Inhibitors of Autoactivation of Plasma Hyaluronan-Binding Protein (Factor VII Activating Protease)
スポンサーリンク
概要
- 論文の詳細を見る
Plasma hyaluronan-binding protein (PHBP), a serine protease that can activate coagulation factor VII and prourokinase, circulates in a single-chain form (pro-PHBP) and autoproteolytically converts to an active two-chain form with the aid of an effector such as spermidine and heparin. It has been postulated that PHBP plays roles in regulating inflammation, vascular function, fibrosis and atherosclerosis. From the comprehensive screening of natural sources for inhibitors of spermidine-induced pro-PHBP autoactivation, we identified several compounds with a polyphenol feature. Of these inhibitors, tannic acid (IC50=0.020 μM), delphinidin (IC50=0.079 μM), hamamelitannin (IC50=0.19 μM), (−)-epicatechin gallate (IC50=0.24 μM), and 3,5-di-O-caffeoylquinic acid (IC50=1.0 μM) were potent and selective, and did not inhibit heparin-induced pro-PHBP autoactivation and the active form of PHBP at concentrations 100 times higher than the respective IC50 values. From evaluation of the activities of related compounds, it has been suggested that a compound with multiple aromatic rings with plural phenolic hydroxyl substituents exhibits potent activity. The inhibitory actions of delphinidin, hamamelitannin, (−)-epicatechin gallate and 3,5-di-O-caffeoylquinic acid were attenuated by catechol, a minimum polyphenol unit. Thus, it is likely that pro-PHBP binds these potent inhibitors through its site(s) that recognize a catechol-like structure. Our results would facilitate understanding of the molecular mechanism of pro-PHBP autoactivation and rational design of a compound for suppressing unregulated pro-PHBP activation.
著者
-
Nishimura Naoko
Department of Applied Biological Science, Tokyo University of Agriculture and Technology
-
Yamamoto Eisaku
Department of Applied Biological Science, Tokyo University of Agriculture and Technology
-
Okada Ken
Department Of Nuclear Medicine And Radiology Institute Of Development Aging And Cancer Tohoku Univer
-
Hasumi Keiji
Department Of Agricultural Chemistry Tokyo Noko University
-
SEKIDO Chikako
Department of Applied Biological Science, Tokyo University of Agriculture and Technology
-
Hasumi Keiji
Dep. Of Applied Biological Sci. Tokyo Noko Univ.
-
Yamamichi Shingo
Department of Applied Biological Science, Tokyo Noko University
-
Nishimura Naoko
Department Of Applied Biological Science Tokyo University Of Agriculture And Technology
-
Sekido Chikako
Department Of Applied Biological Science Tokyo University Of Agriculture And Technology
-
Nishimura Naoko
Department Of Applied Biological Science Tokyo Noko University
-
Yamamoto Eisaku
Department Of Applied Biological Science Tokyo University Of Agriculture And Technology
-
Okada Ken
Department of Applied Biological Science, Tokyo Noko University
-
Sekido Chikako
Department of Applied Biological Science, Tokyo Noko University
-
NISHIMURA Naoko
Department of Applied Biological Science, Tokyo Noko University
-
Yamamoto Eisaku
Department of Applied Biological Science, Tokyo Noko University
関連論文
- Purpurin as a Specific Inhibitor of Spermidine-Induced Autoactivation of the Protease Plasma Hyaluronan-Binding Protein
- A Novel Embolic Model of Cerebral Infarction and Evaluation of Stachybotrys microspora Triprenyl Phenol-7 (SMTP-7), a Novel Fungal Triprenyl Phenol Metabolite
- Inhibition of Glucan Synthesis by Casein Polymers Crosslinked by Glutaraldehyde
- Inhibition of Glucan Synthesis by Flavipin-crosslinked Casein Polymers
- Chemical and Functional Properties of Mutastein, an Inhibitor of Insoluble Glucan Synthesis by Streptococcus sobrinus
- Diagnosing active inflammation in the SAPHO syndrome using ^FDG-PET/CT in suspected metastatic vertebral bone tumors
- Isolation and Absolute Configuration of SMTP-0, a Simplest Congener of the SMTP Family Nonlysine-analog Plasminogen Modulators
- Inhibition of Acyl-CoA:Cholesterol Acyltransferase by Isohalobacillin, a Complex of Novel Cyclic Acylpeptides Produced by Bacillus sp.A1238
- Inhibition of the Binding of Oxidized Low Density Lipoprotein to the Macrophages by Iturin C-related Compounds
- SMTP-4D, -5D, -6D, -7D and -8D, a New Series of the Non-lysine-analog Plasminogen Modulators with a D-Amino Acid Moiety
- Evaluation of portosystemic shunt caused by patent ductus venosus through sequential whole-body scanning using per-sigmoid colon ^I-IMP scintigraphy
- A bone marrow F-18 FDG uptake exceeding the liver uptake may indicate bone marrow hyperactivity
- ^FDG uptake associated with CT density on PET/CT in lungs with and without chronic interstitial lung diseases
- Database of normal human cerebral blood flow measured by SPECT : II. Quantification of I-123-IMP studies with ARG method and effects of partial volume correction
- Database of normal human cerebral blood flow measured by SPECT : I. Comparison between I-123-IMP, Tc-99m-HMPAO, and Tc-99m-ECD as referred with O-15 labeled water PET and voxel-based morphometry
- Effects of tissue heterogeneity on cerebral vascular response to acetazolamide stress measured by an I-123-IMP autoradiographic method with single-photon emission computed tomography
- Community-acquired Acinetobacter baumannii meningitis in a previously healthy 14-month-old boy
- Inhibition of Plasminogen Activator Inhibitor-1 by 11-Keto-9(E), 12(E)-octadecadienoic Acid, a Novel Fatty Acid Produced by Trichoderma sp.
- 11-Keto-9(E), 12(E)-octadecadienoic Acid, a Novel Fatty Acid that Enhances Fibrinolytic Activity of Endothelial Cells
- Prevalence of Maternal Cytomegalovirus (CMV) Antibody and Detection of CMV DNA in Amniotic Fluid
- ヒトパルボウイルスB19感染症が関与した血小板減少性紫斑病の2例
- Inhibitors of Autoactivation of Plasma Hyaluronan-Binding Protein (Factor VII Activating Protease)
- Five-day oral cefditoren pivoxil versus 10-day oral amoxicillin for pediatric group A streptococcal pharyngotonsillitis
- Utility of a rapid diagnosis kit for Mycoplasma pneumoniae pneumonia in children, and the antimicrobial susceptibility of the isolates
- Inhibition of Plasma Hyaluronan-Binding Protein Autoactivation by Laccaic Acid
- Selective Production of Staplabin and SMTPs in Cultures of Stachybotrys microspora Fed with Precursor Amines
- Activation of Fibrinolysis by SMTP-7 and -8, Novel Staplabin Analogs with a Pseudosymmetric Structure
- Antibiotic A10255(Thioplabin) Enhances Fibrin Binding and Activation of Plasminogen
- Stachybotrydial Selectively Enhances Fibrin Binding and Activation of Glu-plasminogen
- Enhancement of Fibrinolytic Activity of Vascular Endothelial Cells by Chaetoglobosin A, Crinipellin B, Geodin and Triticone B
- Isolation, Characterization and Biological Activities of Novel Triprenyl Phenols as Pancreatic Cholesterol Esterase Inhibitors Produced by Stachybotrys sp.F-1839
- Inhibition of Plasma Hyaluronan-Binding Protein Autoactivation by Laccaic Acid
- Productivity of Monacolin K(Mevinolin)in the Genous Monascus.
- Isolation of SMTP-3, 4, 5 and -6, Novel Analogs of Staplabin, and Their Effects on Plasminogen Activation and Fibrinolysis
- Vapochromism of Ionic Dyes in Thin Films of Sugar Gels
- Isolation of Plactins A, B, C and D, Novel Cyclic Pentapeptides that Stimulate Cellular Fibrinolytic Activity
- SMTP-1 and -2, Novel Analogs of Staplabin Produced by Stachybotrys microspora IFO30018
- Clonostachin, a Novel Peptaibol That Inhibits Platelet Aggregation
- Staplabin, a Novel Fungal Triprenyl Phenol which Stimulates the Binding of Plasminogen to Fibrin and U937 Cells
- Microbial Conversion of L-Ascorbic Acid to L-Erythroascorbic Acid
- Glucosyldiacylglycerol Enhances Reciprocal Activation of Prourokinase and Plasminogen
- Enhancement of Fibrinolytic Activity of U937 Cells by Malformin A_1
- Enhancement of Reciprocal Activation of Prourokinase and Plasminogen by the Bacterial Lipopeptide Surfactins and Iturin Cs
- A Novel Embolic Model of Cerebral Infarction and Evaluation of Stachybotrys microspora Triprenyl Phenol-7 (SMTP-7), a Novel Fungal Triprenyl Phenol Metabolite
- Elucidation of Crucial Structures for a Catechol-Based Inhibitor of Plasma Hyaluronan-Binding Protein (Factor VII Activating Protease) Autoactivation
- Promoting effects of carminic acid-enriched cochineal extracts on capsular invasive thyroid carcinomas through targeting activation of angiogenesis in rats
- A new series of the SMTP plasminogen modulator with a phenylglycine-based side chain
- Structure-activity relationships of 11 new congeners of the SMTP plasminogen modulator
- Fibrinolytic Activation Promoted by the Cyclopentapeptide Malformin: Involvement of Cytoskeletal Reorganization
- A new series of the SMTP plasminogen modulators with a phenylamine-based side chain
- Pre-SMTP, a key precursor for the biosynthesis of the SMTP plasminogen modulators
- Detection of Mycoplasma pneumoniae by loop-mediated isothermal amplification (LAMP) assay and serology in pediatric community-acquired pneumonia
- Predicting human performance by channelized Hotelling observer in discriminating between Alzheimer's dementia and controls using statistically processed brain perfusion SPECT
- Assessment of the Loop-Mediated Isothermal Amplification Assay for Rapid Diagnosis of Mycoplasma pneumoniae in Pediatric Community-Acquired Pneumonia
- Clinical Manifestations of Children with Microbiologically Confirmed Pertussis Infection and Antimicrobial Susceptibility of Isolated Strains in a Regional Hospital in Japan, 2008–2012