(Q37972789)

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22212680%20AND%20SRC:MED&resulttype=core&format=json

19 January 2020

title

Targeting proteinase-activated receptors: therapeutic potential and challenges (English)

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19 January 2020

1

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19 January 2020

author name string

Farshid Noorbakhsh

series ordinal

2

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19 January 2020

Kathryn Defea

series ordinal

3

1 reference

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19 January 2020

Morley D Hollenberg

series ordinal

4

1 reference

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19 January 2020

publication date

3 January 2012

1 reference

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Nature Reviews Drug Discovery

19 January 2020

published in

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22212680%20AND%20SRC:MED&resulttype=core&format=json

19 January 2020

volume

11

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19 January 2020

page(s)

69-86

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19 January 2020

issue

1

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https://scigraph.springernature.com/pub.10.1038/nrd3615

19 January 2020

exact match

0 references

cites work

The insulin-like action of pepsin and pepsinogen

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ANABOLIC RESPONSES OF DIAPHRAGM MUSCLE TO INSULIN AND TO OTHER PANCREATIC PROTEINS

31 March 2020

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Proteolytic Enzymes Initiating Cell Division and Escape from Contact Inhibition of Growth

31 March 2020

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Release from Density Dependent Growth Inhibition by Proteolytic Enzymes

31 March 2020

1 reference

Mitogenic activity of blood components. I. Thrombin and prothrombin

31 March 2020

1 reference

Transmembrane action of thrombin initiates chick cell division

31 March 2020

1 reference

Initiation of chick cell division by trypsin action at the cell surface

31 March 2020

1 reference

Protease-activated receptors in hemostasis, thrombosis and vascular biology

31 March 2020

1 reference

Structure, function and pathophysiology of protease activated receptors.

31 March 2020

1 reference

Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation

31 March 2020

1 reference

cDNA cloning and expression of a hamster alpha-thrombin receptor coupled to Ca2+ mobilization.

31 March 2020

1 reference

Molecular cloning of a potential proteinase activated receptor

31 March 2020

1 reference

Molecular cloning and functional expression of the gene encoding the human proteinase-activated receptor 2

31 March 2020

1 reference

Protease-activated receptor 3 is a second thrombin receptor in humans

31 March 2020

1 reference

A dual thrombin receptor system for platelet activation

31 March 2020

1 reference

Cloning and characterization of human protease-activated receptor 4

31 March 2020

1 reference

PAR3 is a cofactor for PAR4 activation by thrombin

31 March 2020

1 reference

Protease-activated receptor-3 (PAR3) regulates PAR1 signaling by receptor dimerization

31 March 2020

1 reference

Proteinase-activated receptors: structural requirements for activity, receptor cross-reactivity, and receptor selectivity of receptor-activating peptides

31 March 2020

1 reference

Proteinase-activated receptor-2 (PAR2): vascular effects of a PAR2-derived activating peptide via a receptor different than PAR2.

31 March 2020

1 reference

Proteinase-activated receptor-2 and human lung epithelial cells: disarming by neutrophil serine proteinases.

31 March 2020

1 reference

Neutrophil elastase acts as a biased agonist for proteinase-activated receptor-2 (PAR2)

31 March 2020

1 reference

Teaching old receptors new tricks: biasing seven-transmembrane receptors

31 March 2020

1 reference

Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery

31 March 2020

1 reference

Functional selectivity and biased receptor signaling.

31 March 2020

1 reference

Role of the thrombin receptor's cytoplasmic tail in intracellular trafficking. Distinct determinants for agonist-triggered versus tonic internalization and intracellular localization

31 March 2020

1 reference

Separate signals for agonist-independent and agonist-triggered trafficking of protease-activated receptor 1.

31 March 2020

1 reference

G protein-coupled receptor kinase-5 regulates thrombin-activated signaling in endothelial cells

31 March 2020

1 reference

Ubiquitination differentially regulates clathrin-dependent internalization of protease-activated receptor-1

31 March 2020

1 reference

Clathrin adaptor AP2 regulates thrombin receptor constitutive internalization and endothelial cell resensitization

31 March 2020

1 reference

beta -Arrestins regulate protease-activated receptor-1 desensitization but not internalization or Down-regulation

31 March 2020

1 reference

Adaptor protein complex-2 (AP-2) and epsin-1 mediate protease-activated receptor-1 internalization via phosphorylation- and ubiquitination-dependent sorting signals.

31 March 2020

1 reference

Mechanisms of desensitization and resensitization of proteinase-activated receptor-2.

31 March 2020

1 reference

The role of the C-terminal tail in protease-activated receptor-2-mediated Ca2+ signalling, proline-rich tyrosine kinase-2 activation, and mitogen-activated protein kinase activity.

31 March 2020

1 reference

Phosphorylation of protease-activated receptor-2 differentially regulates desensitization and internalization

31 March 2020

1 reference

Trafficking of proteinase-activated receptor-2 and beta-arrestin-1 tagged with green fluorescent protein. beta-Arrestin-dependent endocytosis of a proteinase receptor

31 March 2020

1 reference

Endosomal deubiquitinating enzymes control ubiquitination and down-regulation of protease-activated receptor 2.

31 March 2020

1 reference

Hepatocyte growth factor-regulated tyrosine kinase substrate (HRS) mediates post-endocytic trafficking of protease-activated receptor 2 and calcitonin receptor-like receptor

31 March 2020

1 reference

Protease-activated receptors 1 and 4 are shut off with distinct kinetics after activation by thrombin

31 March 2020

1 reference

Arrestin-2 differentially regulates PAR4 and ADP receptor signaling in platelets

31 March 2020

1 reference

The mobile receptor hypothesis and “cooperativity” of hormone binding. Application to insulin

31 March 2020

1 reference

The non-stoichiometric floating receptor model for hormone sensitive adenylyl cyclase

31 March 2020

1 reference

Functional Selectivity and Classical Concepts of Quantitative Pharmacology

31 March 2020

1 reference

Functional selectivity of G protein signaling by agonist peptides and thrombin for the protease-activated receptor-1.

31 March 2020

1 reference

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

31 March 2020

1 reference

Modulation of tissue factor-factor VIIa signaling by lipid rafts and caveolae

31 March 2020

1 reference

Atypical protease-activated receptor mediates endothelium-dependent relaxation of human coronary arteries.

31 March 2020

1 reference

Dual endothelium-dependent vascular activities of proteinase-activated receptor-2-activating peptides: evidence for receptor heterogeneity.

31 March 2020

1 reference

Distinct roles for PAR1- and PAR2-mediated vasomotor modulation in human arterial and venous conduits

31 March 2020

1 reference

Increased expression of protease-activated receptor-2 (PAR2) and PAR4 in human coronary artery by inflammatory stimuli unveils endothelium-dependent relaxations to PAR2 and PAR4 agonists

31 March 2020

1 reference

Endothelium-dependent and -independent responses to protease-activated receptor-2 (PAR-2) activation in mouse isolated renal arteries

31 March 2020

1 reference

Vascular actions of thrombin receptor-derived polypeptides: structure-activity profiles for contractile and relaxant effects in rat aorta

31 March 2020

1 reference

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

31 March 2020

1 reference

Blood pressures, heart rate and locomotor activity during salt loading and angiotensin II infusion in protease-activated receptor 2 (PAR2) knockout mice.

31 March 2020

1 reference

Current perspective on the role of the thrombin receptor in cerebral vasospasm after subarachnoid hemorrhage

31 March 2020

1 reference

Novel insights into the delayed vasospasm following subarachnoid haemorrhage: importance of proteinase signalling

31 March 2020

1 reference

Combined argatroban and anti-oxidative agents prevents increased vascular contractility to thrombin and other ligands after subarachnoid haemorrhage

31 March 2020

1 reference

Cloned platelet thrombin receptor is necessary for thrombin-induced platelet activation

31 March 2020

1 reference

An antibody against the exosite of the cloned thrombin receptor inhibits experimental arterial thrombosis in the African green monkey

31 March 2020

1 reference

Protease-activated receptors 1 and 4 mediate activation of human platelets by thrombin

31 March 2020

1 reference

Blocking the protease-activated receptor 1-4 heterodimer in platelet-mediated thrombosis

31 March 2020

1 reference

Biphasic kinetics of activation and signaling for PAR1 and PAR4 thrombin receptors in platelets

31 March 2020

1 reference

Protease-activated receptor-2 modulates protease-activated receptor-1-driven neointimal hyperplasia

31 March 2020

1 reference

Cathepsin G activates protease-activated receptor-4 in human platelets

31 March 2020

1 reference

Evidence for the presence of a protease-activated receptor distinct from the thrombin receptor in human keratinocytes

31 March 2020

1 reference

Proteinase-activated receptors, targets for kallikrein signaling

31 March 2020

1 reference

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

31 March 2020

1 reference

Characterization of the inflammatory response to proteinase-activated receptor-2 (PAR2)-activating peptides in the rat paw.

31 March 2020

1 reference

Pro- and anti-inflammatory actions of thrombin: a distinct role for proteinase-activated receptor-1 (PAR1).

31 March 2020

1 reference

Proteinase-activated receptor-1 agonists attenuate nociception in response to noxious stimuli

31 March 2020

1 reference

Protease-activated receptor-4: a novel mechanism of inflammatory pain modulation

31 March 2020

1 reference

Agonists of proteinase-activated receptor 2 induce inflammation by a neurogenic mechanism

31 March 2020

1 reference

Proteinase-activated receptor-2 and hyperalgesia: A novel pain pathway

31 March 2020

1 reference

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

31 March 2020

1 reference

Essential role for proteinase-activated receptor-2 in arthritis

31 March 2020

1 reference

Therapeutic promise of proteinase-activated receptor-2 antagonism in joint inflammation

31 March 2020

1 reference

Absence of proteinase-activated receptor-1 signaling affords protection from bleomycin-induced lung inflammation and fibrosis

31 March 2020

1 reference

Thrombin is a potent inducer of connective tissue growth factor production via proteolytic activation of protease-activated receptor-1.

31 March 2020

1 reference

Thrombin stimulates fibroblast procollagen production via proteolytic activation of protease-activated receptor 1

31 March 2020

1 reference

Thrombin differentiates normal lung fibroblasts to a myofibroblast phenotype via the proteolytically activated receptor-1 and a protein kinase C-dependent pathway

31 March 2020

1 reference

Activation of endothelial cell protease activated receptor 1 by the protein C pathway

31 March 2020

1 reference

Protease-activated receptor-1 signaling by activated protein C in cytokine-perturbed endothelial cells is distinct from thrombin signaling

31 March 2020

1 reference

Intratracheal administration of activated protein C inhibits bleomycin-induced lung fibrosis in the mouse

31 March 2020

1 reference

Thrombin induces fibroblast CCL2/JE production and release via coupling of PAR1 to Galphaq and cooperation between ERK1/2 and Rho kinase signaling pathways

31 March 2020

1 reference

Proteinase-activated receptor 4 stimulation-induced epithelial-mesenchymal transition in alveolar epithelial cells

31 March 2020

1 reference

Inflammatory mediators modulate thrombin and cathepsin-G signaling in human bronchial fibroblasts by inducing expression of proteinase-activated receptor-4.

31 March 2020

1 reference

Proteinase-activated receptor2 agonists upregulate granulocyte colony-stimulating factor, IL-8, and VCAM-1 expression in human bronchial fibroblasts.

31 March 2020

1 reference

Mast cell tryptase stimulates human lung fibroblast proliferation via protease-activated receptor-2

31 March 2020

1 reference

Protease-activated receptor 2 mediates eosinophil infiltration and hyperreactivity in allergic inflammation of the airway

31 March 2020

1 reference

Proteinase-activated receptor 2 activation in the airways enhances antigen-mediated airway inflammation and airway hyperresponsiveness through different pathways.

31 March 2020

1 reference

Proteinase-activated receptor-2 promotes allergic sensitization to an inhaled antigen through a TNF-mediated pathway

31 March 2020

1 reference

Mucosal allergic sensitization to cockroach allergens is dependent on proteinase activity and proteinase-activated receptor-2 activation

31 March 2020

1 reference

The house dust mite allergen Der p 1, unlike Der p 3, stimulates the expression of interleukin-8 in human airway epithelial cells via a proteinase-activated receptor-2-independent mechanism

31 March 2020

1 reference

Activation of protease-activated receptor (PAR)-1, PAR-2, and PAR-4 stimulates IL-6, IL-8, and prostaglandin E2 release from human respiratory epithelial cells

31 March 2020

1 reference

House dust mite allergens induce proinflammatory cytokines from respiratory epithelial cells: the cysteine protease allergen, Der p 1, activates protease-activated receptor (PAR)-2 and inactivates PAR-1.

31 March 2020

1 reference

Mucosal sensitization to German cockroach involves protease-activated receptor-2.

31 March 2020

1 reference

A protective role for protease-activated receptors in the airways

31 March 2020

1 reference

Protease-activated receptor-2 activating peptide SLIGRL inhibits bacterial lipopolysaccharide-induced recruitment of polymorphonuclear leukocytes into the airways of mice

31 March 2020

1 reference

Clinical relevance of proteinase activated receptors (pars) in the gut

31 March 2020

1 reference

Evidence for the presence of functional protease activated receptor 4 (PAR4) in the rat colon

31 March 2020

1 reference

Activation of proteinase-activated receptor 1 stimulates epithelial chloride secretion through a unique MAP kinase- and cyclo-oxygenase-dependent pathway

31 March 2020

1 reference

Activation of proteinase-activated receptor-1 inhibits neurally evoked chloride secretion in the mouse colon in vitro

31 March 2020

1 reference

Luminal trypsin may regulate enterocytes through proteinase-activated receptor 2.

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

Proteinase-activated receptor 1 activation induces epithelial apoptosis and increases intestinal permeability

31 March 2020

1 reference

Dual effect mediated by protease-activated receptors on the mechanical activity of rat colon

31 March 2020

1 reference

Contractile actions of proteinase-activated receptor-derived polypeptides in guinea-pig gastric and lung parenchymal strips: evidence for distinct receptor systems

31 March 2020

1 reference

Involvement of nitric oxide and tachykinins in the effects induced by protease-activated receptors in rat colon longitudinal muscle

31 March 2020

1 reference

PAR-2 agonists induce contraction of murine small intestine through neurokinin receptors

31 March 2020

1 reference

In vivo evidence that protease-activated receptors 1 and 2 modulate gastrointestinal transit in the mouse

31 March 2020

1 reference

Induction of intestinal inflammation in mouse by activation of proteinase-activated receptor-2

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

A major role for proteolytic activity and proteinase-activated receptor-2 in the pathogenesis of infectious colitis

31 March 2020

1 reference

Protease-activated receptor 2, dipeptidyl peptidase I, and proteases mediate Clostridium difficile toxin A enteritis.

31 March 2020

1 reference

Role for protease activity in visceral pain in irritable bowel syndrome

31 March 2020

1 reference

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

31 March 2020

1 reference

Proteinase-activated receptor-1 is an anti-inflammatory signal for colitis mediated by a type 2 immune response

31 March 2020

1 reference

Proteinase-activated receptor 2 is an anti-inflammatory signal for colonic lamina propria lymphocytes in a mouse model of colitis

31 March 2020

1 reference

Protective effect of proteinase-activated receptor 2 activation on motility impairment and tissue damage induced by intestinal ischemia/reperfusion in rodents

31 March 2020

1 reference

Four different types of protease-activated receptors are widely expressed in the brain and are up-regulated in hippocampus by severe ischemia.

31 March 2020

1 reference

Focal ischemia induces expression of protease-activated receptor1 (PAR1) and PAR3 on microglia and enhances PAR4 labeling in the penumbra

31 March 2020

1 reference

Persistent protease-activated receptor 4 signaling mediates thrombin-induced microglial activation

31 March 2020

1 reference

Four subtypes of protease-activated receptors, co-expressed in rat astrocytes, evoke different physiological signaling

31 March 2020

1 reference

MSP, a trypsin-like serine protease, is abundantly expressed in the human nervous system

31 March 2020

1 reference

Crystal structure and biochemical characterization of human kallikrein 6 reveals that a trypsin-like kallikrein is expressed in the central nervous system

31 March 2020

1 reference

Prothrombin/thrombin and the thrombin receptors PAR-1 and PAR-4 in the brain: localization, expression and participation in neurodegenerative diseases

31 March 2020

1 reference

The role of thrombin-like (serine) proteases in the development, plasticity and pathology of the nervous system

31 March 2020

1 reference

Proteinase-activated receptors in the nervous system

31 March 2020

1 reference

Protease-activated receptors in the brain: receptor expression, activation, and functions in neurodegeneration and neuroprotection

31 March 2020

1 reference

Thrombin receptor activation protects neurons and astrocytes from cell death produced by environmental insults.

31 March 2020

1 reference

Thrombin induces apoptosis in cultured neurons and astrocytes via a pathway requiring tyrosine kinase and RhoA activities.

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

The contribution of protease-activated receptor 1 to neuronal damage caused by transient focal cerebral ischemia

31 March 2020

1 reference

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

31 March 2020

1 reference

Relative importance of proteinase-activated receptor-1 versus matrix metalloproteinases in intracerebral hemorrhage-mediated neurotoxicity in mice.

31 March 2020

1 reference

Up-regulation of proteinase-activated receptor 1 expression in astrocytes during HIV encephalitis

31 March 2020

1 reference

Exacerbation of dopaminergic terminal damage in a mouse model of Parkinson's disease by the G-protein-coupled receptor protease-activated receptor 1.

31 March 2020

1 reference

Alpha-synuclein activates microglia by inducing the expressions of matrix metalloproteinases and the subsequent activation of protease-activated receptor-1.

31 March 2020

1 reference

Activation of protease-activated receptor-1 triggers astrogliosis after brain injury.

31 March 2020

1 reference

Protease-activated receptor-1 protects rat astrocytes from apoptotic cell death via JNK-mediated release of the chemokine GRO/CINC-1.

31 March 2020

1 reference

Activated protein C promotes neovascularization and neurogenesis in postischemic brain via protease-activated receptor 1.

31 March 2020

1 reference

Proteinase-Activated Receptor-2 Induction by Neuroinflammation Prevents Neuronal Death during HIV Infection

31 March 2020

1 reference

Proteinase-activated receptor 2 modulates neuroinflammation in experimental autoimmune encephalomyelitis and multiple sclerosis

31 March 2020

1 reference

Proteinase-activated receptor-2 exerts protective and pathogenic cell type-specific effects in Alzheimer's disease

31 March 2020

1 reference

Deficiency of PAR-2 gene increases acute focal ischemic brain injury.

31 March 2020

1 reference

Deficiency of PAR4 attenuates cerebral ischemia/reperfusion injury in mice

31 March 2020

1 reference

Activated protein C prevents neuronal apoptosis via protease activated receptors 1 and 3

31 March 2020

1 reference

Tumor cell invasion is promoted by activation of protease activated receptor-1 in cooperation with the alpha vbeta 5 integrin

31 March 2020

1 reference

Thrombin receptor overexpression in malignant and physiological invasion processes

31 March 2020

1 reference

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

31 March 2020

1 reference

Trypsins and their role in carcinoma growth

31 March 2020

1 reference

Trypsin in colorectal cancer: molecular biological mechanisms of proliferation, invasion, and metastasis.

31 March 2020

1 reference

Cancer-associated thrombosis

31 March 2020

1 reference

Mechanisms of cancer-induced thrombosis in cancer

31 March 2020

1 reference

Platelet matrix metalloprotease-1 mediates thrombogenesis by activating PAR1 at a cryptic ligand site

31 March 2020

1 reference

PAR1 is a matrix metalloprotease-1 receptor that promotes invasion and tumorigenesis of breast cancer cells.

31 March 2020

1 reference

Identification of a novel functional androgen response element within hPar1 promoter: implications to prostate cancer progression

31 March 2020

1 reference

31 March 2020

1 reference

31 March 2020

1 reference

31 March 2020

1 reference

Expression and function of the kallikrein-related peptidase 6 in the human melanoma microenvironment

31 March 2020

1 reference

Activation of protease activated receptor 2 by exogenous agonist exacerbates early radiation injury in rat intestine

31 March 2020

1 reference

Protease-activated receptors as drug targets in inflammation and pain

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

Thrombin receptor antagonists. Structure-activity relationships for the platelet thrombin receptor and effects on prostacyclin synthesis by human umbilical vein endothelial cells

31 March 2020

1 reference

Identification of small peptide analogues having agonist and antagonist activity at the platelet thrombin receptor

31 March 2020

1 reference

Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor

31 March 2020

1 reference

Discovery of potent peptide-mimetic antagonists for the human thrombin receptor, protease-activated receptor-1 (PAR-1).

31 March 2020

1 reference

Blockade of the thrombin receptor protease-activated receptor-1 with a small-molecule antagonist prevents thrombus formation and vascular occlusion in nonhuman primates.

31 March 2020

1 reference

Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents

31 March 2020

1 reference

Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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)-

31 March 2020

1 reference

Thrombin-receptor antagonist vorapaxar in acute coronary syndromes

31 March 2020

1 reference

Endothelial barrier protection by activated protein C through PAR1-dependent sphingosine 1-phosphate receptor-1 crossactivation

31 March 2020

1 reference

Protection of vascular barrier integrity by activated protein C in murine models depends on protease-activated receptor-1.

31 March 2020

1 reference

'Role reversal' for the receptor PAR1 in sepsis-induced vascular damage

31 March 2020

1 reference

The in-vitro effects of E5555, a protease-activated receptor (PAR)-1 antagonist, on platelet biomarkers in healthy volunteers and patients with coronary artery disease.

31 March 2020

1 reference

Safety and tolerability of atopaxar in the treatment of patients with acute coronary syndromes: the lessons from antagonizing the cellular effects of Thrombin–Acute Coronary Syndromes Trial

31 March 2020

1 reference

Randomized trial of atopaxar in the treatment of patients with coronary artery disease: the lessons from antagonizing the cellular effect of Thrombin–Coronary Artery Disease Trial

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

Discovery of novel protease activated receptors 1 antagonists with potent antithrombotic activity in vivo

31 March 2020

1 reference

Exploration of a new series of PAR1 antagonists

31 March 2020

1 reference

Modified proteinase-activated receptor-1 and -2 derived peptides inhibit proteinase-activated receptor-2 activation by trypsin

31 March 2020

1 reference

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

31 March 2020

1 reference

Antagonism of Protease-Activated Receptor 2 Protects against Experimental Colitis

31 March 2020

1 reference

Novel agonists and antagonists for human protease activated receptor 2.

31 March 2020

1 reference

Profiling gene expression induced by protease-activated receptor 2 (PAR2) activation in human kidney cells

31 March 2020

1 reference

The role of PAR4 in thrombin-induced thromboxane production in human platelets

31 March 2020

1 reference

Thrombin responses in human endothelial cells. Contributions from receptors other than PAR1 include the transactivation of PAR2 by thrombin-cleaved PAR1.

31 March 2020

1 reference

Pharmacology, biodistribution, and efficacy of GPCR-based pepducins in disease models.

31 March 2020

1 reference

Pepducin-based intervention of thrombin-receptor signaling and systemic platelet activation

31 March 2020

1 reference

Activation and inhibition of G protein-coupled receptors by cell-penetrating membrane-tethered peptides

31 March 2020

1 reference

Blockade of PAR1 signaling with cell-penetrating pepducins inhibits Akt survival pathways in breast cancer cells and suppresses tumor survival and metastasis

31 March 2020

1 reference

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

31 March 2020

1 reference

Regulation of GPCRs by endocytic membrane trafficking and its potential implications

31 March 2020

1 reference

G protein-coupled receptor sorting to endosomes and lysosomes

31 March 2020

1 reference

Termination of protease-activated receptor-1 signaling by beta-arrestins is independent of receptor phosphorylation

31 March 2020

1 reference

A tyrosine-based sorting signal regulates intracellular trafficking of protease-activated receptor-1: multiple regulatory mechanisms for agonist-induced G protein-coupled receptor internalization

31 March 2020

1 reference

Down-regulation of protease-activated receptor-1 is regulated by sorting nexin 1

31 March 2020

1 reference

A novel protease-activated receptor-1 interactor, Bicaudal D1, regulates G protein signaling and internalization

31 March 2020

1 reference

Rab5a and rab11a mediate agonist-induced trafficking of protease-activated receptor 2.

31 March 2020

1 reference

Development of potent thrombin receptor antagonist peptides

31 March 2020

1 reference

RWJ-58259: a selective antagonist of protease activated receptor-1.

31 March 2020

1 reference

Inhibition of arterial thrombosis by a protease-activated receptor 1 antagonist, FR171113, in the guinea pig.

31 March 2020

1 reference

Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110).

31 March 2020

1 reference

Identification and characterization of novel small-molecule protease-activated receptor 2 agonists

31 March 2020

1 reference

Novel antagonists for proteinase-activated receptor 2: inhibition of cellular and vascular responses in vitro and in vivo

31 March 2020

1 reference

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

31 March 2020

1 reference

YD-3, a novel inhibitor of protease-induced platelet activation

31 March 2020

1 reference

Administration of a potent antagonist of protease-activated receptor-1 (PAR-1) attenuates vascular restenosis following balloon angioplasty in rats

31 March 2020

1 reference

12 December 2020

Proteinase-activated receptor 4 (PAR4): activation and inhibition of rat platelet aggregation by PAR4-derived peptides

1 reference

12 December 2020

Kallikrein-mediated cell signalling: targeting proteinase-activated receptors (PARs).

1 reference

12 December 2020

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

1 reference

12 December 2020

Mechanisms of initiation and termination of signalling by neuropeptide receptors: a comparison with the proteinase-activated receptors

1 reference

12 December 2020

Specific inhibition of thrombin-induced cell activation by the neutrophil proteinases elastase, cathepsin G, and proteinase 3: evidence for distinct cleavage sites within the aminoterminal domain of the thrombin receptor.

1 reference

12 December 2020

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

1 reference

12 December 2020

1 reference

12 December 2020

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

1 reference

12 December 2020

Selective inhibition of protease-activated receptor 4-dependent platelet activation by YD-3.

1 reference

12 December 2020

Increased local expression of coagulation factor X contributes to the fibrotic response in human and murine lung injury.

1 reference

12 December 2020

Inhibition of thrombin receptor signaling by a G-protein coupled receptor kinase. Functional specificity among G-protein coupled receptor kinases

1 reference

12 December 2020

Tethered ligand agonist peptides. Structural requirements for thrombin receptor activation reveal mechanism of proteolytic unmasking of agonist function

1 reference

12 December 2020

Proteinase-activated receptor 2 (PAR(2)): development of a ligand-binding assay correlating with activation of PAR(2) by PAR(1)- and PAR(2)-derived peptide ligands.

1 reference

12 December 2020

Proteinase-activated receptor 4 (PAR4): action of PAR4-activating peptides in vascular and gastric tissue and lack of cross-reactivity with PAR1 and PAR2

1 reference

12 December 2020

The distinct roles of two GPCRs, MrgprC11 and PAR2, in itch and hyperalgesia

1 reference

12 December 2020