Protease-activated receptors in health and disease

CJ Peach, LE Edgington-Mitchell… - Physiological …, 2023 - journals.physiology.org
Proteases are signaling molecules that specifically control cellular functions by cleaving
protease-activated receptors (PARs). The four known PARs are members of the large family …

Biased receptor signaling in drug discovery

T Kenakin - Pharmacological reviews, 2019 - ASPET
A great deal of experimental evidence suggests that ligands can stabilize different receptor
active states that go on to interact with cellular signaling proteins to form a range of different …

Don't stress about CRF: assessing the translational failures of CRF1antagonists

SR Spierling, EP Zorrilla - Psychopharmacology, 2017 - Springer
Abstract Background Dr. Athina Markou sought treatments for a common neural substrate
shared by depression and drug dependence. Antagonists of corticotropin-releasing factor …

The G protein–coupled receptor–transient receptor potential channel axis: molecular insights for targeting disorders of sensation and inflammation

NA Veldhuis, DP Poole, M Grace, P McIntyre… - Pharmacological …, 2015 - ASPET
Sensory nerves are equipped with receptors and ion channels that allow them to detect and
respond to diverse chemical, mechanical, and thermal stimuli. These sensory proteins …

Legumain induces oral cancer pain by biased agonism of protease-activated receptor-2

NH Tu, DD Jensen, BM Anderson, E Chen… - Journal of …, 2021 - Soc Neuroscience
Oral squamous cell carcinoma (OSCC) is one of the most painful cancers, which interferes
with orofacial function including talking and eating. We report that legumain (Lgmn) cleaves …

The development of proteinase-activated receptor-2 modulators and the challenges involved

KA McIntosh, MR Cunningham… - Biochemical Society …, 2020 - portlandpress.com
Protease-activated receptor-2 (PAR2) has been extensively studied since its discovery in the
mid-1990. Despite the advances in understanding PAR2 pharmacology, it has taken almost …

Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition

AJ Kennedy, L Sundström, S Geschwindner… - Communications …, 2020 - nature.com
Abstract Protease-activated receptor-2 (PAR2) has been implicated in multiple
pathophysiologies but drug discovery is challenging due to low small molecule tractability …

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 …

Antagonism of protease activated receptor-2 by GB88 reduces inflammation triggered by protease allergen Tyr-p3

YJ Wang, SJ Yu, JJ Tsai, CH Yu, EC Liao - Frontiers in Immunology, 2021 - frontiersin.org
The occurrence of allergic diseases induced by aeroallergens has increased in the past
decades. Among inhalant allergens, mites remain the important causal agent of allergic …

The Yin‐Yang roles of protease‐activated receptors in inflammatory signalling and diseases

X Zhuo, Y Wu, X Fu, X Liang, Y Xiang, J Li… - The FEBS …, 2022 - Wiley Online Library
Inflammatory diseases have become increasingly prevalent throughout the world.
Coronavirus disease 2019 (COVID‐19), which has recently become pandemic, also exhibits …