Neutrophil Elastase and Proteinase-3 Trigger G Protein-biased Signaling through Proteinase-activated Receptor-1 (PAR1)

Signalling bias in new drug discovery: detection, quantification and therapeutic impact

(2013) Terry Kenakin et al.   NATURE REVIEWS DRUG DISCOVERY

Biased agonism of protease-activated receptor 1 by activated protein C caused by noncanonical cleavage at Arg46

(2012) L. O. Mosnier et al.   BLOOD

New concepts in pharmacological efficacy at 7TM receptors: IUPHAR Review 2

(2012) Terry Kenakin   BRITISH JOURNAL OF PHARMACOLOGY

β-Adrenergic Receptor Stimulation Transactivates Protease-Activated Receptor 1 via Matrix Metalloproteinase 13 in Cardiac Cells

(2012) Fabrice Jaffré et al.   CIRCULATION

Protease-activated receptor-1 cleaved at R46 mediates cytoprotective effects

(2012) R. A. SCHUEPBACH et al.   JOURNAL OF THROMBOSIS AND HAEMOSTASIS

Targeting proteinase-activated receptors: therapeutic potential and challenges

(2012) Rithwik Ramachandran et al.   NATURE REVIEWS DRUG DISCOVERY

A matrix metalloprotease-PAR1 system regulates vascular integrity, systemic inflammation and death in sepsis

(2011) Sarah L. Tressel et al.   EMBO Molecular Medicine

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

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

Structure, function and pathophysiology of protease activated receptors

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

Activated protein C promotes protease-activated receptor-1 cytoprotective signaling through  -arrestin and dishevelled-2 scaffolds

(2011) U. J. K. Soh et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Differential association modes of the thrombin receptor PAR1 with Gαi1, Gα12, and β-arrestin 1

(2010) Mohammed Akli Ayoub et al.   FASEB JOURNAL

Functional Selectivity and Biased Receptor Signaling

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

Teaching old receptors new tricks: biasing seven-transmembrane receptors

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

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

Agonist-Biased Signaling via Proteinase Activated Receptor-2: Differential Activation of Calcium and Mitogen-Activated Protein Kinase Pathways

(2009) R. Ramachandran et al.   MOLECULAR PHARMACOLOGY

A matrix metalloproteinase-1/protease activated receptor-1 signaling axis promotes melanoma invasion and metastasis

(2009) J S Blackburn et al.   ONCOGENE

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

Matrix Metalloproteinase-1 and Thrombin Differentially Activate Gene Expression in Endothelial Cells via PAR-1 and Promote Angiogenesis

(2008) Jessica S. Blackburn et al.   AMERICAN JOURNAL OF PATHOLOGY

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

Parstatin, the Cleaved Peptide on Proteinase-Activated Receptor 1 Activation, Is a Potent Inhibitor of Angiogenesis

(2008) P. Zania et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Lipid raft localization regulates the cleavage specificity of protease activated receptor 1 in endothelial cells

(2008) J.-S. BAE et al.   JOURNAL OF THROMBOSIS AND HAEMOSTASIS

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

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