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Protease activated receptor

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https://www.readbyqxmd.com/read/29164814/a-thrombin-receptor-derived-imaging-agent-detects-subclinical-arthritis-in-mice
#1
Beth Friedman, Michael A Whitney, Elamprakash N Savariar, Christa Caneda, Paul Steinbach, Qing Xiong, Dina V Hingorani, Jessica Crisp, Stephen R Adams, Michael Kenner, Csilla N Lippert, Quyen T Nguyen, Monica Guma, Roger Y Tsien, Maripat Corr
OBJECTIVE: Functional imaging of synovitis could improve both early detection of rheumatoid arthritis (RA) and long-term outcomes. Motivated by the intersection of inflammation with coagulation protease activation, we examine coagulation protease activities in arthritic mice with a dual fluorescent Ratiometric thrombin-Activatable Cell Penetrating Peptide (RACPPNleTPRSFL ). METHOD: Mice with chronic transgenic K/BxN arthritis, or with arthritis on Day 1 of passive serum transfer induced arthritis (STIA), were imaged in vivo for Cy5 em: Cy7 em ratiometric fluorescence from proteolytic cleavage and activation of RACPPNleTPRSFL ...
November 22, 2017: Arthritis & Rheumatology
https://www.readbyqxmd.com/read/29164060/tissue-factor-expressing-tumor-derived-extracellular-vesicles-activate-quiescent-endothelial-cells-via-protease-activated-receptor-1
#2
Sara P Y Che, Jeannie Y Park, Tracy Stokol
Tissue factor (TF)-expressing tumor-derived extracellular vesicles (EVs) can promote metastasis and pre-metastatic niche formation, but the mechanisms by which this occurs remain largely unknown. We hypothesized that generation of activated factor X (FXa) by TF expressed on tumor-derived EV could activate protease-activated receptors (PARs) on non-activated endothelial cells to induce a pro-adhesive and pro-inflammatory phenotype. We obtained EV from TF-expressing breast (MDA-MB-231) and pancreatic (BxPC3 and Capan-1) tumor cell lines...
2017: Frontiers in Oncology
https://www.readbyqxmd.com/read/29161013/intelligent-peptide-gathering-mechanical-arm-tames-wild-trojan-horse-peptides-for-the-controlled-delivery-of-cancer-nanotherapeutics
#3
Nian-Qiu Shi, Yan Li, Yong Zhang, Nan Shen, Ling Qi, Shu-Ran Wang, Xian-Rong Qi
Cell-penetrating peptides (CPPs), also called "Trojan-Horse" peptides, have been used for facilitating intracellular delivery of numerous diverse cargoes and even nanocarriers. However, the lack of targeting specificity ("wildness" or nonselectivity) of CPP-nanocarriers remains an intractable challenge for many in vivo applications. In this work, we used an intelligent "peptide-gathering mechanical arm" (Int PMA) to curb CPPs' wildness and enhance the selectivity of R9-liposome-based cargo delivery for tumor targeting...
November 21, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29152144/tissue-type-plasminogen-activator-modulates-macrophage-m2-to-m1-phenotypic-change-through-annexin-a2-mediated-nf-%C3%AE%C2%BAb-pathway
#4
Ling Lin, Kebin Hu
Macrophage accumulation is one of the hallmarks of progressive kidney disease. In response to injury, macrophages undergo a phenotypic polarization to become two functionally distinct subsets: M1 and M2 macrophages. Macrophage polarization is a dynamic process, and recent work indicates that macrophages, in response to kidney injury, can shift their polarity. However, the underlying mechanisms remain largely unknown. Tissue-type plasminogen activator (tPA), a protease up-regulated in the chronically injured kidneys, has been shown to preferably promote M1 macrophage accumulation and renal inflammation...
October 20, 2017: Oncotarget
https://www.readbyqxmd.com/read/29149696/clearance-of-plasmin-pn-1-complexes-by-vascular-smooth-muscle-cells-in-human-aneurysm-of-the-ascending-aorta
#5
Kamel Boukais, Luciano F Borges, Laurence Venisse, Ziad Touat, Déborah François, Véronique Arocas, Guillaume Jondeau, Paul Declerck, Marie-Christine Bouton, Jean-Baptiste Michel
Plasminogen is a circulating zymogen which enters the arterial wall by radial, transmural hydraulic conductance, where it is converted to plasmin by tissue plasminogen activator t-PA on an activation platform involving S100A4 on the vascular smooth muscle cell (vSMC) membrane. Plasmin is involved in the progression of human thoracic aneurysm of the ascending aorta (TAA). vSMCs protect the TAA wall from plasmin-induced proteolytic injury by expressing high levels of antiproteases. Protease nexin-1 (PN-1) is a tissue antiprotease belonging to the serpin superfamily, expressed in the vascular wall, and is able to form a covalent complex with plasmin...
October 24, 2017: Cardiovascular Pathology: the Official Journal of the Society for Cardiovascular Pathology
https://www.readbyqxmd.com/read/29148820/a-functional-kinase-short-interfering-ribonucleic-acid-screen-using-protease-activated-receptor-2-dependent-opening-of-transient-receptor-potential-vanilloid-4
#6
William G Darby, Megan S Grace, Kaylene J Simpson, Owen L Woodman, Peter McIntyre
Protease-activated receptor 2 (PAR2) is a proinflammatory G-protein coupled receptor (GPCR) that is activated by inflammatory proteases, and its activation initiates signaling pathways that modulate the nonselective cation channel transient receptor potential vanilloid-4 (TRPV4). PAR2-dependent opening of TRPV4 has been attributed to kinase activation, but the identity of the responsible enzymes is unknown. Deciphering the signaling pathways involved in the PAR2-dependent opening of TRPV4 may yield new targets for pain treatment...
November 17, 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29146750/trpm7-transient-receptor-potential-melastatin-like-7-channel-kinase-controls-calcium-responses-in-arterial-thrombosis-and-stroke-in-mice
#7
Sanjeev K Gotru, Wenchun Chen, Peter Kraft, Isabelle C Becker, Karen Wolf, Simon Stritt, Susanna Zierler, Heike M Hermanns, Deviyani Rao, Anne-Laure Perraud, Carsten Schmitz, René P Zahedi, Peter J Noy, Michael G Tomlinson, Thomas Dandekar, Masayuki Matsushita, Vladimir Chubanov, Thomas Gudermann, Guido Stoll, Bernhard Nieswandt, Attila Braun
OBJECTIVE: TRPM7 (transient receptor potential melastatin-like 7 channel) is a ubiquitously expressed bifunctional protein comprising a transient receptor potential channel segment linked to a cytosolic α-type serine/threonine protein kinase domain. TRPM7 forms a constitutively active Mg(2+) and Ca(2+) permeable channel, which regulates diverse cellular processes in both healthy and diseased conditions, but the physiological role of TRPM7 kinase remains largely unknown. APPROACH AND RESULTS: Here we show that point mutation in TRPM7 kinase domain deleting the kinase activity in mice (Trpm7(R/R) ) causes a marked signaling defect in platelets...
November 16, 2017: Arteriosclerosis, Thrombosis, and Vascular Biology
https://www.readbyqxmd.com/read/29144748/chemical-modification-for-proteolytic-stabilization-of-the-selective-%C3%AE-v%C3%AE-3-integrin-rgdechi-peptide-in-vitro-and-in-vivo-activities-on-malignant-melanoma-cells
#8
Daniela Comegna, Antonella Zannetti, Annarita Del Gatto, Ivan de Paola, Luigi Russo, Sonia Di Gaetano, Annamaria Liguoro, Domenica Capasso, Michele Saviano, Laura Zaccaro
Herein we report the synthesis and biological characterization of the novel peptide ψRGDechi as the first step towards novel targeted theranostics in melanoma. This pseudo-peptide is designed from our previously reported RGDechi peptide, known to bind selectively αvβ3 integrin, and differs for a modified amide bond at the main protease cleavage site. This chemical modification drastically reduces the enzymatic degradation in serum, compared to its parental peptide, resulting in an overall magnification of the biological activity on a highly expressing αvβ3 human metastatic melanoma cell line...
November 16, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29142404/chalepin-a-compound-from-ruta-angustifolia-l-pers-exhibits-cell-cycle-arrest-at-s-phase-suppresses-nuclear-factor-kappa-b-nf-%C3%AE%C2%BAb-pathway-signal-transducer-and-activation-of-transcription-3-stat3-phosphorylation-and-extrinsic-apoptotic-pathway-in-non-small-cell
#9
Jaime Stella Moses Richardson, Norhaniza Aminudin, Sri Nurestri Abd Malek
Background: Plants have been a major source of inspiration in developing novel drug compounds in the treatment of various diseases that afflict human beings worldwide. Ruta angustifolia L. Pers known locally as Garuda has been conventionally used for various medicinal purposes such as in the treatment of cancer. Objective: A dihydrofuranocoumarin named chalepin, which was isolated from the chloroform extract of the plant, was tested on its ability to inhibit molecular pathways of human lung carcinoma (A549) cells...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29141676/platelets-are-activated-in-anca-associated-vasculitis-via-thrombin-pars-pathway-and-can-activate-the-alternative-complement-pathway
#10
Di Miao, Dan-Yang Li, Min Chen, Ming-Hui Zhao
BACKGROUND: In this study, we investigated the mechanism of platelet activation in patients with antineutrophil cytoplasmic antibody (ANCA)-associated vasculitis (AAV), as well as the activation of the alternative complement pathway by platelets in AAV. METHODS: CD62P and platelet-leukocyte aggregates in AAV patients were tested by flow cytometry. Platelets were stimulated by plasma from active AAV patients. The effect of the thrombin-protease-activated receptors (PARs) pathway was evaluated by blocking thrombin or PAR1 antagonists...
November 15, 2017: Arthritis Research & Therapy
https://www.readbyqxmd.com/read/29141644/lipopolysaccharide-pretreatment-increases-protease-activated-receptor-2-expression-and-monocyte-chemoattractant-protein-1-secretion-in-vascular-endothelial-cells
#11
Hung-Hsing Chao, Po-Yuan Chen, Wen-Rui Hao, Wei-Ping Chiang, Tzu-Hurng Cheng, Shih-Hurng Loh, Yuk-Man Leung, Ju-Chi Liu, Jin-Jer Chen, Li-Chin Sung
BACKGROUND: This study investigated whether lipopolysaccharide (LPS) increase protease-activated receptor-2 (PAR-2) expression and enhance the association between PAR-2 expression and chemokine production in human vascular endothelial cells (ECs). METHODS: The morphology of ECs was observed through microphotography in cultured human umbilical vein ECs (EA. hy926 cells) treated with various LPS concentrations (0, 0.25, 0.5, 1, and 2 μg/mL) for 24 h, and cell viability was assessed using the MTT assay...
November 15, 2017: Journal of Biomedical Science
https://www.readbyqxmd.com/read/29140280/trpv3-channel-in-keratinocytes-in-scars-with-post-burn-pruritus
#12
Chun Wook Park, Hyun Ji Kim, Yong Won Choi, Bo Young Chung, So-Youn Woo, Dong-Keun Song, Hye One Kim
Post-burn pruritus is a common and distressing sequela of burn scars. Empirical antipruritic treatments usually fail to have a satisfactory outcome because of their limited selectivity and possible side effects. Therefore, novel drug targets need to be identified. Here, we aimed to investigate the possible role of protease-activated receptor 2 (PAR2) and transient receptor potential vanniloid 3 (TRPV3), along with the relation of TRPV3 to thymic stromal lymphopoietin (TSLP). Specimens from normal (unscarred) or burn-scarred (with or without pruritus) tissue were obtained from burn patients for this study...
November 15, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29138532/ubiquitin-specific-protease-2-modulates-the-lipopolysaccharide-elicited-expression-of-proinflammatory-cytokines-in-macrophage-like-hl-60-cells
#13
Hiroshi Kitamura, Takeshi Ishino, Yoshinori Shimamoto, Jun Okabe, Tomomi Miyamoto, Eiki Takahashi, Ichiro Miyoshi
We investigated the regulatory roles of USP2 in mRNA accumulation of proinflammatory cytokines in macrophage-like cells after stimulation with a toll-like receptor (TLR) 4 ligand, lipopolysaccharide (LPS). Human macrophage-like HL-60 cells, mouse macrophage-like J774.1 cells, and mouse peritoneal macrophages demonstrated negative feedback to USP2 mRNA levels after LPS stimulation, suggesting that USP2 plays a significant role in LPS-stimulated macrophages. USP2 knockdown (KD) by short hairpin RNA in HL-60 cells promoted the accumulation of transcripts for 25 of 104 cytokines after LPS stimulation...
2017: Mediators of Inflammation
https://www.readbyqxmd.com/read/29134286/proteomic-and-metabolomic-characterization-of-streptozotocin-induced-diabetic-nephropathy-in-timp3-deficient-mice
#14
Claudia Rossi, Valeria Marzano, Ada Consalvo, Mirco Zucchelli, Stefano Levi Mortera, Viviana Casagrande, Maria Mavilio, Paolo Sacchetta, Massimo Federici, Rossella Menghini, Andrea Urbani, Domenico Ciavardelli
AIMS: The tissue inhibitor of metalloproteinase TIMP3 is a stromal protein that restrains the activity of both protease and receptor in the extracellular matrix and has been found to be down-regulated in diabetic nephropathy (DN), the leading cause of end-stage renal disease in developed countries. METHODS: In order to gain deeper insights on the association of loss of TIMP3 and DN, we performed differential proteomic analysis of kidney and blood metabolic profiling of wild-type and Timp3-knockout mice before and after streptozotocin (STZ) treatment, widely used to induce insulin deficiency and hyperglycemia...
November 13, 2017: Acta Diabetologica
https://www.readbyqxmd.com/read/29130686/thioamide-substitution-selectively-modulates-proteolysis-and-receptor-activity-of-therapeutic-peptide-hormones
#15
Xing Chen, Elizabeth G Mietlicki-Baase, Taylor M Barrett, Lauren E McGrath, Kieran Koch-Laskowski, John J Ferrie, Matthew R Hayes, E James Petersson
Peptide hormones are attractive as injectable therapeutics and imaging agents, but they often require extensive modification by mutagenesis and/or chemical synthesis to prevent rapid in vivo degradation. Alternatively, the single-atom, O-to-S modification of peptide backbone thioamidation has the potential to selectively perturb interactions with proteases while preserving interactions with other proteins, such as target receptors. Here, we use the validated diabetes therapeutic, glucagon-like peptide-1 (GLP-1), and the target of clinical investigation, gastric inhibitory polypeptide (GIP), as proof-of-principle peptides to demonstrate the value of thioamide substitution...
November 13, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29122715/nematicidal-activity-of-a-water-soluble-lectin-from-seeds-of-moringa-oleifera
#16
Mário Luan Silva de Medeiros, Maiara Celine de Moura, Thiago Henrique Napoleão, Patrícia Maria Guedes Paiva, Luana Cassandra Breitenbach Barroso Coelho, Ana Carla Diógenes Suassuna Bezerra, Michele Dalvina Correia da Silva
Gastrointestinal nematodes are the major cause of animal diseases, and the indiscriminate use of synthetic anthelmintic contributes to the development of drug resistance. Natural bioproducts are noteworthy since they have proved to be promising for alternative antiparasitic therapies. This study evaluated the in vitro effect of WSMoL (water soluble Moringa oleifera lectin) on hatching of eggs and on the development of early-stage larvae of gastrointestinal nematodes from naturally infected goats. In addition, the interference of WSMoL on activity of proteases was determined and the affinity of the lectin for glycosylated molecules of these parasites was investigated using fluorescein isothiocyanate (FITC)-labeled WSMoL...
November 6, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29121676/naringin-prevents-hiv-1-protease-inhibitors-induced-metabolic-complications-in-vivo
#17
Sanelisiwe Nzuza, Sindiswa Zondi, Peter M O Owira
BACKGROUND: Insulin resistance, glucose intolerance and overt diabetes are known metabolic complications associated with chronic use of HIV-Protease Inhibitors. Naringin is a grapefruit-derived flavonoid with anti-diabetic, anti-dyslipidemia, anti-inflammatory and anti-oxidant activities. OBJECTIVES: The study investigated the protective effects of naringin on glucose intolerance and impaired insulin secretion and signaling in vivo. METHODS: Male Wistar rats were divided into six groups (n = 6) and were daily orally treated with distilled water {3...
2017: PloS One
https://www.readbyqxmd.com/read/29118913/protease-activated-receptor-2-in-diabetic-nephropathy-a-double-edged-sword
#18
Maaike Waasdorp, JanWillem Duitman, Sandrine Florquin, Arnold C Spek
Diabetic nephropathy is a major microvascular complication of diabetes mellitus, and the leading cause of end stage renal disease worldwide. The pathogenesis of diabetic nephropathy is complex, making the development of novel treatments that stop or reverse the progression of microalbuminuria into end stage renal disease a challenge. Protease activated receptor (PAR)-2 has recently been shown to aggravate disease progression in diabetic nephropathy based upon which it was suggested that PAR-2 would be a potential target for the treatment of diabetic nephropathy...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/29114573/plasmin-reduces-fibronectin-deposition-by-mesangial-cells-in-a-protease-activated-receptor-1-independent-manner
#19
Maaike Waasdorp, JanWillem Duitman, C Arnold Spek
Background: Protease-activated receptor-1 (PAR-1) potentiates diabetic nephropathy (DN) as evident from reduced kidney injury in diabetic PAR-1 deficient mice. Although thrombin is the prototypical PAR-1 agonist, anticoagulant treatment does not limit DN in experimental animal models suggesting that thrombin is not the endogenous PAR-1 agonist driving DN. Objectives: To identify the endogenous PAR-1 agonist potentiating diabetes-induced nephropathy. Methods: Unbiased protease expression profiling in glomeruli from human kidneys with DN was performed using publically available microarray data...
July 2017: Biochemistry and Biophysics Reports
https://www.readbyqxmd.com/read/29113347/lunasin-functionally-enhances-ldl-uptake-via-inhibiting-pcsk9-and-enhancing-ldlr-expression-in-vitro-and-in-vivo
#20
Lili Gu, Yue Wang, Yaqiong Xu, Qinghua Tian, Gaoxin Lei, Cheng Zhao, Zhan Gao, Qin Pan, Wenfeng Zhao, Liu Nong, Shuhua Tan
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a serine protease which regulates serum low-density lipoprotein cholesterol (LDL-C) levels by promoting the degradation of the hepatic low-density lipoprotein receptor (LDLR), and has become an attractive therapeutic target for cholesterol lowering intervention. Lunasin, a 43-amino acid polypeptide initially isolated from soybean, has been previously proven to possess cholesterol lowering activity. Here we identified the down-regulation of PCSK9 expression by lunasin as one new mechanism that increased cell-surface LDLR level and enhanced LDL uptake in vitro and in vivo...
October 6, 2017: Oncotarget
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