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 …

RGD peptide‐drug conjugates as effective dual targeting platforms: recent advances

L Battistini, K Bugatti, A Sartori, C Curti… - European Journal of …, 2021 - Wiley Online Library
In recent years, targeted therapies have raised increasing interest as effective strategies to
improve therapeutic efficiency, reduce the impact of adverse side effects, and overcome …

[HTML][HTML] The PAR2 inhibitor I-287 selectively targets Gαq and Gα12/13 signaling and has anti-inflammatory effects

C Avet, C Sturino, S Grastilleur, CL Gouill… - Communications …, 2020 - nature.com
Abstract Protease-activated receptor-2 (PAR2) is involved in inflammatory responses and
pain, therefore representing a promising therapeutic target for the treatment of immune …

A potent antagonist of protease-activated receptor 2 that inhibits multiple signaling functions in human cancer cells

Y Jiang, MK Yau, J Lim, KC Wu, W Xu, JY Suen… - … of Pharmacology and …, 2018 - ASPET
Protease-activated receptor 2 (PAR2) is a cell surface protein linked to G-protein dependent
and independent intracellular signaling pathways that produce a wide range of …

Biased signaling by agonists of protease activated receptor 2

Y Jiang, MK Yau, WM Kok, J Lim, KC Wu… - ACS chemical …, 2017 - ACS Publications
Protease activated receptor 2 (PAR2) is associated with metabolism, obesity, inflammatory,
respiratory and gastrointestinal disorders, pain, cancer, and other diseases. The …

Protease activated receptor 2 (PAR2) modulators: a patent review (2010–2015)

MK Yau, J Lim, L Liu, DP Fairlie - Expert opinion on therapeutic …, 2016 - Taylor & Francis
Introduction: Protease activated receptor 2 (PAR2) is a self-activated G protein-coupled
receptor that has been implicated in several diseases, including inflammatory …

Protease-activated receptor 2: a promising therapeutic target for women's cancers

H Shah, DP Fairlie, J Lim - Journal of Pharmacology and Experimental …, 2024 - ASPET
Cancers affecting women, such as breast, uterine, ovarian, endometrial and cervical
cancers, have become increasingly prevalent. The growing incidence and death rates …

Protease-activated receptor 2 (PAR2)-targeting peptide derivatives for positron emission tomography (PET) imaging

JC LeSarge, P Thibeault, L Yu, MD Childs… - European Journal of …, 2023 - Elsevier
The proteolytically-activated G protein-coupled receptor (GPCR) protease-activated receptor
2 (PAR2), is implicated in various cancers and inflammatory diseases. Synthetic ligands and …

[HTML][HTML] Protease-activated receptors and other G-protein-coupled receptors: the melanoma connection

RA Rosero, GJ Villares, M Bar-Eli - Frontiers in Genetics, 2016 - frontiersin.org
The vast array of G-protein-coupled receptors (GPCRs) play crucial roles in both
physiological and pathological processes, including vision, coagulation, inflammation …

[HTML][HTML] Truncated glucagon-like Peptide-1 and Exendin-4 α-Conotoxin pl14a peptide chimeras maintain potency and α-Helicity and reveal interactions vital for cAMP …

JE Swedberg, CI Schroeder, JM Mitchell… - Journal of Biological …, 2016 - ASBMB
Glucagon-like peptide-1 (GLP-1) signaling through the glucagon-like peptide 1 receptor
(GLP-1R) is a key regulator of normal glucose metabolism, and exogenous GLP-1R agonist …