Page last updated: 2024-08-07 15:44:25
Cathepsin B
A cathepsin B that is encoded in the genome of human. [PRO:DNx, UniProtKB:P07858]
Synonyms
EC 3.4.22.1;
APP secretase;
APPS;
Cathepsin B1
Research
Bioassay Publications (56)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 3 (5.36) | 18.2507 |
| 2000's | 21 (37.50) | 29.6817 |
| 2010's | 26 (46.43) | 24.3611 |
| 2020's | 6 (10.71) | 2.80 |
Compounds (45)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| l 006235 | Homo sapiens (human) | EC50 | 0.7900 | 1 | 1 |
| balicatib | Homo sapiens (human) | EC50 | 2.9000 | 1 | 1 |
Cathepsin B inhibitors: Further exploration of the nitroxoline core.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 28, Issue:7, 2018
Development of new cathepsin B inhibitors: combining bioisosteric replacements and structure-based design to explore the structure-activity relationships of nitroxoline derivatives.Journal of medicinal chemistry, , Jan-24, Volume: 56, Issue:2, 2013
SAR studies of differently functionalized chalcones based hydrazones and their cyclized derivatives as inhibitors of mammalian cathepsin B and cathepsin H.Bioorganic & medicinal chemistry, , Aug-01, Volume: 22, Issue:15, 2014
Acyl hydrazides and triazoles as novel inhibitors of mammalian cathepsin B and cathepsin H.European journal of medicinal chemistry, , Apr-22, Volume: 77, 2014
Development of cell-active non-peptidyl inhibitors of cysteine cathepsins.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
Natural polyprenylated benzophenones inhibiting cysteine and serine proteases.European journal of medicinal chemistry, , Volume: 44, Issue:3, 2009
Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Discovery of novel cyanamide-based inhibitors of cathepsin C.ACS medicinal chemistry letters, , Feb-10, Volume: 2, Issue:2, 2011
Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.Journal of medicinal chemistry, , Jan-04, Volume: 44, Issue:1, 2001
[no title available]RSC medicinal chemistry, , Feb-23, Volume: 13, Issue:2, 2022
Structures and bioactivities of dihydrochalcones from Metrodorea stipularis.Journal of natural products, , Nov-26, Volume: 77, Issue:11, 2014
Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors.Bioorganic & medicinal chemistry, , Sep-15, Volume: 17, Issue:18, 2009
Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.The Journal of biological chemistry, , Jul-20, Volume: 282, Issue:29, 2007
Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Synthesis and Evaluation of Macrocyclic Peptide Aldehydes as Potent and Selective Inhibitors of the 20S Proteasome.ACS medicinal chemistry letters, , Mar-10, Volume: 7, Issue:3, 2016
Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.Journal of medicinal chemistry, , May-18, Volume: 49, Issue:10, 2006
Synopsis of some recent tactical application of bioisosteres in drug design.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.Antimicrobial agents and chemotherapy, , Volume: 54, Issue:11, 2010
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.Antimicrobial agents and chemotherapy, , Volume: 54, Issue:1, 2010
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.Journal of medicinal chemistry, , Mar-09, Volume: 49, Issue:5, 2006
Cathepsin B: Active site mapping with peptidic substrates and inhibitors.Bioorganic & medicinal chemistry, , 01-01, Volume: 27, Issue:1, 2019
Neuroprotective effect of synthetic chalcone derivatives as competitive dual inhibitors against μ-calpain and cathepsin B through the downregulation of tau phosphorylation and insoluble Aβ peptide formation.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Synthesis and investigation of dihydroxychalcones as calpain and cathepsin inhibitors.Bioorganic chemistry, , Volume: 51, 2013
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.Journal of medicinal chemistry, , Dec-01, Volume: 48, Issue:24, 2005
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.Journal of medicinal chemistry, , Dec-01, Volume: 48, Issue:24, 2005
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
The identification of potent, selective, and bioavailable cathepsin S inhibitors.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 17, Issue:17, 2007
Identification of a potent and selective non-basic cathepsin K inhibitor.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 16, Issue:7, 2006
Discovery of selective covalent cathepsin K inhibitors containing novel 4-cyanopyrimidine warhead based on quantum chemical calculations and binding mode analysis.Bioorganic & medicinal chemistry, , Nov-15, Volume: 74, 2022
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
3-Cyano-3-aza-β-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins.ACS medicinal chemistry letters, , Oct-09, Volume: 5, Issue:10, 2014
(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.Journal of medicinal chemistry, , Dec-01, Volume: 48, Issue:24, 2005
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.Journal of medicinal chemistry, , Dec-01, Volume: 48, Issue:24, 2005
Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.Antimicrobial agents and chemotherapy, , Volume: 54, Issue:11, 2010
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.Antimicrobial agents and chemotherapy, , Volume: 54, Issue:1, 2010
Neuroprotective effect of synthetic chalcone derivatives as competitive dual inhibitors against μ-calpain and cathepsin B through the downregulation of tau phosphorylation and insoluble Aβ peptide formation.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophy.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Benzoylalanine-derived ketoamides carrying vinylbenzyl amino residues: discovery of potent water-soluble calpain inhibitors with oral bioavailability.Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
Synthesis and biological evaluation of novel piperidine carboxamide derived calpain inhibitors.Bioorganic & medicinal chemistry letters, , Oct-02, Volume: 10, Issue:19, 2000
Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity.Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Discovery of Di- and Trihaloacetamides as Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity.Journal of the American Chemical Society, , 12-15, Volume: 143, Issue:49, 2021
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.Journal of medicinal chemistry, , 02-24, Volume: 65, Issue:4, 2022
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.Journal of natural products, , Jan-24, Volume: 77, Issue:1, 2014
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| cysteine-type endopeptidase activity | molecular function | Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a mechanism in which the sulfhydryl group of a cysteine residue at the active center acts as a nucleophile. [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE, https://www.ebi.ac.uk/merops/about/glossary.shtml#ENDOPEPTIDASE] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| collagen binding | molecular function | Binding to collagen, a group of fibrous proteins of very high tensile strength that form the main component of connective tissue in animals. Collagen is highly enriched in glycine (some regions are 33% glycine) and proline, occurring predominantly as 3-hydroxyproline (about 20%). [GOC:ai, ISBN:0198506732] |
| peptidase activity | molecular function | Catalysis of the hydrolysis of a peptide bond. A peptide bond is a covalent bond formed when the carbon atom from the carboxyl group of one amino acid shares electrons with the nitrogen atom from the amino group of a second amino acid. [GOC:jl, ISBN:0815332181] |
| cysteine-type peptidase activity | molecular function | Catalysis of the hydrolysis of peptide bonds in a polypeptide chain by a mechanism in which the sulfhydryl group of a cysteine residue at the active center acts as a nucleophile. [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE] |
| proteoglycan binding | molecular function | Binding to a proteoglycan, any glycoprotein in which the carbohydrate units are glycosaminoglycans. [ISBN:0198506732] |
Located In
This protein is located in 11 target(s):
| Target | Category | Definition |
|---|
| extracellular region | cellular component | The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators] |
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
| lysosome | cellular component | A small lytic vacuole that has cell cycle-independent morphology found in most animal cells and that contains a variety of hydrolases, most of which have their maximal activities in the pH range 5-6. The contained enzymes display latency if properly isolated. About 40 different lysosomal hydrolases are known and lysosomes have a great variety of morphologies and functions. [GOC:mah, ISBN:0198506732] |
| external side of plasma membrane | cellular component | The leaflet of the plasma membrane that faces away from the cytoplasm and any proteins embedded or anchored in it or attached to its surface. [GOC:dos, GOC:tb] |
| apical plasma membrane | cellular component | The region of the plasma membrane located at the apical end of the cell. [GOC:curators] |
| endolysosome lumen | cellular component | The volume enclosed by the membrane of an endolysosome. An endolysosome is a transient hybrid organelle formed by fusion of a late endosome with a lysosome. [GOC:pde] |
| melanosome | cellular component | A tissue-specific, membrane-bounded cytoplasmic organelle within which melanin pigments are synthesized and stored. Melanosomes are synthesized in melanocyte cells. [GOC:jl, PMID:11584301] |
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
| collagen-containing extracellular matrix | cellular component | An extracellular matrix consisting mainly of proteins (especially collagen) and glycosaminoglycans (mostly as proteoglycans) that provides not only essential physical scaffolding for the cellular constituents but can also initiate crucial biochemical and biomechanical cues required for tissue morphogenesis, differentiation and homeostasis. The components are secreted by cells in the vicinity and form a sheet underlying or overlying cells such as endothelial and epithelial cells. [GOC:BHF, GOC:rph, PMID:21123617] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
| ficolin-1-rich granule lumen | cellular component | Any membrane-enclosed lumen that is part of a ficolin-1-rich granule. [GO_REF:0000064, GOC:TermGenie, PMID:23650620] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
| lysosome | cellular component | A small lytic vacuole that has cell cycle-independent morphology found in most animal cells and that contains a variety of hydrolases, most of which have their maximal activities in the pH range 5-6. The contained enzymes display latency if properly isolated. About 40 different lysosomal hydrolases are known and lysosomes have a great variety of morphologies and functions. [GOC:mah, ISBN:0198506732] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| peptidase inhibitor complex | cellular component | A protein complex which is capable of peptidase inhibitor activity. [GO_REF:0000088, GOC:bhm, GOC:TermGenie, PMID:20860624] |
Involved In
This protein is involved in 9 target(s):
| Target | Category | Definition |
|---|
| proteolysis | biological process | The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah] |
| thyroid hormone generation | biological process | The formation of either of the compounds secreted by the thyroid gland, mainly thyroxine and triiodothyronine. This is achieved by the iodination and joining of tyrosine molecules to form the precursor thyroglobin, proteolysis of this precursor gives rise to the thyroid hormones. [GOC:jl, ISBN:0716720094] |
| collagen catabolic process | biological process | The proteolytic chemical reactions and pathways resulting in the breakdown of collagen in the extracellular matrix, usually carried out by proteases secreted by nearby cells. [GOC:mah, ISBN:0815316194] |
| epithelial cell differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of an epithelial cell, any of the cells making up an epithelium. [GOC:ecd, PMID:11839751] |
| regulation of apoptotic process | biological process | Any process that modulates the occurrence or rate of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| decidualization | biological process | The cellular and vascular changes occurring in the endometrium of the pregnant uterus just after the onset of blastocyst implantation. This process involves the proliferation and differentiation of the fibroblast-like endometrial stromal cells into large, polyploid decidual cells that eventually form the maternal component of the placenta. [ISBN:0721662544, PMID:11133685] |
| symbiont entry into host cell | biological process | The process by which a symbiont breaches the plasma membrane or cell envelope and enters the host cell. The process ends when the symbiont or its genome is released into the host cell. [GOC:jl] |
| proteolysis involved in protein catabolic process | biological process | The hydrolysis of a peptide bond or bonds within a protein as part of the chemical reactions and pathways resulting in the breakdown of a protein by individual cells. [GOC:ai, GOC:dph, GOC:tb] |
| cellular response to thyroid hormone stimulus | biological process | A change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a thyroid hormone stimulus. [GOC:sjw, PMID:9916872] |