Proteins > Proteasome subunit beta type-5
Page last updated: 2024-08-07 13:10:33
Proteasome subunit beta type-5
A proteasome subunit beta type-5 that is encoded in the genome of human. [PRO:DNx]
Synonyms
EC 3.4.25.1;
Macropain epsilon chain;
Multicatalytic endopeptidase complex epsilon chain;
Proteasome chain 6;
Proteasome epsilon chain;
Proteasome subunit MB1;
Proteasome subunit X
Research
Bioassay Publications (71)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 6 (8.45) | 29.6817 |
2010's | 52 (73.24) | 24.3611 |
2020's | 13 (18.31) | 2.80 |
Compounds (54)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
am 404 | Homo sapiens (human) | EC50 | 28.0000 | 1 | 1 |
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
chlorpromazine | Homo sapiens (human) | EC200 | 45.1250 | 4 | 4 |
bortezomib | Homo sapiens (human) | Ki50 | 0.0100 | 2 | 2 |
pr-957 | Homo sapiens (human) | Ki50 | 0.3350 | 2 | 2 |
Discovery of a Novel Oral Proteasome Inhibitor to Block NLRP3 Inflammasome Activation with Anti-inflammation Activity.Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Metabolism guided optimization of peptidomimetics as non-covalent proteasome inhibitors for cancer treatment.European journal of medicinal chemistry, , Apr-05, Volume: 233, 2022
Structure-Based Optimization and Discovery of M3258, a Specific Inhibitor of the Immunoproteasome Subunit LMP7 (β5i).Journal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
Structure-Based Design of Selective LONP1 Inhibitors for Probing Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Covalent docking modelling-based discovery of tripeptidyl epoxyketone proteasome inhibitors composed of aliphatic-heterocycles.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Design, synthesis, in vitro and in vivo evaluation, and structure-activity relationship (SAR) discussion of novel dipeptidyl boronic acid proteasome inhibitors as orally available anti-cancer agents for the treatment of multiple myeloma and mechanism studBioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
Discovery of novel 20S proteasome inhibitors by rational topology-based scaffold hopping of bortezomib.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 28, Issue:12, 2018
Ridaifen-F conjugated with cell-penetrating peptides inhibits intracellular proteasome activities and induces drug-resistant cell death.European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Immunoproteasome inhibition and bioactivity of thiasyrbactins.Bioorganic & medicinal chemistry, , 01-15, Volume: 26, Issue:2, 2018
Synthesis and antiproteasomal activity of novel O-benzyl salicylamide-based inhibitors built from leucine and phenylalanine.European journal of medicinal chemistry, , Jul-28, Volume: 135, 2017
Synthesis and biological activity of peptide proline-boronic acids as proteasome inhibitors.Bioorganic & medicinal chemistry, , 08-01, Volume: 25, Issue:15, 2017
Design, synthesis and biological evaluation of novel non-peptide boronic acid derivatives as proteasome inhibitors.European journal of medicinal chemistry, , Mar-10, Volume: 128, 2017
Urea-containing peptide boronic acids as potent proteasome inhibitors.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Substituted quinolines as noncovalent proteasome inhibitors.Bioorganic & medicinal chemistry, , 06-01, Volume: 24, Issue:11, 2016
Design, synthesis and docking studies of novel dipeptidyl boronic acid proteasome inhibitors constructed from αα- and αβ-amino acids.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 26, Issue:8, 2016
3D-QSAR-aided design, synthesis, in vitro and in vivo evaluation of dipeptidyl boronic acid proteasome inhibitors and mechanism studies.Bioorganic & medicinal chemistry, , 06-01, Volume: 24, Issue:11, 2016
Design, synthesis and biological evaluation of peptidyl epoxyketone proteasome inhibitors composed of β-amino acids.Chemical biology & drug design, , Volume: 84, Issue:5, 2014
Optimization of peptidomimetic boronates bearing a P3 bicyclic scaffold as proteasome inhibitors.European journal of medicinal chemistry, , Aug-18, Volume: 83, 2014
Design, synthesis and biological evaluation of novel tripeptidyl epoxyketone derivatives constructed from β-amino acid as proteasome inhibitors.Bioorganic & medicinal chemistry, , Jun-01, Volume: 22, Issue:11, 2014
Identification of a new series of amides as non-covalent proteasome inhibitors.European journal of medicinal chemistry, , Apr-09, Volume: 76, 2014
Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Development of peptidomimetic boronates as proteasome inhibitors.European journal of medicinal chemistry, , Volume: 64, 2013
Potent proteasome inhibitors derived from the unnatural cis-cyclopropane isomer of Belactosin A: synthesis, biological activity, and mode of action.Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013
Molecular mechanisms of acquired proteasome inhibitor resistance.Journal of medicinal chemistry, , Dec-13, Volume: 55, Issue:23, 2012
Development of isoquinolinone derivatives as immunoproteasome inhibitors.Bioorganic & medicinal chemistry letters, , 01-01, Volume: 55, 2022
Identification of neomacrophorins isolated from Trichoderma sp. 1212-03 as proteasome inhibitors.Bioorganic & medicinal chemistry, , 12-15, Volume: 27, Issue:24, 2019
Tripeptide analogues of MG132 as protease inhibitors.Bioorganic & medicinal chemistry, , 01-15, Volume: 27, Issue:2, 2019
Synthesis and Biological Activity of Peptide α-Ketoamide Derivatives as Proteasome Inhibitors.ACS medicinal chemistry letters, , Jul-11, Volume: 10, Issue:7, 2019
Identification of 2-thioxoimidazolidin-4-one derivatives as novel noncovalent proteasome and immunoproteasome inhibitors.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 28, Issue:3, 2018
Terminal functionalized thiourea-containing dipeptides as multidrug-resistance reversers that target 20S proteasome and cell proliferation.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Identification of noncovalent proteasome inhibitors with high selectivity for chymotrypsin-like activity by a multistep structure-based virtual screening.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Development of novel proteasome inhibitors based on phthalazinone scaffold.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 26, Issue:12, 2016
A novel tamoxifen derivative, ridaifen-F, is a nonpeptidic small-molecule proteasome inhibitor.European journal of medicinal chemistry, , Volume: 71, 2014
Dimerized linear mimics of a natural cyclopeptide (TMC-95A) are potent noncovalent inhibitors of the eukaryotic 20S proteasome.Journal of medicinal chemistry, , Apr-25, Volume: 56, Issue:8, 2013
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
Structure-based design of derivatives of tyropeptin A as the potent and selective inhibitors of mammalian 20S proteasome.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 15, Issue:7, 2005
Ridaifen-F conjugated with cell-penetrating peptides inhibits intracellular proteasome activities and induces drug-resistant cell death.European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Discovery of novel non-covalent inhibitors selective to the β5-subunit of the human 20S proteasome.European journal of medicinal chemistry, , Jun-15, Volume: 98, 2015
Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Cinnabaramides A-G: analogues of lactacystin and salinosporamide from a terrestrial streptomycete.Journal of natural products, , Volume: 70, Issue:2, 2007
Dimerized linear mimics of a natural cyclopeptide (TMC-95A) are potent noncovalent inhibitors of the eukaryotic 20S proteasome.Journal of medicinal chemistry, , Apr-25, Volume: 56, Issue:8, 2013
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
P3 and P4 position analysis of vinyl ester pseudopeptide proteasome inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 16, Issue:12, 2006
Natural products from mangrove sediments-derived microbes: Structural diversity, bioactivities, biosynthesis, and total synthesis.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
(S)-4-Trimethylsilyl-3-butyn-2-ol as an auxiliary for stereocontrolled synthesis of salinosporamide analogs with modifications at positions C2 and C5.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 23, Issue:24, 2013
Molecular mechanisms of acquired proteasome inhibitor resistance.Journal of medicinal chemistry, , Dec-13, Volume: 55, Issue:23, 2012
Structure-Based Optimization and Discovery of M3258, a Specific Inhibitor of the Immunoproteasome Subunit LMP7 (β5i).Journal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
Optimization of piperidine constructed peptidyl derivatives as proteasome inhibitors.Bioorganic & medicinal chemistry, , 01-01, Volume: 29, 2021
Macrocyclic Immunoproteasome Inhibitors as a Potential Therapy for Alzheimer's Disease.Journal of medicinal chemistry, , 08-12, Volume: 64, Issue:15, 2021
Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
[no title available]Bioorganic & medicinal chemistry, , 09-15, Volume: 27, Issue:18, 2019
Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Development of Novel Epoxyketone-Based Proteasome Inhibitors as a Strategy To Overcome Cancer Resistance to Carfilzomib and Bortezomib.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Covalent docking modelling-based discovery of tripeptidyl epoxyketone proteasome inhibitors composed of aliphatic-heterocycles.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Reviewing Hit Discovery Literature for Difficult Targets: Glutathione Transferase Omega-1 as an Example.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Design, synthesis, and evaluation of cystargolide-based β-lactones as potent proteasome inhibitors.European journal of medicinal chemistry, , Sep-05, Volume: 157, 2018
Exploration of novel piperazine or piperidine constructed non-covalent peptidyl derivatives as proteasome inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Design, synthesis and biological evaluation of novel non-covalent piperidine-containing peptidyl proteasome inhibitors.Bioorganic & medicinal chemistry, , 12-01, Volume: 24, Issue:23, 2016
Design, synthesis and biological evaluation of peptidyl epoxyketone proteasome inhibitors composed of β-amino acids.Chemical biology & drug design, , Volume: 84, Issue:5, 2014
Design, synthesis and biological evaluation of novel tripeptidyl epoxyketone derivatives constructed from β-amino acid as proteasome inhibitors.Bioorganic & medicinal chemistry, , Jun-01, Volume: 22, Issue:11, 2014
Development of peptide epoxyketones as selective immunoproteasome inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
LMP2 Inhibitors as a Potential Treatment for Alzheimer's Disease.Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
Structure-based design of human immuno- and constitutive proteasomes inhibitors.European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morphoJournal of medicinal chemistry, , 12-27, Volume: 61, Issue:24, 2018
Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit.ACS medicinal chemistry letters, , Apr-13, Volume: 8, Issue:4, 2017
Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Development of a new class of proteasome inhibitors with an epoxyketone warhead: Rational hybridization of non-peptidic belactosin derivatives and peptide epoxyketones.Bioorganic & medicinal chemistry, , Jun-15, Volume: 22, Issue:12, 2014
Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Potent proteasome inhibitors derived from the unnatural cis-cyclopropane isomer of Belactosin A: synthesis, biological activity, and mode of action.Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013
Discovery of novel tripeptide propylene oxide proteasome inhibitors for the treatment of multiple myeloma.Bioorganic & medicinal chemistry, , 06-15, Volume: 40, 2021
Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Development of Macrocyclic Peptides Containing Epoxyketone with Oral Availability as Proteasome Inhibitors.Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Molecular mechanisms of acquired proteasome inhibitor resistance.Journal of medicinal chemistry, , Dec-13, Volume: 55, Issue:23, 2012
Discovery of a Novel Oral Proteasome Inhibitor to Block NLRP3 Inflammasome Activation with Anti-inflammation Activity.Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
[no title available]Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Design, synthesis, in vitro and in vivo evaluation, and structure-activity relationship (SAR) discussion of novel dipeptidyl boronic acid proteasome inhibitors as orally available anti-cancer agents for the treatment of multiple myeloma and mechanism studBioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
Molecular mechanisms of acquired proteasome inhibitor resistance.Journal of medicinal chemistry, , Dec-13, Volume: 55, Issue:23, 2012
Enables
This protein enables 4 target(s):
Target | Category | Definition |
threonine-type endopeptidase activity | molecular function | Catalysis of the hydrolysis of internal peptide bonds in a polypeptide chain by a mechanism in which the hydroxyl group of a threonine 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] |
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] |
endopeptidase activity | molecular function | Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain. [http://merops.sanger.ac.uk/about/glossary.htm#ENDOPEPTIDASE] |
Located In
This protein is located in 5 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
centrosome | cellular component | A structure comprised of a core structure (in most organisms, a pair of centrioles) and peripheral material from which a microtubule-based structure, such as a spindle apparatus, is organized. Centrosomes occur close to the nucleus during interphase in many eukaryotic cells, though in animal cells it changes continually during the cell-division cycle. [GOC:mah, ISBN:0198547684] |
cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
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] |
Active In
This protein is active in 3 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Part Of
This protein is part of 3 target(s):
Target | Category | Definition |
proteasome complex | cellular component | A large multisubunit complex which catalyzes protein degradation, found in eukaryotes, archaea and some bacteria. In eukaryotes, this complex consists of the barrel shaped proteasome core complex and one or two associated proteins or complexes that act in regulating entry into or exit from the core. [GOC:rb, Wikipedia:Proteasome] |
proteasome core complex | cellular component | A multisubunit barrel shaped endoprotease complex, which is the core of the proteasome complex. [GOC:rb, PMID:10806206] |
proteasome core complex, beta-subunit complex | cellular component | The proteasome core subcomplex that constitutes the two inner rings of the proteasome core complex. An example of this component is found in Mus musculus. [GOC:jl, GOC:mtg_sensu, GOC:rb, PMID:10854779] |
Involved In
This protein is involved in 2 target(s):
Target | Category | Definition |
response to oxidative stress | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of oxidative stress, a state often resulting from exposure to high levels of reactive oxygen species, e.g. superoxide anions, hydrogen peroxide (H2O2), and hydroxyl radicals. [GOC:jl, PMID:12115731] |
proteasome-mediated ubiquitin-dependent protein catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of a protein or peptide by hydrolysis of its peptide bonds, initiated by the covalent attachment of ubiquitin, and mediated by the proteasome. [GOC:go_curators] |