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serin protease inhibitor

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https://www.readbyqxmd.com/read/28732041/understanding-russell-s-viper-venom-factor-v-activator-s-substrate-specificity-by-surface-plasmon-resonance-and-in-silico-studies
#1
Pradeep K Yadav, Christian B Antonyraj, Syed Ibrahim Basheer Ahamed, Sistla Srinivas
Blood coagulation factor V (FV) is activated either by Factor X or thrombin, cleaving at three different sites viz., Site I (Arg709-Ser710), site II (Arg1018-Thr1019), and site III (Arg1545-Ser1546). Russell's viper venom factor V activator (RVV-V) is a thrombin-like serine proteinase that activates FV with selective, single cleavage at site III. A long lasting effort is being pending in understanding the 'selective' binding specificity of the RVV-V towards site III. Here, we present the binding kinetic study of RVV-V with two designed peptides corresponding to the regions from site I (Gln699-Asn713) and site II (1008Lys-Pro1022), respectively, that include 15 amino acids...
2017: PloS One
https://www.readbyqxmd.com/read/28729054/isosorbide-based-peptidomimetics-as-inhibitors-of-hepatitis-c-virus-serine-protease
#2
Aline C Portela, Thalita G Barros, Camilo H da S Lima, Luiza R S Dias, Pedro H R de A Azevedo, Anna Sophia C L Dantas, Ronaldo Mohana-Borges, Gustavo T Ventura, Sergio Pinheiro, Estela M F Muri
Hepatitis C infection is a cause of chronic liver diseases such as cirrhosis and carcinoma. The current therapy for hepatitis C has limited efficacy and low tolerance. The HCV encodes a serine protease which is critical for viral replication, and few protease inhibitors are currently on the market. In this paper, we describe the synthesis and screening of novel isosorbide-based peptidomimetic inhibitors, in which the compounds 1d, 1e, and 1i showed significant inhibition of the protease activity in vitro at 100µM...
July 8, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28726978/analysis-of-the-substrate-specificity-of-factor-vii-activating-protease-fsap-and-design-of-specific-and-sensitive-peptide-substrates
#3
Emrah Kara, Dipankar Manna, Geir Åge Løset, Eric L Schneider, Charles S Craik, Sandip Kanse
Factor VII (FVII) activating protease (FSAP) is a circulating serine protease that is likely to be involved in a number of disease conditions such as stroke, atherosclerosis, liver fibrosis, thrombosis and cancer. To date, no systematic information is available about the substrate specificity of FSAP. Applying phage display and positional scanning substrate combinatorial library (PS-SCL) approaches we have characterised the specificity of FSAP towards small peptides. Results were evaluated in the context of known protein substrates as well as molecular modelling of the peptides in the active site of FSAP...
July 20, 2017: Thrombosis and Haemostasis
https://www.readbyqxmd.com/read/28726057/macrophage-migration-inhibitory-factor-mif-modulates-trophic-signaling-through-interaction-with-serine-protease-htra1
#4
Åsa Fex Svenningsen, Svenja Löring, Anna Lahn Sørensen, Ha Uyen Buu Huynh, Simone Hjæresen, Nellie Martin, Jesper Bonnet Moeller, Maria Louise Elkjær, Uffe Holmskov, Zsolt Illes, Malin Andersson, Solveig Beck Nielsen, Eirikur Benedikz
Macrophage migration inhibitory factor (MIF), a small conserved protein, is abundant in the immune- and central nervous system (CNS). MIF has several receptors and binding partners that can modulate its action on a cellular level. It is upregulated in neurodegenerative diseases and cancer although its function is far from clear. Here, we report the finding of a new binding partner to MIF, the serine protease HTRA1. This enzyme cleaves several growth factors, extracellular matrix molecules and is implicated in some of the same diseases as MIF...
July 19, 2017: Cellular and Molecular Life Sciences: CMLS
https://www.readbyqxmd.com/read/28724693/new-peptide-inhibitor-of-dipeptidyl-peptidase-iv-emdb-1-extends-the-half-life-of-glp-2-and-attenuates-colitis-in-mice-after-topical-administration
#5
Maciej Salaga, Anna Mokrowiecka, Marta Zielinska, Ewa Malecka-Panas, Radzislaw Kordek, Elzbieta Kamysz, Jakub Fichna
Protease inhibition has become a new possible approach in the inflammatory bowel disease (IBD) therapy. A serine exopeptidase, dipeptidyl peptidase IV (DPP IV) is responsible for inactivation of incretine hormone, glucagon-like peptide 2 (GLP-2), a potent stimulator of intestinal epithelium regeneration and growth. Recently we showed that the novel peptide analog of endomorphin-2, EMDB-1 is a potent blocker of DPP IV and has an inhibitory effect on gastrointestinal (GI) smooth muscle contractility. The aim of this study was to characterize the anti-inflammatory effect and mechanism of action of EMDB-1 in the mouse GI tract...
July 19, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28722823/rational-design-of-a-highly-potent-and-selective-peptide-inhibitor-of-pace4-by-salt-bridge-interaction-with-d160-at-position-p3
#6
Vahid Dianati, Azar Shamloo, Anna Kwiatkowska, Roxane Desjardins, Armand Soldera, Robert Day, Yves L Dory
PACE4, a member of the proprotein convertases (PCs) family of serine proteases, is a validated target for prostate cancer. Our group has developed a potent and selective PACE4 inhibitor: Ac-LLLLRVKR-NH2 . In seeking for modifications to increase the selectivity of this ligand toward PACE4, we replaced one of its P3 Val methyl groups with a basic group capable of forming a salt bridge with D160 of PACE4. The resulting inhibitor is eight times more potent than the P3 Val parent inhibitor and two times more selective over furin, because the equivalent salt bridge with furin E257 is not optimal...
July 19, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28713775/salivary-tick-cystatin-omc2-targets-lysosomal-cathepsins-s-and-c-in-human-dendritic-cells
#7
Tina Zavašnik-Bergant, Robert Vidmar, Andreja Sekirnik, Marko Fonović, Jiří Salát, Lenka Grunclová, Petr Kopáček, Boris Turk
To ensure successful feeding tick saliva contains a number of inhibitory proteins that interfere with the host immune response and help to create a permissive environment for pathogen transmission. Among the potential targets of the salivary cystatins are two host cysteine proteases, cathepsin S, which is essential for antigen- and invariant chain-processing, and cathepsin C (dipeptidyl peptidase 1, DPP1), which plays a critical role in processing and activation of the granule serine proteases. Here, the effect of salivary cystatin OmC2 from Ornithodoros moubata was studied using differentiated MUTZ-3 cells as a model of immature dendritic cells of the host skin...
2017: Frontiers in Cellular and Infection Microbiology
https://www.readbyqxmd.com/read/28710277/phosphorylation-of-the-type-ii-transmembrane-serine-protease-tmprss13-in-hepatocyte-growth-factor-activator-inhibitor-1-and-2-mediated-cell-surface-localization
#8
Andrew S Murray, Fausto A Varela, Thomas E Hyland, Andrew J Schoenbeck, Jordan M White, Lauren M Tanabe, Sokol V Todi, Karin List
TMPRSS13 is a member of the type II transmembrane serine protease (TTSP) family. While various TTSPs have been characterized in detail biochemically and functionally, the basic properties of TMPRSS13 remain unclear. Here, we investigate the activation, inhibition, posttranslational modification, and localization of TMPRSS13. We show that TMPRSS13 is a glycosylated, active protease and that its own proteolytic activity mediates zymogen cleavage. Full-length, active TMPRSS13 exhibits impaired cell-surface expression in the absence of the cognate Kunitz-type serine protease inhibitors, hepatocyte growth factor activator inhibitor (HAI)-1 or HAI-2...
July 14, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28705940/characterisation-of-eppin-function-expression-and-activity-in-the-lung
#9
Aaron Scott, Arlene Glasgow, Donna Small, Simon Carlile, Maelíosa McCrudden, Denise McLean, Ryan Brown, Declan Doherty, Fionnuala T Lundy, Umar I Hamid, Cecilia M O'Kane, Daniel F McAuley, Malcolm Brodlie, Michael Tunney, J Stuart Elborn, Chris R Irwin, David J Timson, Clifford C Taggart, Sinéad Weldon
Eppin is a serine protease inhibitor expressed in male reproductive tissues.The aim of this study was to investigate the localisation and regulation of eppin expression in myeloid and epithelial cell lines, and explore its potential role as a multifunctional host defence protein.Using immunohistochemistry and Western blotting, eppin was detected in the lungs of patients with acute respiratory distress syndrome and cystic fibrosis lung disease. Expression of eppin in monocytic cells was unaffected by stimulation with Toll-like receptor agonists, cytokines and hormone receptor agonists...
July 2017: European Respiratory Journal: Official Journal of the European Society for Clinical Respiratory Physiology
https://www.readbyqxmd.com/read/28700665/solution-conformations-of-zika-ns2b-ns3pro-and-its-inhibition-by-natural-products-from-edible-plants
#10
Amrita Roy, Liangzhong Lim, Shagun Srivastava, Yimei Lu, Jianxing Song
The recent Zika viral (ZIKV) epidemic has been associated with severe neurological pathologies such as neonatal microcephaly and Guillain-Barre syndrome but unfortunately no vaccine or medication is effectively available yet. Zika NS2B-NS3pro is essential for the proteolysis of the viral polyprotein and thereby viral replication. Thus NS2B-NS3pro represents an attractive target for anti-Zika drug discovery/design. Here, we have characterized the solution conformations and catalytic parameters of both linked and unlinked Zika NS2B-NS3pro complexes and found that the unlinked complex manifested well-dispersed NMR spectra...
2017: PloS One
https://www.readbyqxmd.com/read/28700339/trypsin-protease-activated-receptor-2-signaling-contributes-to-pancreatic-cancer-pain
#11
Jiao Zhu, Xue-Rong Miao, Kun-Ming Tao, Hai Zhu, Zhi-Yun Liu, Da-Wei Yu, Qian-Bo Chen, Hai-Bo Qiu, Zhi-Jie Lu
Pain treatment is a critical aspect of pancreatic cancer patient clinical care. This study investigated the role of trypsin-protease activated receptor-2 (PAR-2) in pancreatic cancer pain. Pancreatic tissue samples were collected from pancreatic cancer (n=22) and control patients (n=22). Immunofluorescence analyses confirmed colocalization of PAR-2 and neuronal markers in pancreatic cancer tissues. Trypsin levels and protease activities were higher in pancreatic cancer tissue specimens than in the controls...
June 27, 2017: Oncotarget
https://www.readbyqxmd.com/read/28699813/prolylcarboxypeptidase-prcp-inhibitors-and-the-therapeutic-uses-thereof-a-patent-review
#12
Thomas H Graham
Prolylcarboxypeptidase (PrCP) is a serine protease that produces or degrades signaling proteins in several important pathways including the renin-angiotensin system (RAS), kallikrein-kinin system (KKS) and pro-opiomelanocortin (POMC) system. PrCP has the potential to be a therapeutic target for cardiovascular, inflammatory and metabolic diseases. Numerous classes of PrCP inhibitors have been developed by rational drug design and from high-throughput screening hits. These inhibitors have been tested in mouse models to assess their potential as new therapeutics...
July 12, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28697174/uv-radiation-promotes-melanoma-dissemination-mediated-by-the-sequential-reaction-axis-of-cathepsins-tgf-%C3%AE-1-fap-%C3%AE
#13
Petra Wäster, Kyriakos Orfanidis, Ida Eriksson, Inger Rosdahl, Oliver Seifert, Karin Öllinger
BACKGROUND: Ultraviolet radiation (UVR) is the major risk factor for development of malignant melanoma. Fibroblast activation protein (FAP)-α is a serine protease expressed on the surface of activated fibroblasts, promoting tumour invasion through extracellular matrix (ECM) degradation. The signalling mechanism behind the upregulation of FAP-α is not yet completely revealed. METHODS: Expression of FAP-α was analysed after UVR exposure in in vitro co-culture systems, gene expression arrays and artificial skin constructs...
July 11, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/28695302/argatroban-attenuates-diabetic-cardiomyopathy-in-rats-by-reducing-fibrosis-inflammation-apoptosis-and-protease-activated-receptor-expression
#14
Yogesh Bulani, Shyam Sunder Sharma
PURPOSE: Chronic diabetes is associated with cardiovascular dysfunctions. Diabetic cardiomyopathy (DCM) is one of the serious cardiovascular complications associated with diabetes. Despite significant efforts in understanding the pathophysiology of DCM, management of DCM is not adequate due to its complex pathophysiology. Recently, involvement of protease-activated receptors (PARs) has been postulated in cardiovascular diseases. These receptors are activated by thrombin, trypsin, or other serine proteases...
July 10, 2017: Cardiovascular Drugs and Therapy
https://www.readbyqxmd.com/read/28694438/stress-induces-more-serious-barrier-dysfunction-in-follicle-associated-epithelium-than-villus-epithelium-involving-mast-cells-and-protease-activated-receptor-2
#15
Lei Zhang, Jun Song, Tao Bai, Wei Qian, Xiao-Hua Hou
Psychological stress has been associated with intestinal epithelial hyperpermeability, the basic process in various functional and organic bowel diseases. In the present study, we aimed to clarify the differences and underlining mechanisms in stress-induced barrier disruption in functionally and structurally distinct epitheliums, including the villus epithelium (VE) and follicle-associated epithelium (FAE), a specialized epithelium overlaid the domes of Peyer's lymphoid follicles. Employing an Ussing Chamber system, the epithelial permeability was assessed in rats following water avoidance stress (WAS) in vivo and in mucosa tissues exposed to corticotropin-releasing factor (CRF) ex vivo...
July 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28690145/salivary-gland-transcripts-of-the-kissing-bug-panstrongylus-chinai-a-vector-of-chagas-disease
#16
Hirotomo Kato, Ryan C Jochim, Eduardo A Gomez, Shunsuke Tsunekawa, Jesus G Valenzuela, Yoshihisa Hashiguchi
The saliva of hematophagous arthropods injected during blood feeding contains potent pharmacologically active components to counteract the host hemostatic and inflammatory systems. In the present study, dominant salivary gland transcripts of Panstrongylus chinai, a vector of Chagas disease, were analyzed by sequencing randomly selected clones of the salivary gland cDNA library. This analysis showed that 56.5% of the isolated transcripts coded for putative secreted proteins, of which 73.7% coded for proteins belonging to the lipocalin family...
July 6, 2017: Acta Tropica
https://www.readbyqxmd.com/read/28688220/assessment-of-the-protein-interaction-between-coagulation-factor-xii-and-corn-trypsin-inhibitor-by-molecular-docking-and-biochemical-validation
#17
Badraldin K Hamad, Monika Pathak, Rosa Manna, Peter M Fischer, Jonas Emsley, Lodewijk V Dekker
BACKGROUND: Corn trypsin inhibitor (CTI) has selectivity for serine proteases coagulation factor XII (FXII) and trypsin. CTI is in widespread use as a reagent that specifically inhibits the intrinsic pathway of blood coagulation but not the extrinsic pathway. OBJECTIVES: To investigate the molecular basis of FXII inhibition by CTI. METHODS: We performed molecular docking of CTI, using its known crystal structure, with a model of the activated FXII (FXIIa) protease domain...
July 8, 2017: Journal of Thrombosis and Haemostasis: JTH
https://www.readbyqxmd.com/read/28680886/the-phosphatase-inhibitor-calyculin-a-impairs-clot-retraction-platelet-activation-and-thrombin-generation
#18
Renáta Hudák, János Vincze, László Csernoch, Ildikó Beke Debreceni, Tamás Oláh, Ferenc Erdődi, Kenneth J Clemetson, János Kappelmayer
The aim of this study was to investigate the effect of the serine/threonine protein phosphatase inhibitor, calyculin-A (CLA), on clot formation and on the procoagulant activity of human platelets. Platelet-rich plasma (PRP) samples were preincubated with buffer or CLA and subsequently platelets were activated by the protease-activated receptor 1 (PAR-1) activator, thrombin receptor activating peptide (TRAP). Clot retraction was detected by observing clot morphology up to 1 hour, phosphatidylserine- (PS-) expression was studied by flow cytometry, and thrombin generation was measured by a fluorimetric assay...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28678476/core-shell-molecularly-imprinted-polymer-nanoparticles-as-synthetic-antibodies-in-a-sandwich-fluoroimmunoassay-for-trypsin-determination-in-human-serum
#19
Jingjing Xu, Karsten Haupt, Bernadette Tse Sum Bui
We describe the application of a fluorescently labeled water-soluble core-shell molecularly imprinted polymer (MIP) for fluorescence immunoassay (FIA) to detect trypsin. p-Aminobenzamidine (PAB), a competitive inhibitor of trypsin, was immobilized in the wells of a microtiter plate enabling the capture of trypsin in an oriented position, thus maintaining its native conformation. Fluorescent MIP nanoparticles, which bound selectively to trypsin, were used for quantification. The MIP was prepared by a multistep solid-phase synthesis approach on glass beads functionalized with PAB, orientating all trypsin molecules in the same way...
July 17, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28677772/vaspin-prevents-leptin%C3%A2-induced-inflammation-and-catabolism-by-inhibiting-the-activation-of-nuclear-factor%C3%A2-%C3%AE%C2%BAb-in-rat-chondrocytes
#20
Jia-Peng Bao, Lang-Hai Xu, Ji-Sheng Ran, Yan Xiong, Li-Dong Wu
The present study aimed to investigate the function and possible underlying mechanism of various concentrations of visceral adipose tissue‑derived serine protease inhibitor (vaspin) on leptin‑induced inflammatory and metabolic responses in rat chondrocytes. Rat articular chondrocytes were isolated and treated with different concentrations of vaspin, which was followed by stimulation with leptin. The expression of genes, secretion of nitric oxide and tumor necrosis factor‑α, and activation of the nuclear factor (NF)‑κB pathway were analyzed by reverse transcription‑quantitative polymerase chain reaction, ELISA and western blotting...
September 2017: Molecular Medicine Reports
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