Search results for "Peptidases"

showing 10 items of 319 documents

A three-component Mannich-type condensation leading to phosphinic dipeptides—extended transition state analogue inhibitors of aminopeptidases

2011

Abstract N-Protected α-aminoalkylphosphinic acids bearing a P–H function were found to be novel practical building blocks in three-component condensations with formaldehyde and secondary amines (amino acids). Such Mannich-type N -phosphonomethylation is a common approach for phosphorus acid derived substrates and leads to multifunctional (phosphonic/amino/carboxylic) compounds of diverse relevance. The utility of this reaction was examined for construction, in a single synthetic step, of advanced phosphinic pseudodipeptides designed to act as extended transition state analogue inhibitors of selected aminopeptidases. Phosphinomethylation of primary amino acids was less efficient and yielded …

chemistry.chemical_classificationDipeptideStereochemistryCarboxylic acidOrganic ChemistryPeptidePhosphorus acidCondensation reactionBiochemistryAmino acidchemistry.chemical_compoundtransition state inhibitorschemistryTransition state analogDrug DiscoveryphosphinomethylationaminopeptidasesMannich reactionMannich condensationTetrahedron Letters
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Calculation of the molecular masses of two newly synthesized thermostable enzymes isolated from thermophilic microorganisms

1995

Two thermostable enzymes synthesized by thermophilic microorganisms were isolated and purified. A thermostable beta-galactosidase was produced in a continuous fermentation process by Bacillus stearothermophilus TP 32 as an intracellular enzyme. After applying different concentration procedures the raw extract enzyme was prepurified on a Sephadex G-200 size exclusion column. The isolated beta-galactosidase fraction was then separated with HPLC on a TSK G 3000 SW size exclusion column to determine the molecular mass based on calibration curves of standard proteins. The other enzyme, a thermostable protease, was synthesized by Bacillus stearothermophilus TP 26 as an extracellular enzyme. After…

chemistry.chemical_classificationHot TemperatureProteaseChromatographybiologyMolecular massmedicine.medical_treatmentThermophileSize-exclusion chromatographyGeneral Chemistrybeta-Galactosidasebiology.organism_classificationBacillalesHigh-performance liquid chromatographyGeobacillus stearothermophilusMolecular WeightEnzymechemistrySephadexEndopeptidasesEnzyme StabilityChromatography GelmedicineChromatography High Pressure LiquidJournal of Chromatography B: Biomedical Sciences and Applications
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Controlled cleavage of KLH1 and KLH2 by the V8 protease from Staphylococcus aureus reassociation, electrophoretic and transmission electron microscop…

1999

The reassociation behaviour of protease V8-cleaved peptides from KLH1 and KLH2, the two hemocyanin isoforms from the giant keyhole limpet Megathura crenulata, has been studied by transmission electron microscopy of negatively stained specimens and SDS/PAGE. Reassociation of the complete mixture of protease cleavage products and of combinations of peptide fragments purified by HPLC was performed in the presence of 100 mm CaCl2 and 100 mm MgCl2 at pH 7.4, over a period of 1 to 4 weeks. The V8 protease splits KLH1 into peptide fragments containing the functional units abc, def, defg, defgh, g and h. This mixture of peptide fragments reassociated to form helical tubular polymers, with a diamete…

chemistry.chemical_classificationProteasebiologyStereochemistrymedicine.medical_treatmentProtein subunitHydrolysisSerine EndopeptidasesHemocyaninPeptideMegathura crenulatabiology.organism_classificationCleavage (embryo)BiochemistryPeptide FragmentsMicroscopy ElectronBiochemistrychemistryPolymerizationHemocyaninsmedicineProtein IsoformsElectrophoresis Polyacrylamide GelPolyacrylamide gel electrophoresisEuropean journal of biochemistry
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Immunohistochemical localization of the pro-peptide processing enzymes PC1/PC3 and PC2 in the human anal canal.

1997

Abstract HORsch, D., R. Day, N. G. Seidah, E. Weihe and M. K.-H. SchAFer. Immunohistochemical localization of the pro-peptide processing enzymes PC1/PC3 and PC2 in the human anal canal. Peptides 18(5) 755–760, 1997.—The distribution of prohormone/pro-peptide convertases PC1/PC3 and PC2 was investigated in the human anal canal by immunohistochemistry. Both prohormone convertases exhibited region-specific distribution patterns and were observed in neural and neuroendocrine cells and in nonneuroendocrine cellular elements. PC1/PC3 immunoreactivity was present in enteric neurons, subsets of nerve fibers, and neuroendocrine cells, and also in epithelial cells like intestinal stem cells, and a su…

endocrine systemPathologymedicine.medical_specialtyPhysiologyProhormoneNeuropeptideRectumAnal CanalBiologyBiochemistryImmunoenzyme TechniquesCellular and Molecular NeuroscienceEndocrinologymedicineChromograninsAspartic Acid EndopeptidasesHumansSubtilisinsAnal Transitional ZoneNeuronsNeuropeptidesAnal canalNeurosecretory SystemsEpitheliumNeoplasm Proteinsmedicine.anatomical_structureProprotein Convertase 2Fluorescent Antibody Technique DirectChromogranin AProprotein ConvertasesStem cellImmunostainingmedicine.drugPeptides
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Estudio de las bases de la resistencia a las proteínas insecticidas de bacillus thuringiensis en ostrinia nubilalis

2013

Ostrinia nubilalis (Hübner) es una de las plagas más devastadoras de los cultivos de maíz de Europa y Norte América, y a nivel económico la obtención de un control eficaz de esta plaga es un logro fundamental. En 1996, se permitió la comercialización de las plantas transgénicas que llevan insertado en el genoma un gen procedente de Bacillus thuringiensis (Berliner) (Bt) y que codifica para una proteína insecticida de las que esta bacteria produce en forma de cristales paraesporales (proteínas Cry). A partir de esta fecha, la adopción de los cultivos de maíz Bt que expresan en concreto la toxina Cry1Ab ha ido aumentando progresivamente en todo el mundo, con el resultado de que las pérdidas e…

european corn borertaladro del maiztoxinas cryUNESCO::CIENCIAS DE LA VIDAamonipeptidases ncry toxinsaminopeptidasas n:CIENCIAS AGRARIAS [UNESCO]:CIENCIAS DE LA VIDA [UNESCO]UNESCO::CIENCIAS AGRARIAS
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Influence of bioremediation stimulators in soil on development of oat seedlings (Avena sativa) and their aminopeptidase activity / Wpływ pozostałości…

2015

Abstract The selection of bioremediation techniques is important for purification of contaminated soil for agricultural use. Studies on soil contaminated with petroleum substances have indicated that the applied method of remediation has a bigger impact on the development of oat seedlings than the level of contamination. A yeast inoculum appeared to be a technique which was the friendliest to vegetation of oat

food.ingredientlcsh:Environmental protectionpetroleum residues bioremediationIndustrial chemistryGeneral MedicineBiologyAminopeptidaseSoil contaminationAvenafoodBioremediationAgronomyBotanylcsh:TD169-171.8oat seedlingsaminopeptidasesArchives of Environmental Protection
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RUNX3 and T-Bet in Immunopathogenesis of Ankylosing Spondylitis—Novel Targets for Therapy?

2019

Susceptibility to ankylosing spondylitis (AS) is polygenic with more than 100 genes identified to date. These include HLA-B27 and the aminopeptidases (ERAP1, ERAP2, and LNPEPS), which are involved in antigen processing and presentation to T-cells, and several genes (IL23R, IL6R, STAT3, JAK2, IL1R1/2, IL12B, and IL7R) involved in IL23 driven pathways of inflammation. AS is also strongly associated with polymorphisms in two transcription factors, RUNX3 and T-bet (encoded by TBX21), which are important in T-cell development and function. The influence of these genes on the pathogenesis of AS and their potential for identifying drug targets is discussed here.

lcsh:Immunologic diseases. Allergy0301 basic medicineTBX21Mini ReviewImmunologyBiologyCD8-Positive T-Lymphocytesmedicine.disease_causeAminopeptidasesInterleukin-23Polymorphism Single NucleotideAutoimmunity03 medical and health sciences0302 clinical medicineankylosing spondylitisInterleukin 23medicineImmunology and AllergyHumansImmunologic FactorsSpondylitis AnkylosingMolecular Targeted TherapyInterleukin-7 receptorTranscription factorHLA-B27 AntigenAnkylosing spondylitistherapyAntigen processingautoimmunityReceptors Interleukinmedicine.disease3. Good healthKiller Cells Natural030104 developmental biologyCore Binding Factor Alpha 3 SubunitGene Expression RegulationinflammationImmunologylcsh:RC581-607T-Box Domain ProteinsFunctional genomicsfunctional genomics030215 immunologyFrontiers in Immunology
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The NG2 Proteoglycan Protects Oligodendrocyte Precursor Cells against Oxidative Stress via Interaction with OMI/HtrA2.

2015

The NG2 proteoglycan is characteristically expressed by oligodendrocyte progenitor cells (OPC) and also by aggressive brain tumours highly resistant to chemo- and radiation therapy. Oligodendrocyte-lineage cells are particularly sensitive to stress resulting in cell death in white matter after hypoxic or ischemic insults of premature infants and destruction of OPC in some types of Multiple Sclerosis lesions. Here we show that the NG2 proteoglycan binds OMI/HtrA2, a mitochondrial serine protease which is released from damaged mitochondria into the cytosol in response to stress. In the cytosol, OMI/HtrA2 initiates apoptosis by proteolytic degradation of anti-apoptotic factors. OPC in which NG…

lcsh:MedicineApoptosisdrug effects [Cytosol]HTRA2 protein humangenetics [RNA Small Interfering]genetics [Serine Endopeptidases]genetics [Glioblastoma]570 Life sciencespathology [Glioblastoma]MiceCytosolCerebellumpathology [Cerebellum]RNA Small Interferinglcsh:Sciencemetabolism [Antigens]Mice Knockoutchondroitin sulfate proteoglycan 4metabolism [Proteoglycans]Brain NeoplasmsSerine Endopeptidasesdrug effects [Mitochondria]metabolism [Cerebellum]High-Temperature Requirement A Serine Peptidase 2Mitochondriametabolism [Brain Neoplasms]Gene Expression Regulation Neoplasticpharmacology [Antibodies Neutralizing]genetics [Mitochondrial Proteins]Proteoglycans570 BiowissenschaftenResearch ArticleProtein BindingSignal Transductionpathology [Brain Neoplasms]Primary Cell Culturedrug effects [Cerebellum]drug effects [Apoptosis]metabolism [Mitochondrial Proteins]Mitochondrial Proteinsantagonists & inhibitors [Proteoglycans]pharmacology [Hydrogen Peroxide]genetics [Antigens]Cell Line Tumormetabolism [Serine Endopeptidases]AnimalsHumansddc:610metabolism [RNA Small Interfering]Antigenslcsh:RHtra2 protein mouseHydrogen Peroxidemetabolism [Mitochondria]Antibodies Neutralizinggenetics [Proteoglycans]genetics [Brain Neoplasms]Mice Inbred C57BLOxidative Stressnervous systemlcsh:Qmetabolism [Cytosol]Glioblastomametabolism [Glioblastoma]
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Modular Solid-Phase Synthesis of Antiprotozoal Barnesin Derivatives

2020

Here, we applied and optimized a solid support (SP)-based Horner-Wadsworth-Emmons reagent to prepare SP-bound vinylogous amino acids. Subsequent SP-based peptide synthesis, global deprotection, and chemical modifications yielded 14 lipodipeptides carrying vinylogous amino acids, including the natural product barnesin A (1). Biological evaluation revealed that several synthesized derivatives show micromolar to nanomolar inhibitory activity against papain-like cysteine proteases, human cathepsin L, and rhodesain.

medicine.drug_classAntiprotozoal AgentsChemistry Techniques Synthetic010402 general chemistry01 natural sciencesBiochemistrychemistry.chemical_compoundSolid-phase synthesisPeptide synthesismedicineSolid-Phase Synthesis TechniquesHumansPhysical and Theoretical ChemistrySolid-Phase Synthesis Techniqueschemistry.chemical_classificationNatural productMolecular Structure010405 organic chemistryOrganic ChemistryCombinatorial chemistry0104 chemical sciencesAmino acidCysteine EndopeptidaseschemistryReagentAntiprotozoalCysteineOrganic Letters
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Reduced serum protease activity in Complex Regional Pain Syndrome: The impact of angiotensin-converting enzyme and carboxypeptidases.

2021

Complex Regional Pain Syndrome (CRPS) occurs in about 2% of patients after fracture of the limbs. In an earlier clinical study with 102 probands we have shown that the serum protease network in CRPS might be less effective. Based on these results we hypothesized that angiotensin-converting enzyme (ACE) and carboxypeptidase N (CPN) activity contribute to the differences of labeled bradykinin (DBK) degradation by patients' sera. Details of the enzymatic processes remained however unclear. The contributions of ACE and CPN in the serum degradation of DBK were studied using specific inhibitors. CPN1-ELISA was performed in serum. It was confirmed that the majority of DBK was degraded by ACE and C…

medicine.medical_specialtyAngiotensinsmedicine.medical_treatmentClinical BiochemistryPharmaceutical ScienceBradykininCarboxypeptidasesBradykininAnalytical Chemistrychemistry.chemical_compoundInternal medicineDrug DiscoverymedicineHumansSpectroscopyProteasebiologyCaptoprilAngiotensin-converting enzymemedicine.diseaseBlood proteinsCarboxypeptidasePathophysiologyEndocrinologyComplex regional pain syndromechemistrybiology.proteinFemaleComplex Regional Pain Syndromesmedicine.drugPeptide HydrolasesJournal of pharmaceutical and biomedical analysis
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