Protease inhibitorProteasesInhibition of cathepsinSelectivityCell-permeable calpain inhibitorHighly potentLysosomal cysteineCalpainEnzymeReversibleIntracellularNitrile inhibitorsSmall molecule inhibitorIrreversiblePapainOrally activeElastase2017AutophagyRecombinantRegulatesOdanacatibMatrix metalloproteinaseProteinProteolyticPeptideCompoundsMicrotubuleSynthesisMaturationHumanCtssCTSBLigandHSP90PeptidaseActivityPotentiallyActivatorAgonistTherapiesCancersCells
Protease inhibitor8
- Cathepsin B may enhance the activity of other proteases, including matrix metalloproteinase, urokinase (serine protease urokinase plasminogen activator), and cathepsin D, and thus it has an essential position for the proteolysis of extracellular matrix components, intercellular communication disruption, and reduced protease inhibitor expression. (wikipedia.org)
- We recognized that if the nitrile functional group of a protease inhibitor could be bound in a stable fashion to a metal center it would likely be inert towards attack by active site cysteines. (sciencepop.org)
- SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor. (ejbio.org)
- 2010) Identification and pre-clinical testing of a reversible cathepsin protease inhibitor reveals anti-tumor efficacy in a pancreatic cancer model. (guidetoimmunopharmacology.org)
- 2021) A Clinical-Stage Cysteine Protease Inhibitor blocks SARS-CoV-2 Infection of Human and Monkey Cells. (guidetoimmunopharmacology.org)
- Z-FA-FMK is an irreversible cysteine protease inhibitor. (adooq.com)
- Cysteine Protease inhibitor is an inhibitor of cysteine protease. (adooq.com)
- Leupeptin is a reversible protease inhibitor known to target various cathepsins, calpain and trypsin. (agscientific.com)
Proteases7
- Cathepsin B belongs to a family of lysosomal cysteine proteases known as the cysteine cathepsins and plays an important role in intracellular proteolysis. (wikipedia.org)
- 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)
- Selective Dual Inhibitors of the Cancer-Related Deubiquitylating Proteases USP7 and USP47. (glpbio.com)
- Herein, the synthesis of a new scaffold useful for the preparation of peptidyl-AOMKs is reported and it is demonstrated that the new synthetic probes bearing a 4-functionalized 2,6-dimethylbenzoate efficiently inhibit cysteine proteases like cathepsin B. (thieme-connect.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)
- We describe the application of ligand based virtual screening technologies towards the discovery of novel plasmepsin (PM) inhibitors, a family of malarial parasitic aspartyl proteases. (cardiff.ac.uk)
- MG-101 (ALLN) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins. (adooq.com)
Inhibition of cathepsin3
- 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)
- Inhibition of cathepsin K is a novel approach to the treatment of osteoporosis that differs from those of currently approved treatments. (healthnewstrack.com)
- Overall, the results of this study demonstrate the molecular, kinetic, and protease specificity features of CA-074 pH-dependent inhibition of cathepsin B. (bvsalud.org)
Selectivity8
- Synthetic derivatization of the initial hit led to a more potent agent, 2-(fluorosulfonyl)phenyl fluorosulfate with IC 50 0.24 μM and greater than 833-fold selectivity over the homologous neutrophil serine protease, cathepsin G. The optimized, yet simple benzenoid probe only modified active hNE and not its denatured form. (nih.gov)
- 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)
- Upon photolysis the nitrile-based inhibitor is definitely unleashed providing high levels of selectivity for enzyme inhibition under light vs. dark conditions. (sciencepop.org)
- To gain in-depth knowledge of CA-074 inhibition under these different pH conditions, this study evaluated the molecular features, potency, and selectivity of CA-074 for cathepsin B inhibition under acidic and neutral pH conditions. (bvsalud.org)
- These values are at least 1000-fold lower than those K i obtained for human cathepsin L (HsCL) and human cathepsin K (HsCK) demonstrating the selectivity of the ppFhCL3 for parasite cathepsins L. By exploiting 3-D structural data we identified key molecular interactions in the specific binding between the ppFhCL3 and FhCL3 mature domain. (biomedcentral.com)
- 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)
- The virtual hits were biologically assessed for activity and selectivity using whole cell Plasmodium falciparum parasites and on target in PM II, PM IV and the closely related human homologue, Cathepsin D assays. (cardiff.ac.uk)
- PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 uM for μ-Calpain, about 20-fold selectivity over m-calpain. (adooq.com)
Cell-permeable calpain inhibitor2
- Calpeptin is a cell permeable calpain inhibitor. (adooq.com)
- MDL-28170 is a potent and selective cell permeable calpain inhibitor which inhibits the oxidative damage-induced apoptosis in PC12 cells and capsaicin-induced apoptosis in dorsal root ganglion neurons (1). (mayflowerbio.com)
Highly potent3
- 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)
- 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)
- 2) A highly potent microtubule inhibitor, monomethyl auristatin E. 3) A drug activation/release mechanism using a linker cleavable by cathepsin B, which we demonstrate to be abundant in the tumor microenvironment. (monash.edu)
Lysosomal cysteine3
- CA-074 is a selective inhibitor of cathepsin B, a lysosomal cysteine protease. (bvsalud.org)
- Promising candidates are lysosomal cysteine cathepsins, proteolytical enzymes involved in various critical steps during cancer progression. (bvsalud.org)
- Cathepsin S, is a lysosomal cysteine protease, whch plays an important role in antigen presentation. (guidetoimmunopharmacology.org)
Calpain7
- Acetyl-Calpastatin (184-210) (human), selective calpain inhibitor. (adooq.com)
- Strongly inhibits calpain I (Ki = 0.2 nM) and II but does not inhibit papain, trypsin and cathepsin L (Ki = 6 uM). (adooq.com)
- Calpain Inhibitor II, ALLM is a cell-permeable inhibitor of calpain I, calpain II, cathepsin L and cathepsin B with Ki values of 120 nM, 230 nM, 0.6 nM and 100 nM, respectively. (adooq.com)
- MDL 28170 is a cell permeable selective inhibitor of Calpain 1, a Ca2+-dependent cysteine protease which has been implicated in apoptosis of immune cells as well as neuronal cells. (adooq.com)
- SJA6017 is a cell permeable peptide aldehyde which functions as a reversible calpain inhibitor. (adooq.com)
- PD 150606 is a cell-permeable, non-competitive, selective, non-peptide Ca2+ dependent calpain inhibitor for calpain-1 and for calpain-2 directed towards the Ca2+ binding sites of calpain. (adooq.com)
- in isolated enzyme assays Calpain I has a Ki = 8 nM and Cathepsin B has a Ki = 24 nM with an IC50 = 0.3 µM in intact cell assay (4). (mayflowerbio.com)
Enzyme9
- 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)
- 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)
- Odanacatib selectively inhibits the cathepsin K enzyme believed to play a central role in osteoclastic bone resorption, particularly in the degradation of the protein component of bone. (healthnewstrack.com)
- Thus metal binding would cage the inhibitor which could be buy 51014-29-0 released upon photolysis to interact with the target enzyme (Figure 1). (sciencepop.org)
- Finding a combination of stereoisomers will not influence enzyme inhibition because 1 can be released from 2 during photolysis and [RuII(bpy)2(H2O)2]2+ will not become a powerful inhibitor (vide infra). (sciencepop.org)
- Deubiquitylating enzyme, cathepsin B and 20S proteasome chymotrypsin like protease activities are measured. (glpbio.com)
- 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)
- SB 204990 is an effective and specific ATP citrate lyase enzyme inhibitor. (targetmol.com)
- We also consider the novel attributes of the NS3 protease-binding pocket that challenged development of small molecule inhibitors, and the studies that ultimately yielded milligram quantities of this enzyme in a soluble, tractable form suitable for inhibitor screening programs. (xiahepublishing.com)
Reversible1
- Furthermore, the simultaneous inhibition of both cathepsins B and X with potent, selective, reversible inhibitors exerted a synergistic effect in impairing processes of tumor progression in in vitro cell-based assays of tumor cell migration and spheroid growth. (bvsalud.org)
Intracellular6
- Intracellular electrolyte changes may involve prostaglandin synthesis but do not require cathepsin B activation. (jci.org)
- Open in a separate window Physique 1 Pioglitazone (Actos) Intracellular levels of elastase and cathepsin G in PMNLs measured in whole blood. (oscars2019info.com)
- Pioglitazone (Actos) (b, c) Representative histogram of flow cytometry showing intracellular elastase and cathepsin G intensity in HD and NC PMNLs, respectively. (oscars2019info.com)
- d, e) PMNL intracellular elastase and cathepsin G from NC subjects and HD patients detected by flow cytometry (= 10). (oscars2019info.com)
- A significant negative correlation was found between the fluorescent intensity of intracellular elastase and cathepsin G and membrane CD11b expression on PMNLs, (= ?0.43 and = ?0.51, resp. (oscars2019info.com)
- Immunohistochemical Staining of Elastase and Cathepsin G in PMNLs The intracellular levels and locations of elastase and cathepsin G were also evaluated by immunohistochemical staining of PMNLs in smears of whole blood, as represented in Physique 2. (oscars2019info.com)
Nitrile inhibitors3
- WO2004110988 discloses peptidyl nitrile inhibitors as dipeptidyl-peptidase I (DPPI) inhibitors for the treatment of a series of diseases. (justia.com)
- WO2009074829 and WO2010142985 also disclose peptidyl nitrile inhibitors as dipeptidyl-peptidase I (DPPI) inhibitors for the treatment asthma, COPD or allergic rhinitis. (justia.com)
- 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)
Small molecule inhibitor3
- In this review, we describe the key scientific discoveries that led to the approval of boceprevir, a first-generation, selective, small molecule inhibitor of the NS3 protease. (xiahepublishing.com)
- In this paper, we focus on the studies that contributed to our present knowledge of the structure and replication of HCV, and the subsequent development of boceprevir as a selective small molecule inhibitor of the NS3 protease. (xiahepublishing.com)
- By using RNAi and small molecule inhibitor approaches, we also confirmed that G9a is the major methyltransferase to catalyze H3K27me1 for MMP-9-dependent H3NT proteolysis and trigger the expression of osteoclast-specific genes. (biomedcentral.com)
Irreversible4
- Potent, irreversible inhibitor of PI 3-kinase. (tocris.com)
- Under these acidic and neutral pH conditions, CA-074 maintained its specificity for cathepsin B over other cysteine cathepsins, displayed irreversible inhibition, and inhibited diverse cleavages of peptide substrates of cathepsin B assessed by profiling mass spectrometry. (bvsalud.org)
- Peptidyl-acyloxymethyl ketones (AOMKs) belong to a class of selective, irreversible inhibitors (activity-based probes) widely used as chemical tools of investigating proteins, for example, in activity-based protein profiling. (thieme-connect.com)
- CA-074 methyl ester is a cell-permeable analog of CA-074 that acts as an irreversible cathepsin B inhibitor. (adooq.com)
Papain2
- C1: Papain: cathepsin Z. Last modified on 28/07/2015. (guidetopharmacology.org)
- 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)
Orally active1
- 2-Furoic acid, an orally active selective human cathepsin K inhibitor, may have the therapeutic potential for the treatment of diseases characterized by excessiv. (targetmol.com)
Elastase10
- We report here a SuFEx-enabled, agnostic approach for the discovery and optimization of covalent inhibitors of human neutrophil elastase (hNE). (nih.gov)
- Examination of the cells under a light microscope revealed that elastase and cathepsin G were abundant and distributed in PMNLs of NC, while sparse in HD PMNLs, and even missing in some patients. (oscars2019info.com)
- Open in a separate windows Physique 2 Localization of elastase and cathepsin G in PMNLs in whole blood smears. (oscars2019info.com)
- Indirect immunostaining of elastase (aCd) and cathepsin G (eCh) in blood smears of two NC subjects and two HD patients (light microscopy, magnification 100). (oscars2019info.com)
- Plasma Levels of Elastase and Cathepsin G Plasma of NC and HD was depleted of albumin and immunoglobulins in order to enrich it with elastase and cathepsin G. After depletion, plasma proteins were separated on SDS-PAGE followed by western blot analysis (Physique 3). (oscars2019info.com)
- HD plasma contained higher levels of free elastase and cathepsin G (30?KDa) than NC plasma (common of 1 1.3 0.14 versus 0.76 0.08 relative density units, resp. (oscars2019info.com)
- A significant negative correlation was found between the amounts of the plasma levels of elastase and cathepsin G (30?KDa) and their levels in PMNLs (Figures 3(d) and 3(e)) (= ?0.5 and = ?0.6, resp. (oscars2019info.com)
- Open in KLF10 a separate windows Physique 3 Levels of elastase and cathepsin G in HD and NC plasma. (oscars2019info.com)
- a) A representative western blot of elastase and cathepsin G. Bands were visible at 30?kDa (inhibitor unbound) and higher M.W Pioglitazone (Actos) complexes of 40, 50, and 70?kDa in NC and HD plasma. (oscars2019info.com)
- b), (c)) Densities of unbound elastase and cathepsin G. (oscars2019info.com)
20171
- 2017) Cathepsin S inhibition combines control of systemic and peripheral pathomechanisms of autoimmune tissue injury. (guidetoimmunopharmacology.org)
Autophagy5
- In this study, we clarified that Fangjihuangqi Decoction (FJHQ, traditional Chinese medicine) is an autophagy inhibitor, which can synergistically enhance the effect of cisplatin and paclitaxel on non-small cell lung cancer (NSCLC) cells. (biomedcentral.com)
- 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)
- Collectively, these results demonstrate that FJHQ is a novel late-stage autophagy inhibitor that can amplify the anti-tumor effect of cisplatin and paclitaxel against NSCLC cells. (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)
- Unfortunately, due to their high toxicity, the use of autophagy inhibitors is limited in clinical applications. (biomedcentral.com)
Recombinant1
- BMS-303141 is a potent ATP-citrate lyase (ACL) inhibitor (IC50: 0.13 uM, human recombinant ACL). (targetmol.com)
Regulates1
- Cathepsin D regulates cathepsin B activation and disease severity predominantly in inflammatory cells during experimental pancreatitis. (uni-bielefeld.de)
Odanacatib2
- 2 year data from a Phase IIB study of odanacatib (formerly MK-0822), an investigational, selective cathepsin-K inhibitor in development for the treatment of osteoporosis by Merck & Co., Inc., demonstrated dose-dependent increases in bone mineral density (BMD) at the total hip, lumbar spine and femoral neck fracture sites and decreased indices of bone resorption compared to placebo in postmenopausal women with low BMD. (healthnewstrack.com)
- 2008) The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett , 18 (3): 923-8. (guidetopharmacology.org)
Matrix metalloproteinase2
- Saikosaponins A and D inhibited the formation of resorptive pits by reducing the secreted levels of matrix metalloproteinase- (MMP-) 2, MMP-9, and cathepsin K in RANKL-induced osteoclasts. (hindawi.com)
- Thus, emerging therapies, including cathepsin K, matrix metalloproteinase, or nonreceptor tyrosine kinase Src inhibitors, are being introduced for prevention and treatment of osteoporosis and cancer bone metastasis. (hindawi.com)
Protein4
- In addition, it down-regulated the activity of key enzymes known to be crucial for the entry of the SARS-CoV-2 virus, such as TMPRSS2, furin and cathepsin L, but not their expression at protein level. (ejbio.org)
- Our results confirm that cathepsin-B inhibition is compensated by an increase in cathepsin X activity and protein levels. (bvsalud.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)
- Free shipping on inhibitor and protein orders over $500. (adooq.com)
Proteolytic1
- Attenuation of cathepsin B (CATB) proteolytic activity and/or inhibition serves as a potential therapeutic target in cancer metastasis. (bvsalud.org)
Peptide1
- Cathepsin B is synthesized on the rough endoplasmic reticulum as a preproenzyme of 339 amino acids with a signal peptide of 17 amino acids. (wikipedia.org)
Compounds2
- Evaluation of our ever-growing collection of SuFExable compounds toward various biological assays unexpectedly revealed a selective and covalent hNE inhibitor: benzene-1,2-disulfonyl fluoride. (nih.gov)
- Pharmacophore queries were used to screen vendor libraries in search of active and selective compounds. (cardiff.ac.uk)
Microtubule1
- Hypothesizing that activated platelets in the tumor microenvironment provide a targeting epitope for tumor-directed chemotherapy, we developed an antibody-drug conjugate (ADC), comprised of a single-chain antibody (scFv) against the platelet integrin GPIIb/IIIa (scFvGPIIb/IIIa) linked to the potent chemotherapeutic microtubule inhibitor, monomethyl auristatin E (MMAE). (monash.edu)
Synthesis1
- Citations to Inhibitors of prostaglandin synthesis or cathepsin B prevent muscle wasting due to sepsis in the rat. (jci.org)
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)
Human5
- 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)
- 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)
- Cathepsin B in numerous human disease mechanisms involves its translocation from acidic lysosomes of pH 4.6 to neutral pH 7.2 of cellular locations, including the cytosol and extracellular environment. (bvsalud.org)
- Induction of cathepsin B by the CXCR3 chemokines CXCL9 and CXCL10 in human breast cancer cells. (uni-bielefeld.de)
- NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay),indirectly disrupting citrate binding vi. (targetmol.com)
Ctss1
- Cathepsin S, also known as CTSS, contains an active cysteine residue in the buy uroxatral 24x7 active situate in the direction of the volume of intrastallular and additionalroomular pbalderdasheins. (upb.ro)
CTSB4
- In humans, cathepsin B is encoded by the CTSB gene. (wikipedia.org)
- Entrez Gene: CTSB cathepsin B". Kirschke H, Barrett AJ, Rawlings ND (1995). (wikipedia.org)
- 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)
Ligand1
- Bisphosphonates and denosumab, a receptor activator of nuclear factor kappa-B ligand (RANKL) inhibitor, delay time to first skeletal related event. (hindawi.com)
HSP901
- Additional studies are subsumed under the aegis character in our lab in animal xenograft models of core and cheapest uroxatral online paypal prostate cancer to verify and validate in vivo the yield sigvariety to treatment buy uroxatral now with PI3K and HSP90 inhibitors using on cloud nine resolution magic oblique spinning (HR-MAS) MRS and MR spectroscopic imaging. (upb.ro)
Peptidase2
- 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)
- Taken together, our data demonstrate that Z9 impairs tumor progression both in vitro and in vivo and can be used in combination with other peptidase inhibitors as an innovative approach to overcome resistance to antipeptidase therapy. (bvsalud.org)
Activity5
- 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)
- While high levels of CA-074 or CA-074Me (converted by cellular esterases to CA-074) are used in biological studies to inhibit cathepsin B at both acidic and neutral pH locations, it is possible that adjusted levels of CA-074 or CA-074Me may be explored to differentially affect cathepsin B activity at these different pH values. (bvsalud.org)
- One of the mechanisms by which cathepsin X contributes to cancer progression is the compensation of cathepsin-B activity loss. (bvsalud.org)
- D), illustrating that NO donors improve ventricular Glyoxalase (GLO) Synonyms sarcKATP channel activity but the enhancement is reversed in the presence of inhibitors selective for sGC or PKG. (cathepsin-s.com)
Potentially1
- Cathepsin B has been proposed as a potentially effective biomarker for a variety of cancers. (wikipedia.org)
Activator1
- 3.The higher the number of " * " is, the more potent the inhibitor or activator is. (adooq.com)
Agonist1
- MEDICA16 is a selective agonist for GPR40 as well as a partial agonist for GPR120. (targetmol.com)
Therapies1
- Given its critical role in the replication of HCV, the NS3 protease has been recognized as a potential drug target for the development of selective HCV therapies. (xiahepublishing.com)
Cancers3
- Cathepsin B is upregulated in certain cancers, in pre-malignant lesions, and in various other pathological conditions. (wikipedia.org)
- Overexpression of cathepsin B is correlated with invasive and metastatic cancers. (wikipedia.org)
- cathepsins are overexpressed in a number of cancers. (sciencepop.org)
Cells1
- Cells may become carcinogenic when cathepsin B is unregulated. (wikipedia.org)