Protease-activated receptors (PARs): mechanisms of action and potential therapeutic modulators in PAR-driven inflammatory diseases

DM Heuberger, RA Schuepbach - Thrombosis journal, 2019 - Springer
Inflammatory diseases have become increasingly prevalent with industrialization. To
address this, numerous anti-inflammatory agents and molecular targets have been …

G protein–coupled receptor signaling through β-arrestin–dependent mechanisms

PY Jean-Charles, S Kaur… - Journal of cardiovascular …, 2017 - journals.lww.com
β-arrestin1 (or arrestin2) and β-arrestin2 (or arrestin3) are ubiquitously expressed cytosolic
adaptor proteins that were originally discovered for their inhibitory role in G protein–coupled …

Severe malaria is associated with parasite binding to endothelial protein C receptor

L Turner, T Lavstsen, SS Berger, CW Wang… - Nature, 2013 - nature.com
Sequestration of Plasmodium falciparum-infected erythrocytes in host blood vessels is a key
triggering event in the pathogenesis of severe childhood malaria, which is responsible for …

Structure, function and pathophysiology of protease activated receptors

MN Adams, R Ramachandran, MK Yau, JY Suen… - Pharmacology & …, 2011 - Elsevier
Discovered in the 1990s, protease activated receptors 1 (PARs) are membrane-spanning
cell surface proteins that belong to the G protein coupled receptor (GPCR) family. A defining …

Tissue factor as a link between inflammation and coagulation

M Witkowski, U Landmesser, U Rauch - Trends in cardiovascular medicine, 2016 - Elsevier
Due to its receptor activity for factor VII, tissue factor (TF) is primary initiator of the blood
coagulation cascade and ensures rapid hemostasis in case of organ damage. Inflammatory …

Biased signaling of protease-activated receptors

P Zhao, M Metcalf, NW Bunnett - Frontiers in endocrinology, 2014 - frontiersin.org
In addition to their role in protein degradation and digestion, proteases can also function as
hormone-like signaling molecules that regulate vital patho-physiological processes …

Targeting proteinase-activated receptors: therapeutic potential and challenges

R Ramachandran, F Noorbakhsh, K DeFea… - Nature reviews Drug …, 2012 - nature.com
Abstract Proteinase-activated receptors (PARs), a family of four seven-transmembrane G
protein-coupled receptors, act as targets for signalling by various proteolytic enzymes. PARs …

Driving Rho GTPase activity in endothelial cells regulates barrier integrity

CML Beckers, VWM van Hinsbergh… - Thrombosis and …, 2010 - thieme-connect.com
In the past decade understanding of the role of the Rho GTPases RhoA, Rac1 and Cdc42
has been developed from regulatory proteins that regulate specific actin cytoskeletal …

Endothelial cells: source, barrier, and target of defensive mediators

LT Roumenina, J Rayes, M Frimat… - Immunological …, 2016 - Wiley Online Library
Endothelium is strategically located at the interface between blood and interstitial tissues,
placing thus endothelial cell as a key player in vascular homeostasis. Endothelial cells are …

Neutrophil elastase and proteinase-3 trigger G protein-biased signaling through proteinase-activated receptor-1 (PAR1)

K Mihara, R Ramachandran, B Renaux… - Journal of Biological …, 2013 - ASBMB
Neutrophil proteinases released at sites of inflammation can affect tissue function by either
activating or disarming signal transduction mediated by proteinase-activated receptors …