• SAR114137, a Cathepsin S inhibitor, did not progress past phase I for chronic pain. (wikipedia.org)
  • In 2022, STI-1558, a Cathepsin L inhibitor, received FDA clearance to begin phase I studies to treat COVID-19. (wikipedia.org)
  • Directed screening of nitrile compounds revealed 3 as a highly potent cathepsin K inhibitor but with cathepsin S activity and very poor stability to microsomes. (rcsb.org)
  • In manchen Systemen ist die durch Cathepsin D mediierte Apoptose durch seinen Inhibitor Pepstatin A hemmbar, in anderen ist die enzymatische Aktivität des Cathepsin D für seine apoptotische Involvierung entbehrlich. (uni-marburg.de)
  • In addition to our assays for studying binding of SARS-CoV-2 to the ACE2 receptor and screening for respective inhibitors/drugs (see below), we offer the Furin Activity Assay Kit & Furin Inhibitor Screening Kit as well as Cathepsin L Activity Assay Kit & Cathepsin L Inhibitor Screening Kit as tools to develop new targeted therapeutics for Covid-19. (promocell.com)
  • 2010) Identification and pre-clinical testing of a reversible cathepsin protease inhibitor reveals anti-tumor efficacy in a pancreatic cancer model. (guidetopharmacology.org)
  • 4. 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. (guidetopharmacology.org)
  • 5. Takahashi K, Ueno T, Tanida I, Minematsu-Ikeguchi N, Murata M, Kominami E. (2009) Characterization of CAA0225, a novel inhibitor specific for cathepsin L, as a probe for autophagic proteolysis. (guidetopharmacology.org)
  • 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)
  • 2008) The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett , 18 (3): 923-8. (guidetoimmunopharmacology.org)
  • 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)
  • Inhibition of the Furin protease and Cathepsin L might therefore be an efficient way to attenuate the infection process and reduce the spread and severity of COVID-19. (promocell.com)
  • Amino-acid sequence alignment and inhibition studies showed that the barley aspartic proteinase resembles mammalian lysosomal cathepsin D (EC 3.4.23.5). (lu.se)
  • 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)
  • By screening a combinatorial pentapeptide amide collection in an inhibition assay, we systematically evaluated the potential of 19 proteinogenic amino acids and seven nonproteinogenic amino acids to serve as building blocks for inhibitors of human cathepsin L. Particularly efficient were aromatic, bulky, hydrophobic amino-acid residues, especially leucine, and positively charged residues, especially arginine. (uni-bielefeld.de)
  • RNAi mediated depletion of CD44 and MT1-MMP expression and pharmacological inhibition of cathepsin K attenuated CD44 promoted invasion through a collagen I matrix. (biomedcentral.com)
  • 2017) Cathepsin S inhibition combines control of systemic and peripheral pathomechanisms of autoimmune tissue injury. (guidetoimmunopharmacology.org)
  • 2010) Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L. Bioorg Med Chem Lett , 20 (22): 6610-5. (guidetopharmacology.org)
  • Cathepsin B may function as a beta-secretase 1, cleaving amyloid precursor protein to produce amyloid beta. (wikipedia.org)
  • Osteoclasts are the bone resorbing cells of the body, and they secrete cathepsin K in order to break down collagen, the major component of the non-mineral protein matrix of the bone. (wikipedia.org)
  • The enzyme, cathepsin B (CatB), caught the attention of Li Gan at the Gladstone Institute of Neurological Disease in San Francisco several years ago when it appeared to prevent buildup of amyloid plaques in the brains of AD mice overexpressing mutant human amyloid precursor protein (APP). (alzforum.org)
  • 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)
  • This protein mediates either fusion of the virus membrane with the host cell membrane (TMPRSS2 activated mediation) or endocytosis of the virus particle (Cathepsin-activated mediation) and its entry into the cell. (promocell.com)
  • A further host protease required for activation of the S Protein is Cathepsin L which also facilitates SARS-CoV-2 entry into target cells through an alternative route. (promocell.com)
  • The S Protein is then processed/activated by the lysosomal Cathepsin L in the late endosomes (endo-lysosomes) following endocytosis of the virus. (promocell.com)
  • Specific Furin and Cathepsin L inhibitors which block proteolytic activation of the S Protein , and thus SARS-CoV-2 virus entry and replication, are potential antiviral agents to counteract SARS-CoV-2 infection and pathogenesis. (promocell.com)
  • Reacts with mouse CTSD / Cathepsin D. Cross reacts with human and rat protein. (covalab.com)
  • The encoded protein is also known as cathepsin X and cathepsin P. This gene is ubiquitously expressed in cancer cell lines and primary tumors and, like other members of this family, may be involved in tumorigenesis. (enigmadiagnostics.com)
  • The deduced amino acid sequence between the primers was identical to that reported for neutrophil cathepsin G, indicating that the protein of cutaneous mast cells previously shown to be immunologically cross-reactive with neutrophil cathepsin G has a comparable amino acid sequence. (duke.edu)
  • Quantitative real-time PCR, immuno-blotting and ELISA-based experiments have demonstrated that the transcript and protein expression of cathepsin K and MT1MMP increase in response to CD44/HA signalling in a panel of CD44-expressing breast cancer cell lines (MDA231, MDA157 and MCF7F). (biomedcentral.com)
  • Furthermore, CD44/HA signalling was shown to increase cathepsin K and MT1MMP mRNA and protein expression in the MDAMB231BO cells. (biomedcentral.com)
  • Cathepsin E Protein, Human (HEK293, His) is an approximately 46.0 kDa mouse cathepsin Dwith a His tag. (medchemexpress.com)
  • Human Cathepsin E is synthesized as a precursor protein, consisting of a signal peptide (residues 1 17), a propeptide (residues 18 53), and a mature chain (residues 54 396) [3] . (medchemexpress.com)
  • Furthermore, the discovery of Cathepsin B secretion and function as an extracellular matrix protein has broadened our appreciation for the impact of Cathepsin B on cancer progression. (edu.rs)
  • 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)
  • This invention relates to a compound of formula I and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases. (justia.com)
  • Thus, inhibitors of Cathepsin C could potentially be useful therapeutics for the treatment of neutrophil-dominated inflammatory diseases such as chronic obstructive pulmonary disease (COPD), pulmonary emphysema, asthma, multiple sclerosis, and cystic fibrosis (Guay et al. (justia.com)
  • The cysteinal lysosomal proteases, cathepsin L (CL) and cathepsin S (CS), have been shown to process invariant chain, thereby facilitating MHC class II maturation. (nih.gov)
  • Cathepsins are a class of globular lysosomal proteases playing a vital role in mammalian cellular turnover. (eurogentec.com)
  • The cathepsin family consists of 12 cysteine proteases with broad exo- and endopeptidase activity, of which Cathepsin B is a member. (eurogentec.com)
  • Neutrophils are recruited to the site of joint inflammation and release Cathepsin G, elastase and proteinase 3, proteases which are believed to be responsible for cartilage destruction associated with rheumatoid arthritis. (justia.com)
  • Cathepsin E is an aspartic protease and a member of the peptidase A1 family of proteases. (medchemexpress.com)
  • Cathepsins represent a group of such proteases aimed at maintenance of cellular homeostasis. (edu.rs)
  • Cathepsin K is the most potent mammalian collagenase. (wikipedia.org)
  • It has been surprisingly found that the bicyclic compounds of the present invention possess potent Cathepsin C activity, high selectivity against other Cathepsins, e.g. (justia.com)
  • Among the most potent novel inhibitors, one peptide, RKLLW-NH2, shares the amphiphilic character of the nonamer fragment VMNGLQNRK of the autoinhibitory, substrate-like, but reverse-binding prosegment of human cathepsin L which blocks the active center of the enzyme. (uni-bielefeld.de)
  • Highly potent inhibitors of human cathepsin L identified by screening combinatorial pentapeptide amide collections", EUROPEAN JOURNAL OF BIOCHEMISTRY , vol. 267, 2000, pp. 5085-5092. (uni-bielefeld.de)
  • Cathepsins have a vital role in mammalian cellular turnover. (wikipedia.org)
  • Finally, we discuss how insights from yeast cathepsin D and its role in regulated cell death can unveil novel functions of mammalian cathepsin D in apoptosis and cancer . (bvsalud.org)
  • Cathepsin B is a lysosomal cysteine proteinase that will hydrolyze proteins with a broad specificity for peptide bonds, but will preferentially cleave at the carboxyl side of Arg-Arg bonds in small molecule substrates. (sigmaaldrich.com)
  • 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 SensoLyte® 440 Cathepsin B Assay Kit provides a fluorogenic peptide for measurement of enzyme activity. (eurogentec.com)
  • This peptide releases the AMC (7-amino-4-methylcoumarin) fluorophore upon cathepsin B cleavage and can be detected with excitation at 354 nm and emission at 442 nm. (eurogentec.com)
  • Synthetic peptide surrounding aa 140 of mouse cathepsins D. (covalab.com)
  • Cathepsin E functions by breaking down proteins through the hydrolysis of peptide bonds at a specific peptide sequence site. (medchemexpress.com)
  • One of the less explored is the milk enzyme cathepsin D, proteolytic enzyme located in the lysosomes, which are an integral part of the somatic cells whose number varies depending on the animal's health. (srce.hr)
  • Cathepsins B, H and L have become important therapeutic targets as their proteolytic activity has been implicated in several pathological inflammatory conditions, such as arthritis and periodontitis. (guidetopharmacology.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)
  • However, cathepsin D can have both anti- and pro- survival functions depending on its proteolytic activity, cellular context and stress stimulus. (bvsalud.org)
  • Cathepsin zymography separates different cathepsins based on their migration through a polyacrylamide gel co-polymerized with a gelatin substrate. (wikipedia.org)
  • The substrate Nα-CBZ-Arg-Arg-7-amido-4-methylcoumarin is used for the fluorometric detection of Cathepsin B activity. (sigmaaldrich.com)
  • Add 50 μl of the diluted, activated Cathepsin B (0.0025 µg/well) to a black well and start the reaction by adding 50 μl of 40 μM substrate. (biolegend.com)
  • Sensitive fluorogenic substrate for the quantitative determination of cathepsin B activity. (emdmillipore.com)
  • There are, however, exceptions such as cathepsin K, which works extracellularly after secretion by osteoclasts in bone resorption. (wikipedia.org)
  • 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)
  • Cathepsin B, also known as CTSB, is a lysosomal cysteine protease. (biolegend.com)
  • While most cathepsins are exclusively endopeptidases, CTSB exhibits both carboxypeptidase and endopeptidase activities. (biolegend.com)
  • 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)
  • Cathepsin B (CTSB), a lysosomal cysteine protease, plays an important role in human physiology and pathology. (jcancer.org)
  • This study establishes the primary structure of human skin chymase and provides further evidence for the presence of a cathepsin G-like proteinase within human mast cells. (duke.edu)
  • 2. Dilute the recombinant mouse Cathepsin B to 0.05 μg/ml in assay buffer (25 mM MES, pH 5.0). (biolegend.com)
  • In addition, a broad range of other Cathepsin Assays , Cathepsin Inhibitors as well as recombinant Cathepsins , Cathepsin antibodies & ELISAs also useful to study SARS-CoV infections (e.g. (promocell.com)
  • Cathepsin D (an aspartyl protease) appears to cleave a variety of substrates such as fibronectin and laminin. (wikipedia.org)
  • Cathepsin K, among other cathepsins, plays a role in cancer metastasis through the degradation of the extracellular matrix. (wikipedia.org)
  • 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)
  • 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)
  • Wang J, Zheng M, Yang X, Zhou X, Zhang S. The Role of Cathepsin B in Pathophysiologies of Non-tumor and Tumor tissues: A Systematic Review. (jcancer.org)
  • Nevertheless, recent reports suggest that Cathepsin B executes other cellular programs such as controlling tumor growth, migration, invasion, angiogenesis, and metastases development. (edu.rs)
  • Underneath a façade of an intracellular protease with limited therapeutic potential hides a central role of cathepsins in extracellular functions. (edu.rs)
  • Here we discuss the role of Cathepsin B in the oncogenic process and perspective the use of Cathepsin B for diagnostic and therapeutic applications. (edu.rs)
  • In particular, cathepsin D is often overexpressed and hypersecreted in cancer cells , implying it may constitute a therapeutic target. (bvsalud.org)
  • The cathepsin A activity in lysates of metastatic lesions of malignant melanoma is significantly higher than in primary focus lysates. (wikipedia.org)
  • Five cyclic peptides show inhibitory activity towards human cathepsins L, B, H, and K. Several inhibitors have reached clinical trials, targeting cathepsins K and S as promising therapeutics for osteoporosis, osteoarthritis, and chronic pain. (wikipedia.org)
  • This procedure applies to all products that have a specification for Cathepsin B activity, such as product numbers C0150 and C8571 , determined by the liberation of 7-amino-4-methylcoumarin from Z-Arg-Arg 7-amido-4-methylcoumarin. (sigmaaldrich.com)
  • Cathepsin B activity was selectively elevated early in the course of illness. (jci.org)
  • Muscle wasting and impaired contractility associated with sepsis may involve selective prostaglandin stimulation of cathepsin B activity. (jci.org)
  • Immunohistochemical investigations on cathepsin D activity in structures of cholesteatoma. (medscimonit.com)
  • 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)
  • Cathepsin G Protease Assay for compound screening and profiling via fluorescence-based quantification of enzyme activity. (reactionbiology.com)
  • Cathepsins B and L are involved in matrix degradation and cell invasion. (wikipedia.org)
  • And Cathepsin E plays an important role in the degradation of proteins, the generation of bioactive proteins, and antigen processing [2] . (medchemexpress.com)
  • Cathepsin L-deficient mice were shown to have less adipose tissue, lower serum glucose and insulin levels, more insulin receptor subunits, more glucose transporter (GLUT4) and more fibronectin than wild type controls. (wikipedia.org)
  • To compare the levels of Dynamin and Cathepsin L in serum and urine of participants with proteinuric kidney disease to those of normal controls. (wits.ac.za)
  • Methods A prospective study of 37 patients with proteinuric kidney disease versus a healthy control group of 40 individuals, where the serum and urine levels of Cathepsin L and Dynamin were determined using an Enzyme Linked immunosorbent assay and the levels compared between the two groups. (wits.ac.za)
  • An independent sample t-test was used to assess whether the mean serum Dynamin, urine Dynamin, serum Cathepsin L and urine Cathepsin L differed for the control group compared with kidney disease group. (wits.ac.za)
  • There was no difference in the levels of serum Cathepsin L between the renal disease and the control groups (p= 0.23). (wits.ac.za)
  • Intracellular electrolyte changes may involve prostaglandin synthesis but do not require cathepsin B activation. (jci.org)
  • As an intracellular, hydrolytic aspartic protease, Cathepsin E is mainly expressed in cells of the immune and gastrointestinal systems, lymphoid tissues, erythrocytes, and cancer cells [1] . (medchemexpress.com)
  • UP-cDNA demonstrating amplification products for cathepsin G did not demonstrate amplification products for human neutrophil elastase, suggesting that the cathepsin G PCR amplification product was not derived from neutrophils or monocytes possibly contaminating the lesion. (duke.edu)
  • Cathepsin B has also been implicated in the progression of various human tumors including ovarian cancer. (wikipedia.org)
  • Mouse cathepsin L is homologous to human cathepsin V. Mouse cathepsin L has been shown to play a role in adipogenesis and glucose intolerance in mice. (wikipedia.org)
  • Hier sind Cathepsin G Antikörper für eine Vielzahl von Species wie anti-Human Cathepsin G, anti-Rat Cathepsin G, anti-Mouse Cathepsin G zu finden. (antikoerper-online.de)
  • Buy Purified Native Human Cathepsin G (CatG), Human Neutrophil. (athensresearch.com)
  • This random approach for the design of inhibitors was introduced to compensate for the inaccuracy induced by shifted docking of combinatorial compound collections at the active center of cathepsin L. Thereby, we obtained structurally defined pentapeptide amides which inhibited human cathepsin L at nanomolar concentrations. (uni-bielefeld.de)
  • Scholars@Duke publication: Determination of the primary structures of human skin chymase and cathepsin G from cutaneous mast cells of urticaria pigmentosa lesions. (duke.edu)
  • Amplification of the same UP-cDNA with primers coding for the NH2- and COOH-terminal sequences of human neutrophil cathepsin G also produced a specific amplification product which was sequenced. (duke.edu)
  • Cathepsin D has garnered increased attention in recent years, mainly since it has been associated with several human pathologies . (bvsalud.org)
  • Cathepsin L levels were elevated in the urine of the renal disease group, in keeping with the notion that Cathepsin L proteolysis plays a critical role in the various forms of proteinuria. (wits.ac.za)
  • In this review , we provide an overview of the role of cathepsin D in physiological and pathological scenarios. (bvsalud.org)
  • Mouse Cathepsin B, amino acids (His18-Phe339) (Accession# P10605), with C-terminal 10x His tag, was expressed in CHO cells. (biolegend.com)
  • Cathepsin K has also been shown to play a role in arthritis. (wikipedia.org)
  • Emphasis is given to the role of the yeast protease Pep4p, the vacuolar counterpart of cathepsin D , in life and death . (bvsalud.org)
  • Role of engineered metal oxide nanoparticle agglomeration in reactive oxygen species generation and cathepsin B release in NLRP3 inflammasome activation and pulmonary toxicity. (cdc.gov)
  • Therefore, specific particle parameters, i.e. preexposure dispersion status and particle surface area, of two ENM (NiO and CeO2) were used to evaluate the role of ROS generation and cathepsin B release during ENM-induced toxicity. (cdc.gov)
  • Hier sind Cathepsin G Antikörper zu finden, welche für eine bestimmte Anwendung wie WB, FACS, ELISA, IHC validiert wurde. (antikoerper-online.de)
  • In fact, elevated levels of Cathepsins are found under different pathological conditions including inflammation, infection, neurodegenerative disease, and cancer. (edu.rs)
  • Therefore, a more detailed understanding of cathepsin D regulation and how to modulate its apoptotic functions is clearly needed. (bvsalud.org)
  • Elevated levels of cathepsin B were detected in metastases and neurological disorders including Alzheimer's disease (AD). (eurogentec.com)
  • Stroke Traumatic brain injury Alzheimer's disease Arthritis Ebola, Cathepsin B and to a lesser extent cathepsin L have been found to be necessary for the virus to enter host cells. (wikipedia.org)
  • 1) You stated that there is a lack of information on other SNPs of cathepsin, after a few minutes in Clarivate's Web of Science a paper was found (10.1016/j.jpeds.2017.08.063) describing an extra cathepsin mutation (Q334P) possibly involved in pancreatitis, though not tropical calcific pancreatitis. (peerj.com)
  • The expression of cathepsin K in cultured endothelial cells is regulated by shear stress. (wikipedia.org)
  • Further experiments conducted using a parental and bone-homing subclone of the MDAMB231 cell line (MDAMB213BO) have shown that the expression of CD44, cathepsin K and MT1MMP is elevated in the MDAMB231BO cells relative to their parental counterparts. (biomedcentral.com)
  • CpG DNA inhibits the proliferation of pro-B, but not pre-B, cells by inducing caspase-independent cell death through a pathway that requires the expression of cathepsin B. This pathway is operative in Rag-deficient mice carrying an SP6 transgene, in which B lymphopoiesis is compromised, to reduce the size of the B lymphocyte precursor compartments in the bone marrow. (pasteur.fr)
  • The genetic knockout for cathepsin S and K in mice with atherosclerosis was shown to reduce the size of atherosclerotic lesions. (wikipedia.org)
  • Tatò, Maia Lucia (2019): Untersuchungen zur Rolle von Cathepsin S beim experimentellen und humanen Systemischen Lupus Erythematodes. (uni-muenchen.de)