Improved synthesis of the PAR-1 thrombine receptor antagonist RWJ-58259 [PDF]
ARKIVOC, 2009 A significant improvement on the synthesis of the PAR-1 antagonist RWJ-58259 is described, which involves a base-related two-fold yield increase in the indazole N-alkylation, and an easier purification and a nine-fold yield increase in the urea formation, by using triphosgene/propylene oxide as urea coupling traceless reagents.
Ángel M. Valdivielso +2 more
doaj +3 more sources
The predictive role of protease-activated receptor (PAR-1) polymorphisms and activated microplatelets on the severity of atherosclerosis – preliminary studies [PDF]
Frontiers in Molecular BiosciencesThis study is a comprehensive analysis of PAR-1 – involved in thrombin interaction with platelets (PLT), present on PLT and microparticles (PMP) – to understand its role in diabetic macroangiopathy (DM) and atherosclerosis obliterans (AO). The applied RT-
Urszula Jakobsche-Policht +20 more
doaj +2 more sources
Role of protease‐activated receptor‐1 (PAR‐1) in the glomerular filtration barrier integrity
Physiological Reports, 2022 Protease‐activated receptors (PAR) play an important role in the regulation of cellular function by the coagulation system, and they are activated by thrombin. PAR‐1 is expressed in both endothelial cells and podocytes in the kidney.
Ajay Medipally +8 more
doaj +3 more sources
Proximity labeling of DAF-16 FOXO highlights aging regulatory proteins [PDF]
Nature CommunicationsInsulin/insulin-like growth factor signaling inhibits FOXO transcription factors to control development, homeostasis, and aging. Here, we use proximity labeling to identify proteins interacting with the C. elegans FOXO DAF-16.
Murat Artan, Hanna Schoen, Mario de Bono
doaj +2 more sources
The role of protease-activated receptors (PARs) in the functioning of platelets and platelet-derived microparticles (PMPs) [PDF]
Frontiers in Molecular BiosciencesProtease-activated receptors (PARs), present on the surface of platelets and platelet-derived microparticles (PMPs), belong to a superfamily of membrane receptors that play a key role in initiating intracellular G protein-dependent signaling pathways ...
Urszula Jakobsche-Policht +20 more
doaj +2 more sources
Protease-Activated Receptor-1 Supports Locomotor Recovery by Biased Agonist Activated Protein C after Contusive Spinal Cord Injury. [PDF]
PLoS ONE, 2017 Thrombin-induced secondary injury is mediated through its receptor, protease activated receptor-1 (PAR-1), by "biased agonism." Activated protein C (APC) acts through the same PAR-1 receptor but functions as an anti-coagulant and anti-inflammatory ...
William D Whetstone +5 more
doaj +1 more source
Role and regulation of the thrombin receptor (PAR-1) in human melanoma [PDF]
Oncogene, 2003 To determine treatment strategies and predict the clinical outcome of patients with melanoma it is important to understand the etiology of this disease. Recently, there has been some insight into molecular basis of melanoma including identification of a few of the regulatory factors and genes involved in this disease.
Carmen, Tellez, Menashe, Bar-Eli
openaire +2 more sources
Protease-Activated Receptor-1 Antagonist Protects Against Lung Ischemia/Reperfusion Injury
Frontiers in Pharmacology, 2021 Protease-activated receptor (PAR)-1 is a thrombin-activated receptor that plays an essential role in ischemia/reperfusion (IR)-induced acute inflammation. PAR-1 antagonists have been shown to alleviate injuries in various IR models.
Shi-Jye Chu +5 more
doaj +1 more source
Journal of Pharmacological Sciences, 2017 The kidney expresses protease-activated receptor-1 (PAR-1). PAR-1 is known as a thrombin receptor, but its role in kidney injury is not well understood.
Yu Guan +13 more
doaj +1 more source
Etk/Bmx regulates proteinase-activated-receptor1 (PAR1) in breast cancer invasion: signaling partners, hierarchy and physiological significance. [PDF]
PLoS ONE, 2010 BACKGROUND: While protease-activated-receptor 1 (PAR(1)) plays a central role in tumor progression, little is known about the cell signaling involved.
Irit Cohen +11 more
doaj +1 more source