[HTML][HTML] 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 …

Molecular mechanisms regulating Proteinase‐Activated Receptors (PARs)

A Chandrabalan, R Ramachandran - The FEBS Journal, 2021 - Wiley Online Library
Proteinase‐activated receptors (PARs) are a four‐member family of G protein‐coupled
receptors defined by their irreversible proteolytic mechanism of activation. PARs have …

Proteinase-activated receptors (PARs)–focus on receptor-receptor-interactions and their physiological and pathophysiological impact

F Gieseler, H Ungefroren, U Settmacher… - Cell Communication and …, 2013 - Springer
Proteinase-activated receptors (PARs) are a subfamily of G protein-coupled receptors
(GPCRs) with four members, PAR 1, PAR 2, PAR 3 and PAR 4, playing critical functions in …

Cathepsin S causes inflammatory pain via biased agonism of PAR2 and TRPV4

P Zhao, TM Lieu, N Barlow, M Metcalf… - Journal of Biological …, 2014 - ASBMB
Serine proteases such as trypsin and mast cell tryptase cleave protease-activated receptor-2
(PAR 2) at R 36↓ S 37 and reveal a tethered ligand that excites nociceptors, causing …

Beyond thrombosis: the impact of tissue factor signaling in cancer

D Unruh, C Horbinski - Journal of Hematology & Oncology, 2020 - Springer
Tissue factor (TF) is the primary initiator of the coagulation cascade, though its effects extend
well beyond hemostasis. When TF binds to Factor VII, the resulting TF: FVIIa complex can …

Biased signalling and proteinase‐activated receptors (PAR s): targeting inflammatory disease

MD Hollenberg, K Mihara, D Polley… - British journal of …, 2014 - Wiley Online Library
Although it has been known since the 1960s that trypsin and chymotrypsin can mimic
hormone action in tissues, it took until the 1990s to discover that serine proteinases can …

Rational design and synthesis of an orally bioavailable peptide guided by NMR amide temperature coefficients

CK Wang, SE Northfield, B Colless… - Proceedings of the …, 2014 - National Acad Sciences
Enhancing the oral bioavailability of peptide drug leads is a major challenge in drug design.
As such, methods to address this challenge are highly sought after by the pharmaceutical …

Protease-activated receptor 2 (PAR2) protein and transient receptor potential vanilloid 4 (TRPV4) protein coupling is required for sustained inflammatory signaling

DP Poole, S Amadesi, NA Veldhuis… - Journal of biological …, 2013 - ASBMB
G protein-coupled receptors of nociceptive neurons can sensitize transient receptor potential
(TRP) ion channels, which amplify neurogenic inflammation and pain. Protease-activated …

Macrophage TLR4 and PAR2 signaling: role in regulating vascular inflammatory injury and repair

S Rayees, I Rochford, JC Joshi, B Joshi… - Frontiers in …, 2020 - frontiersin.org
Macrophages play a central role in dictating the tissue response to infection and
orchestrating subsequent repair of the damage. In this context, macrophages residing in the …

Functional proteomic profiling of secreted serine proteases in health and inflammatory bowel disease

A Denadai-Souza, C Bonnart, NS Tapias, M Marcellin… - Scientific reports, 2018 - nature.com
While proteases are essential in gastrointestinal physiology, accumulating evidence
indicates that dysregulated proteolysis plays a pivotal role in the pathophysiology of …