restenosis by Down-Regulation of Tumor Necrosis Factor   and Matrix Metalloproteinase 7 Expression, Migration, and Proliferation of Vascular Smooth Muscle Cells

(2010) P. Chieng-Yane 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

Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

(2010) T. Kenakin et al.   PHARMACOLOGICAL REVIEWS

Profiling Gene Expression Induced by Protease-Activated Receptor 2 (PAR2) Activation in Human Kidney Cells

(2010) Jacky Y. Suen et al.   PLoS One

Roles and interactions among protease-activated receptors and P2ry12 in hemostasis and thrombosis

(2010) I. Cornelissen et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Evaluation of a novel antiplatelet agent for secondary prevention in patients with a history of atherosclerotic disease: Design and rationale for the Thrombin-Receptor Antagonist in Secondary Prevention of Atherothrombotic Ischemic Events (TRA 2°P)-TIMI 50 trial

(2009) David A. Morrow et al.   AMERICAN HEART JOURNAL

The Thrombin Receptor Antagonist for Clinical Event Reduction in Acute Coronary Syndrome (TRA•CER) trial: study design and rationale

(2009) The TRA•CER Executive and Steering Committees   AMERICAN HEART JOURNAL

Dual effect of the novel peptide antagonist K-14585 on proteinase-activated receptor-2-mediated signalling

(2009) Fui Goon Goh et al.   BRITISH JOURNAL OF PHARMACOLOGY

Novel antagonists for proteinase-activated receptor 2: inhibition of cellular and vascular responsesin vitroandin vivo

(2009) T Kanke et al.   BRITISH JOURNAL OF PHARMACOLOGY

Blockade of PAR1 Signaling with Cell-Penetrating Pepducins Inhibits Akt Survival Pathways in Breast Cancer Cells and Suppresses Tumor Survival and Metastasis

(2009) E. Yang et al.   CANCER RESEARCH

Platelet Matrix Metalloprotease-1 Mediates Thrombogenesis by Activating PAR1 at a Cryptic Ligand Site

(2009) Vishal Trivedi et al.   CELL

Protease-activated receptor 1-dependent neuronal damage involves NMDA receptor function

(2009) Cecily E. Hamill et al.   EXPERIMENTAL NEUROLOGY

Protease-Activated Receptor-1 Down-regulates the Murine Inflammatory and Humoral Response to Helicobacter pylori

(2009) Janet L.K. Wee et al.   GASTROENTEROLOGY

Proteinase activated receptor (PAR) involvement in mediating arthritis pain and inflammation

(2009) F. A. Russell et al.   INFLAMMATION RESEARCH

Endosomal Deubiquitinating Enzymes Control Ubiquitination and Down-regulation of Protease-activated Receptor 2

(2009) Burcu Hasdemir et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Phosphorylation of Protease-activated Receptor-2 Differentially Regulates Desensitization and Internalization

(2009) Tiffany K. Ricks et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of Novel Protease Activated Receptors 1 Antagonists with Potent Antithrombotic Activity in Vivo

(2009) Michel Perez et al.   JOURNAL OF MEDICINAL CHEMISTRY

Safety and tolerability of SCH 530348 in patients undergoing non-urgent percutaneous coronary intervention: a randomised, double-blind, placebo-controlled phase II study

(2009) Richard C Becker et al.   LANCET

Cellular assays as portals to seven-transmembrane receptor-based drug discovery

(2009) Terry P. Kenakin   NATURE REVIEWS DRUG DISCOVERY

A regulatory role for protease-activated receptor-2 in motivational learning in rats

(2009) Rink-Jan Lohman et al.   NEUROBIOLOGY OF LEARNING AND MEMORY

Protease-activated receptors as drug targets in inflammation and pain

(2009) Nathalie Vergnolle   PHARMACOLOGY & THERAPEUTICS

Caveolae are required for protease-selective signaling by protease-activated receptor-1

(2009) A. Russo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Relative Importance of Proteinase-Activated Receptor-1 Versus Matrix Metalloproteinases in Intracerebral Hemorrhage-Mediated Neurotoxicity in Mice

(2009) Mengzhou Xue et al.   STROKE

Increased faecal serine protease activity in diarrhoeic IBS patients: a colonic lumenal factor impairing colonic permeability and sensitivity

(2008) K. Gecse et al.   GUT

Protease-activated receptor-2 activation: a major actor in intestinal inflammation

(2008) E Hyun et al.   GUT

Kallikrein-related Peptidase 4 (KLK4) Initiates Intracellular Signaling via Protease-activated Receptors (PARs)

(2008) Andrew J. Ramsay et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of a Novel, Orally Active Himbacine-Based Thrombin Receptor Antagonist (SCH 530348) with Potent Antiplatelet Activity

(2008) Samuel Chackalamannil et al.   JOURNAL OF MEDICINAL CHEMISTRY

Activated Protein C Promotes Neovascularization and Neurogenesis in Postischemic Brain via Protease-Activated Receptor 1

(2008) M. Thiyagarajan et al.   JOURNAL OF NEUROSCIENCE

Identification and Characterization of Novel Small-Molecule Protease-Activated Receptor 2 Agonists

(2008) L. R. Gardell et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Thrombin Induces Fibroblast CCL2/JE Production and Release via Coupling of PAR1 to Gαq and Cooperation between ERK1/2 and Rho Kinase Signaling Pathways

(2008) Xiaoling Deng et al.   MOLECULAR BIOLOGY OF THE CELL

Protease-activated receptor-2 regulates trypsin expression in the brain and protects against seizures and epileptogenesis

(2008) Rink-Jan Lohman et al.   NEUROBIOLOGY OF DISEASE

EGF receptor transactivation and MAP kinase mediate proteinase-activated receptor-2-induced chloride secretion in intestinal epithelial cells

(2007) Jacques Q. van der Merwe et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

Regulation of GPCRs by Endocytic Membrane Trafficking and Its Potential Implications

(2007) Aylin C. Hanyaloglu et al.   Annual Review of Pharmacology and Toxicology

G Protein–Coupled Receptor Sorting to Endosomes and Lysosomes

(2007) Adriano Marchese et al.   Annual Review of Pharmacology and Toxicology

Synthesis and antiplatelet activity of ethyl 4-(1-benzyl-1H-indazol-3-yl)benzoate (YD-3) derivatives

(2007) Hua-Sin Chen et al.   BIOORGANIC & MEDICINAL CHEMISTRY

β-arrestins and heterotrimeric G-proteins: collaborators and competitors in signal transduction

(2007) K DeFea   BRITISH JOURNAL OF PHARMACOLOGY

Proteinases and signalling: pathophysiological and therapeutic implications via PARs and more

(2007) R Ramachandran et al.   BRITISH JOURNAL OF PHARMACOLOGY