AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and ProcessesInformation Science
CathepsinsCathepsin BCathepsin LCathepsin DCathepsin KCathepsin GCathepsin HCathepsin ECathepsin CCathepsin FCathepsin ZCysteine EndopeptidasesCathepsin WLysosomesCathepsin APepstatinsCystatinsEndopeptidasesCysteine Proteinase InhibitorsDiazomethaneDipeptidesSerine EndopeptidasesProtease InhibitorsPapainCystatin BCysteine ProteasesEnzyme PrecursorsCystatin APancreatic ElastaseLeukocyte ElastaseAmino Acid SequenceMolecular Sequence DataHydrogen-Ion ConcentrationPapillon-Lefevre DiseaseCystatin CFasciola hepaticaSubstrate SpecificityBenzoylarginine-2-NaphthylamideKineticsPeptide HydrolasesHydrolysisDipeptidyl-Peptidases and Tripeptidyl-PeptidasesLeucineElectrophoresis, Polyacrylamide GelRecombinant ProteinsMannosephosphatesOligopeptides
InhibitionCysteineExpert Opin Ther PatInhibitorsEnzymeSecrete cathepsinProteasesRecombinantMacrophagesAutophagyProteaseGlioma cellsCtssImmunologyMaturationActivityLysosomeOsteoarthritisLettEpubMRNACTSB2000P10605CleavageAutoimmunePotentRegulatesPeptidaseSerumInductionInhibitsDegradationFasciolaImmuneCitationsCancer cellTherapeuticMechanismHumanJournalSyndromeExpressionCellsRole
Inhibition9
  • Pharmacological inhibition of cathepsin activity with CA074-Me resulted in a substantial reduction of both mature IL-1β production and caspase-1 activation in infected macrophages. (frontiersin.org)
  • Moreover, cathepsin inhibition abolished the interaction between NLRP3 and ASC, measured by immunofluorescence imaging in H37Rv-infected macrophages, demonstrating a critical role of the enzyme in NLRP3-inflammasome activation. (frontiersin.org)
  • Contrary, inhibition of cathepsin S will lead to a delay in degradation of Ii and loading the antigen into MHC II as well as inappropriate presence of uncleaved Li-fragments in MHC II on the cell surface. (wikipedia.org)
  • SerpinB1 is critical for neutrophil survival through cell-autonomous inhibition of cathepsin G." Blood 121, no. 19 (2013): 3900-3907 van den Berg, Carmen W., et al. (athensresearch.com)
  • Because some experiments suggest that combining cathepsin L inhibition with regular chemotherapeutics is a promising therapeutic option for cancer therapy19 20 21 we hypothesized that cathepsin L inhibition may also be a promising tool to improve radiation therapy effectiveness. (healthanddietblog.info)
  • Our study revealed that cathepsin L inhibition could enhance the radiosensitivity of U251 cells. (healthanddietblog.info)
  • Little is known, however, about the mechanism by which the propeptide of FhCL3, a cathepsin L peptidase secreted by the infective newly excysted juveniles (NEJs), regulates the inhibition and activation of the mature enzyme before it is secreted into host tissues. (biomedcentral.com)
  • 6. Méthot N, Rubin J, Guay D, Beaulieu C, Ethier D, Reddy TJ, Riendeau D, Percival MD. (2007) Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing. (guidetoimmunopharmacology.org)
  • 2017) Cathepsin S inhibition combines control of systemic and peripheral pathomechanisms of autoimmune tissue injury. (guidetoimmunopharmacology.org)
Cysteine7
  • Cathepsin B, also known as CTSB, is a lysosomal cysteine protease. (biolegend.com)
  • Cathepsin S is a member of the peptidase C1 family of cysteine cathepsins, a lysosomal cysteine protease that may participate in the degradation of antigenic proteins to peptides for presentation to the MHC class II. (wikipedia.org)
  • Cathepsin S is a lysosomal enzyme that belongs to the papain-like protease of cysteine proteases. (wikipedia.org)
  • Purpose: Cathepsin L is a lysosomal cysteine protease that plays important roles in cancer tumorigenesis proliferation and chemotherapy resistance. (healthanddietblog.info)
  • Part of the parasite's wide-ranging virulence is attributed to the expression and secretion of large amounts of papain-like cysteine peptidases, namely cathepsin L and cathepsin B [ 3 ]. (biomedcentral.com)
  • Cysteine-type cathepsins promote the effector phase of acute cutaneous delayed-type hypersensitivity reactions. (uni-bielefeld.de)
  • Cathepsin S, is a lysosomal cysteine protease, whch plays an important role in antigen presentation. (guidetoimmunopharmacology.org)
Expert Opin Ther Pat1
  • Cathepsin B and L inhibitors: a patent review (2010 - present).Expert Opin Ther Pat. (idrblab.net)
Inhibitors4
  • Our enzyme kinetics data demonstrates high potency and selectivity of the ppFhCL3 for its cognate FhCL3 enzyme, information that could be utilised to design inhibitors of parasite cathepsin L peptidases. (biomedcentral.com)
  • Consequently, cathepsin S inhibitors are being investigated for clinical efficacy in autoimmune conditions. (guidetoimmunopharmacology.org)
  • 2. Frizler M, Schmitz J, Schulz-Fincke AC, Gütschow M. (2012) Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F. J Med Chem , 55 (12): 5982-6. (guidetoimmunopharmacology.org)
  • 4. Lee-Dutra A, Wiener DK, Sun S. (2011) Cathepsin S inhibitors: 2004-2010. (guidetoimmunopharmacology.org)
Enzyme4
  • In vitro, cathepsin S retains some enzyme activity in the presence of 3M urea. (wikipedia.org)
  • Cathepsin L (Cat L) enzyme, found in all stages of the liver flukes, plays a significant role in the biological functions of the parasites, such as migration, nutrition, and immune evasion ( 2 ). (brieflands.com)
  • Finally and as a possible consequence of these alterations in lysosomal enzyme transport, cathepsin L and D maturation were found suppressed in CLN3 cells. (ac.ir)
  • A treatment known as MIV-711 targets an enzyme called cathepsin K that is thought to play a role in the destruction of cartilage and the breakdown of too much bone. (medscape.com)
Secrete cathepsin1
  • Immune cells, including macrophages and microglia, secrete cathepsin S in response to inflammatory mediators including lipopolysaccharides, proinflammatory cytokines and neutrophils. (wikipedia.org)
Proteases4
  • In contrast, cortical thymic epithelial cells do not express cathepsin S. While pH optima of many lysosomal proteases are acidic, cathepsin S is an exception. (wikipedia.org)
  • While lysosomal proteases terminally degrade proteins in lysosomes, cathepsin S has own distinctive physiological role. (wikipedia.org)
  • Chronologically, action of cathepsin S follows two cleavages performed by aspartyl proteases. (wikipedia.org)
  • Recent studies have shown that the high concentration of activated neutrophils in the ILT of AAA are associated with high levels of proteolytic enzymes including cathepsins, elastases, collagen proteases, and other metalloproteinases. (cardiologyonline.com)
Recombinant3
  • 1. Dilute the recombinant mouse Cathepsin B to 10 μg/ml in activation buffer (25 mM MES, 1 mM DTT, pH 5.0) and incubate the protein at 25°C for 3 min. (biolegend.com)
  • 2. Dilute the recombinant mouse Cathepsin B to 0.05 μg/ml in assay buffer (25 mM MES, pH 5.0). (biolegend.com)
  • The yeast Pichia pastoris expression system was investigated for the production of human cathepsin C (CatC) recombinant protein. (iyte.edu.tr)
Macrophages5
  • Cathepsin S can function as an elastase over a broad pH range in alveolar macrophages. (wikipedia.org)
  • Cathepsin S is expressed by antigen presenting cells including macrophages, B-lymphocytes, dendritic cells and microglia. (wikipedia.org)
  • In macrophages, cathepsin S can be replaced by cathepsin F. Secreted cathepsin S cleaves some extracellular matrix (ECM) proteins. (wikipedia.org)
  • Cathepsin S is expressed in the lysosome of antigen presenting cells (dendritic cells, B-cells and macrophages) where it processes the invariant chain-MHC-II complex (a chaperone protein that prevents premature peptide loading) inside antigen presenting cells and in this way controls antigen presentation. (guidetoimmunopharmacology.org)
  • We identified the activity of the lysosomal protease cathepsin B in macrophages as a rate-limiting factor in degrading asparaginase both in vitro and in vivo. (nih.gov)
Autophagy2
  • We observed the changes of autophagy level in NSCLC cells under the effect of FJHQ, and verified the level of the autophagy marker protein and cathepsin. (biomedcentral.com)
  • Bafilomycin A1 (BafA1) is an inhibitor of vesicle-type ATPase, which can interfere with the fusion of autophagy vesicles and lysosomes, as well as inhibit lysosomal acidification, affecting cathepsin maturation [ 12 ]. (biomedcentral.com)
Protease2
  • The nociceptive activity results from cathepsin S functioning as a signaling molecule via activation of protease-activated receptors 2 and 4 members of the G-protein coupled receptor family. (wikipedia.org)
  • 2010) Identification and pre-clinical testing of a reversible cathepsin protease inhibitor reveals anti-tumor efficacy in a pancreatic cancer model. (guidetoimmunopharmacology.org)
Glioma cells2
Ctss1
  • Cathepsin S is a protein that in humans is encoded by the CTSS gene. (wikipedia.org)
Immunology1
  • I moved to UMB in October 2017 as an associate professor in Microbiology and Immunology. (umaryland.edu)
Maturation1
  • Co-localization experiments further showed that while FJHQ did not inhibit autophagosome and lysosome fusion, it affected the maturation of cathepsin and thus inhibited the autophagic pathway. (biomedcentral.com)
Activity12
  • The activity of Cathepsin B is determined by its ability to cleave the fluorogenic peptide substrate, Z-Leu-Arg-AMC (Z=Benzyloxycarbonyl, and AMC=7-amino-4-methylcoumarin) after activation. (biolegend.com)
  • The activity of cathepsin S is tightly regulated by its endogenous inhibitor, cystatin C, which also has a role in antigen presentation. (wikipedia.org)
  • Cystatin A and B have a lower activity compared to cystatin C. The active cleavage sites -(-Val-Val-Arg-)- of cathepsin S are supposed to have at least two amino acids surrounding it from each side. (wikipedia.org)
  • Cathepsin S expression and activity has also been shown to be upregulated in the skin of psoriasis patients. (wikipedia.org)
  • Results: Serum TRAcP5b activity, but not cathepsin K-immunoreactivity, was associated with density of TRAcP-positive osteoclasts in the subchondral bone of medial tibia plateaux. (nottingham.ac.uk)
  • By contrast other studies have also reported that increased cathepsin L activity is associated with cancer cell death17 18 From these contradictory results LMK-235 we considered that the effect of cathepsin L on tumors remains unclear. (healthanddietblog.info)
  • Immunohistochemical investigations on cathepsin D activity in structures of cholesteatoma. (medscimonit.com)
  • Background:Serum cathepsin B activity has been considered a potential marker of tumor progression. (medscimonit.com)
  • The aim of this study was to assess serum cathepsin activity during tumor progression and regression.Material/Methods: Of 60 female rats inoculated with Morris hepatoma cells, 45 were treated with BRT, and the remaining 15 were left without treatment. (medscimonit.com)
  • Serum cathepsin B activity was determined, tumor volumes were measured, and histological examinations of the tumor tissues were performed.Results: Of the 45 BRT-treated rats, tumor regression was observed in 31 rats, and serum cathepsin activity was analyzed in these rats. (medscimonit.com)
  • To measure lysosomal Cathepsin B activity, cells were incubated with Magic Red CathepsinB (ImmunoChemistry Technologies, Cat#: 938) for 1 hr according to the manufacturer's instructions. (immunochemistry.com)
  • Enzymatic activity assay Cathepsin L activity in living cells was monitored using the Magic Red Cathepsin L detection kit (ImmunoChemistry Technologies, MN, USA). (immunochemistry.com)
Lysosome2
  • In contrast, cathepsin S remains stable and has a physiological role outside the lysosome. (wikipedia.org)
  • HF-SCS restored lysosomal function, increased the levels of lysosome-associated membrane protein 2 (LAMP2) and the mature form of cathepsin D (matu-CTSD), and alleviated the abnormally elevated levels of microtubule-associated protein 1A/B-light chain 3 (LC3)-II and sequestosome 1 (P62) in spinal nerve-injured rats. (iasp-pain.org)
Osteoarthritis1
  • Objectives: To investigate serum biomarkers, tartrate resistant acid phosphatase 5b (TRAcP5b) and cathepsin K, indicative of osteoclastic bone resorption, and their relationship to pain and pain change in knee osteoarthritis (OA). (nottingham.ac.uk)
Lett1
Epub1
MRNA2
  • Determination of cathepsin L mRNA levels by RT-PCR Total RNA was isolated using TRIzol Reagent (Invitrogen Carlsbad CA USA) according to the manufacturer's instructions. (healthanddietblog.info)
  • Homo sapiens cathepsin C (CTSC), transcript variant 1, mRNA. (lu.se)
CTSB3
  • Lysosomal cathepsin B (CTSB) has been proposed to play a role in the induction of acute inflammation. (frontiersin.org)
  • These observations suggest that during Mtb infection, lysosomal release of activated CTSB and possibly other cathepsins inhibitable by CA07-Me is critical for the induction of inflammasome-mediated IL-1β processing by regulating NLRP3-inflammasome assembly in the cytosol. (frontiersin.org)
  • While most cathepsins are exclusively endopeptidases, CTSB exhibits both carboxypeptidase and endopeptidase activities. (biolegend.com)
20001
  • The insert sequences used were as follows: 5 and 5 A non-silencing RNA was used as the control treatment (5′-CACCGTATGACAACAGCCTCAAGTTCAAGAGACTTGAGGCTGTTGTCATACTTTTTTG-3′ 5 Transfection and isolation of stable cell clones To obtain stable clones cells were transfected with control shRNA or cathepsin L shRNA using Lipofectamine 2000 (Invitrogen Carlsbad CA USA) with stably transfected cell clones designated U251-Con shRNA and U251-Cathepsin L shRNA respectively. (healthanddietblog.info)
P106051
  • Mouse Cathepsin B, amino acids (His18-Phe339) (Accession# P10605), with C-terminal 10x His tag, was expressed in CHO cells. (biolegend.com)
Cleavage1
  • For instance, cleavage of laminin-5 by cathepsin S leads to generation of proangiogenic peptides. (wikipedia.org)
Autoimmune1
  • Thus, we can speculate that overexpression of cathepsin S may lead to premature degradation of Ii, occasional loading of MHC II and an autoimmune attack. (wikipedia.org)
Potent1
  • Cathepsin S may be considered the most potent elastase known. (wikipedia.org)
Regulates1
  • Cathepsin D regulates cathepsin B activation and disease severity predominantly in inflammatory cells during experimental pancreatitis. (uni-bielefeld.de)
Peptidase1
  • Dipeptidyl-peptidase I precursor (EC 3.4.14.1) (DPP-I) (DPPI) (Cathepsin C) (Cathepsin J) (Dipeptidyl transferase). (lu.se)
Serum1
  • Serum Levels of a Cathepsin-K Generated Periostin Fragment Predict Incident Low-Trauma Fractures in Postmenopausal Women Independently of BMD and FRAX. (viollier.ch)
Induction1
Inhibits1
Degradation2
  • Cathepsin S participates in the degradation of the invariant or Ii chain that prevents loading the antigen into the complex. (wikipedia.org)
  • Cell surface biotinylation after EGF (2 ng/mL) stimulation, EGF phosphorylation (Tyr-845), retromer and cation-independent mannose-6-phosphate receptor (CI-MPR) levels and stability, EGF degradation pathways and cathepsin L and D levels were analysed by western blots. (ac.ir)
Fasciola2
Immune1
  • 2017). Differential expression of Cathepsin E in transthyretin amyloidosis: From neuropathology to the immune system . (up.pt)
Citations1
Cancer cell2
  • Conclusions: Cathepsin B may play an important role, not only in tumor expansion, but also during the processes of cancer cell death and resorption. (medscimonit.com)
  • Cancer Cell, 2017 Oct 9. (nih.gov)
Therapeutic1
Mechanism1
  • Unexpected cross-reactivity of anti-cathepsin B antibodies leads to uncertainties regarding the mechanism of action of anti-CD20 monoclonal antibody GA101. (uni-bielefeld.de)
Human3
Journal1
  • Surface cathepsin B protects cytotoxic lymphocytes from self-destruction after degranulation", JOURNAL OF EXPERIMENTAL MEDICINE , vol. 196, 2002, pp. 493-503. (uni-bielefeld.de)
Syndrome1
  • Roche's cathepsin S inhibitor petesicatib (RO5459072 or RG7625) completed Phase 2 clinical evaluation in Sjögren's syndrome ( NCT02701985 ) and Phase 1 in celiac disease ( NCT02679014 ), but there are no active clinical trials registered with ClinicalTrials.gov . (guidetoimmunopharmacology.org)
Expression2
  • The expression of cathepsin S can be triggered by proinflammatory factors secreted by tumor cells. (wikipedia.org)
  • Construction of shRNA expression plasmids Annealed sets of oligonucleotides encoding short hairpin transcripts that correspond LMK-235 to cathepsin L were ligated into a vector according to the manufacturer's instructions (Ambion Life Technologies Austin TX USA) to generate the knockdown vector. (healthanddietblog.info)
Cells1
  • Cathepsin S is expressed by some epithelial cells. (wikipedia.org)
Role2
  • Cathepsin S plays an active role in blood vessels permeability and angiogenesis due to its elastolytic and collagenolytic activities. (wikipedia.org)
  • Whether it has a definitive role in causing the pathology of psoriasis is as yet unknown, however in the same study it was shown to specially cleave and activate the psoriasis-associated proinflammatory cytokine IL-36γ Cathepsin S has a role in nociception, including itch and gastrointestinal pain. (wikipedia.org)