Protease‐activated receptor 2 promotes actomyosin dependent transforming microvesicles generation from human breast cancer
Sign Up to like & getrecommendations! Published in 2018 at "Molecular Carcinogenesis"
DOI: 10.1002/mc.22891
Abstract: Apart from blood coagulation, coagulation proteases are involved inextricably in cancer progression/propagation via intra/inter‐cellular signaling, mediated predominantly by protease‐activated receptors (PARs). Microvesicles (MVs), a plasma membrane shredded component, has recently been identified as an important… read more here.
Keywords: human breast; breast cancer; generation; protease activated ... See more keywords
Design of a protease‐activated PD‐L1 inhibitor
Sign Up to like & getrecommendations! Published in 2023 at "Protein Science"
DOI: 10.1002/pro.4578
Abstract: Immune checkpoint inhibitors that bind to the cell surface receptor PD‐L1 are effective anti‐cancer agents but suffer from immune‐related adverse events as PD‐L1 is expressed on both healthy and cancer cells. To mitigate toxicity, researchers… read more here.
Keywords: protease; activated inhibitor; protease activated; inhibitor ... See more keywords
Protease-activated receptor 2 stabilizes Bcl-xL and regulates EGFR-targeted therapy response in colorectal cancer.
Sign Up to like & getrecommendations! Published in 2021 at "Cancer letters"
DOI: 10.1016/j.canlet.2021.05.040
Abstract: The Bcl-2 homolog Bcl-xL is emerging as a key factor in tumorigenesis due to its prominent pro-survival and cell death-independent functions. However, the regulation of Bcl-xL by microenvironment and its implication in cancer therapy of… read more here.
Keywords: par2; egfr targeted; protease activated; activated receptor ... See more keywords
Protease activated receptor 2 signaling promotes self-renewal and metastasis in colorectal cancer through β-catenin and periostin.
Sign Up to like & getrecommendations! Published in 2021 at "Cancer letters"
DOI: 10.1016/j.canlet.2021.08.032
Abstract: The maintenance and expansion of cancer stem-like cells (CSCs) is necessary for metastasis. Although protease-activated receptor 2 (PAR2) is strongly associated with colorectal cancer (CRC) progression, it is unclear how it regulates distal metastasis, and… read more here.
Keywords: par2; catenin; protease activated; activated receptor ... See more keywords
The domino effect triggered by the tethered ligand of the protease activated receptors.
Sign Up to like & getrecommendations! Published in 2020 at "Thrombosis research"
DOI: 10.1016/j.thromres.2020.08.004
Abstract: Protease activated receptors (PARs) are G-protein coupled receptors (GPCRs) that have a unique activation mechanism. Unlike other GPCRs that can be activated by free ligands, under physiological conditions, PARs are activated by the tethered ligand,… read more here.
Keywords: tethered ligand; domino effect; protease activated; activated receptors ... See more keywords
Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c02048
Abstract: Vorapaxar is an approved drug for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction or with peripheral arterial disease. Subsequent to the discovery of Vorapaxar, medicinal chemistry efforts were… read more here.
Keywords: optimization advance; lead optimization; chemistry; advance protease ... See more keywords
Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00359
Abstract: Protease-activated receptor 4 (PAR4) is a G-protein coupled receptor that is expressed on human platelets and activated by the coagulation enzyme thrombin. PAR4 plays a key role in blood coagulation, and its importance in pathological… read more here.
Keywords: bms 986120; bms; protease activated; activated receptor ... See more keywords
Asymmetric Si-rhodamine scaffolds: rational design of pH-durable protease-activated NIR probes in vivo.
Sign Up to like & getrecommendations! Published in 2020 at "Chemical communications"
DOI: 10.1039/c9cc09666c
Abstract: A group of asymmetric Si-rhodamine scaffolds was designed for protease-activated NIR probes. Dual pH-inertia for both spirocyclized fluorescent probes and fluorescent products of zwitterions form over a wide range of pH (4.0-11.0). Leucine aminopeptidase (LAP)… read more here.
Keywords: asymmetric rhodamine; protease activated; activated nir; nir probes ... See more keywords
New oral protease-activated receptor 4 antagonist BMS-986120: tolerability, pharmacokinetics, pharmacodynamics, and gene variant effects in humans
Sign Up to like & getrecommendations! Published in 2022 at "Platelets"
DOI: 10.1080/09537104.2022.2088719
Abstract: Abstract BMS-986120 is a novel first-in-class oral protease-activated receptor 4 (PAR4) antagonist exhibiting robust antithrombotic activity that has shown low bleeding risk in monkeys. We sought to assess pharmacokinetics, pharmacodynamics, and tolerability of BMS-986120 in… read more here.
Keywords: bms 986120; protease activated; par4; oral protease ... See more keywords
Protease-activated receptor 2 deficiency mediates cardiac fibrosis and diastolic dysfunction.
Sign Up to like & getrecommendations! Published in 2019 at "European heart journal"
DOI: 10.1093/eurheartj/ehz117
Abstract: AIMS Heart failure with preserved ejection fraction (HFpEF) and pathological cardiac aging share a complex pathophysiology, including extracellular matrix remodelling (EMR). Protease-activated receptor 2 (PAR2) deficiency is associated with EMR. The roles of PAR1 and… read more here.
Keywords: par2; fibrosis; cardiac fibrosis; protease activated ... See more keywords
Deficiency of protease-activated receptor (PAR) 1 and PAR2 exacerbates collagen-induced arthritis in mice via differing mechanisms.
Sign Up to like & getrecommendations! Published in 2020 at "Rheumatology"
DOI: 10.1093/rheumatology/keaa701
Abstract: OBJECTIVES Protease-activated receptor (PAR) 1 and PAR2 have been implicated in RA, however their exact role is unclear. Here, we detailed the mechanistic impact of these receptors on the onset and development of inflammatory arthritis… read more here.
Keywords: par2; induced arthritis; receptor par; par par2 ... See more keywords