Roles > proteasome inhibitor
Page last updated: 2024-08-05 15:28:41

proteasome inhibitor

A drug that blocks the action of proteasomes, cellular complexes that break down proteins.

ChEBI ID: 52726

Members (11)

MemberDefinitionClass
benzyloxycarbonylleucyl-leucyl-leucine aldehydeA tripeptide that is L-leucyl-L-leucyl-L-leucine in which the C-terminal carboxy group has been reduced to the corresponding aldehyde and the N-terminal amino group is protected as its benzyloxycarbonyl derivative.N-benzyloxycarbonyl-L-leucyl-L-leucyl-L-leucinal
bortezomibL-Phenylalaninamide substituted at the amide nitrogen by a 1-(dihydroxyboranyl)-3-methylbutyl group and at N(alpha) by a pyrazin-2-ylcarbonyl group. It is a dipeptidyl boronic acid that reversibly inhibits the 26S proteasome.bortezomib
carfilzomibA synthetic tetrapeptide consisting of morpholin-4-acetyl, L-2-amino-4-phenylbutanoyl, L-leucyl and L-phenylalanyl residues joined in sequence with the C-terminus connected to the amino group of (2S)-2-amino-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-1-one via an amide linkage. Used for the treatment of patients with multiple myelomacarfilzomib
delanzomibA C-terminal boronic acid peptide inhibitor which induces apoptosis in multiple myeloma, hematological and solid tumor cell lines.delanzomib
epoxomicinA tripeptide consisting of an Ile-Ile-Thr-NH2 sequence N-substituted on the threonamide amidic nitrogen with a (2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl group and with acetyl and methyl groups on the nitrogen of the isoleucine residue distal to the threonamide; a naturally occurring selective proteasome inhibitor with anti-inflammatory activity.epoxomicin
gliotoxinA pyrazinoindole with a disulfide bridge spanning a dioxo-substituted pyrazine ring; mycotoxin produced by several species of fungi.gliotoxin
ixazomibA glycine derivative that is the amide obtained by formal condensation of the carboxy group of N-(2,5-dichlorobenzoyl)glycine with the amino group of [(1R)-1-amino-3-methylbutyl]boronic acid. The active metabolite of ixazomib citrate, it is used in combination therapy for treatment of multiple myeloma.ixazomib
marizomibA salinosporamide in which the core (1R)-6-oxa-2-azabicyclo[3.2.0]heptane-3,7-dione skeleton is substituted at positions 1, 4, and 5 by (1S)-cyclohex-2-en-1-yl(hydroxy)methyl, 2-chloroethyl, and methyl groups, respectively (the 1R,4R,5S diastereoisomer). A potent proteasome inhibitor, it has attracted interest for potential use in the treatment of various cancers.salinosporamide A
scutellarinThe glycosyloxyflavone which is the 7-O-glucuronide of scutellarein.scutellarin
tmc-95aA 17-membered macrocyclic lactam that incorporates a phenol and a substituted indole moiety. It includes a R-hydroxy group at position 11 and a (3-methyl-2-oxopentanoyl)amino group at position at position 18 with a S-methyl group. It acts as a proteasome inhibitor and is obtained from Apiospora montagnei Sacc. TC 1093, isolated from a soil sample.TMC-95A
tmc-95bA 17-membered macrocyclic lactam that incorporates a phenol and a substituted indole moiety. A stereoisomer of TMC-95A, it has a [(3R)-3-methyl-2-oxopentanoyl]amino group at position 18. It acts as a proteasome inhibitor and is isolated from Apiospora montagnei Sacc. TC 1093, isolated from a soil sample.TMC-95B

Research

Studies (10,925)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199066 (0.60)18.7374
1990's189 (1.73)18.2507
2000's2,994 (27.41)29.6817
2010's5,900 (54.00)24.3611
2020's1,776 (16.26)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials1,075 (9.15%)5.53%
Reviews1,267 (10.79%)6.00%
Case Studies945 (8.05%)4.05%
Observational54 (0.46%)0.25%
Other8,405 (71.56%)84.16%

Protein Targets (181)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
acetylcholinesteraseHomo sapiens (human)Potency30.900811
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency14.125411
AR proteinHomo sapiens (human)Potency0.6125719
Ataxin-2Homo sapiens (human)Potency0.048613
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency0.050326
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency0.238612
caspase-3Cricetulus griseus (Chinese hamster)Potency0.027012
caspase-3Homo sapiens (human)Potency0.238612
Caspase-7Cricetulus griseus (Chinese hamster)Potency0.027012
Cellular tumor antigen p53Homo sapiens (human)Potency0.033126
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency22.334211
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency3.106223
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency0.023213
estrogen nuclear receptor alphaHomo sapiens (human)Potency0.1849924
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency1.226624
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency0.0408613
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency8.912511
EWS/FLI fusion proteinHomo sapiens (human)Potency0.1712420
farnesoid X nuclear receptorHomo sapiens (human)Potency3.488724
Fumarate hydrataseHomo sapiens (human)Potency0.499016
GLI family zinc finger 3Homo sapiens (human)Potency0.016522
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency0.076737
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency0.113812
heat shock protein beta-1Homo sapiens (human)Potency0.207824
Histone H2A.xCricetulus griseus (Chinese hamster)Potency15.556511
Interferon betaHomo sapiens (human)Potency0.3606220
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency0.038724
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency0.044711
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency0.010612
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency0.268537
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency0.066336
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency0.377935
phosphopantetheinyl transferaseBacillus subtilisPotency2.511911
polyproteinZika virusPotency0.499016
PPM1D proteinHomo sapiens (human)Potency0.3913112
pregnane X nuclear receptorHomo sapiens (human)Potency0.023012
progesterone receptorHomo sapiens (human)Potency1.281923
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.444124
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency0.031934
retinoid X nuclear receptor alphaHomo sapiens (human)Potency0.120924
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency0.840322
survival motor neuron protein isoform dHomo sapiens (human)Potency0.891311
TDP1 proteinHomo sapiens (human)Potency0.008026
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency0.056138
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency1.627936
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency21.895912
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency0.113812

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
26S proteasome complex subunit SEM1Homo sapiens (human)IC500.428545
26S proteasome non-ATPase regulatory subunit 1Homo sapiens (human)IC500.428545
26S proteasome non-ATPase regulatory subunit 11Homo sapiens (human)IC500.428545
26S proteasome non-ATPase regulatory subunit 12Homo sapiens (human)IC500.428545
26S proteasome non-ATPase regulatory subunit 13Homo sapiens (human)IC500.428545
26S proteasome non-ATPase regulatory subunit 14Homo sapiens (human)IC500.428545
26S proteasome non-ATPase regulatory subunit 2Homo sapiens (human)IC500.428545
26S proteasome non-ATPase regulatory subunit 3Homo sapiens (human)IC500.428545
26S proteasome non-ATPase regulatory subunit 4Homo sapiens (human)IC500.428545
26S proteasome non-ATPase regulatory subunit 6Homo sapiens (human)IC500.428545
26S proteasome non-ATPase regulatory subunit 7Homo sapiens (human)IC500.428545
26S proteasome non-ATPase regulatory subunit 8Homo sapiens (human)IC500.428545
26S proteasome regulatory subunit 10BHomo sapiens (human)IC500.428545
26S proteasome regulatory subunit 4Homo sapiens (human)IC500.428545
26S proteasome regulatory subunit 6AHomo sapiens (human)IC500.428545
26S proteasome regulatory subunit 6BHomo sapiens (human)IC500.428545
26S proteasome regulatory subunit 7Homo sapiens (human)IC500.428545
26S proteasome regulatory subunit 8Homo sapiens (human)IC500.428545
5-hydroxytryptamine receptor 7Homo sapiens (human)IC5063.400011
Acetolactate synthase catalytic subunit, mitochondrialSaccharomyces cerevisiae S288CIC500.200011
AromataseHomo sapiens (human)IC500.044011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
ATP-dependent Clp protease proteolytic subunitStaphylococcus aureus subsp. aureus NCTC 8325IC505.300012
Beta-carbonic anhydrase 1Mycobacterium tuberculosis H37RvKi7.300011
Bile salt export pumpHomo sapiens (human)IC50133.000011
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC5010.000011
Calpain-2 catalytic subunitHomo sapiens (human)Ki0.653011
Calpain-9Homo sapiens (human)IC509.880011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50104.000022
Carbonic anhydrase 1Homo sapiens (human)Ki1.290022
Carbonic anhydrase 12Homo sapiens (human)Ki5.870011
Carbonic anhydrase 13Homo sapiens (human)Ki8.450011
Carbonic anhydrase 14Homo sapiens (human)Ki3.280011
Carbonic anhydrase 15Mus musculus (house mouse)Ki2.680011
Carbonic anhydrase 2Homo sapiens (human)Ki1.160022
Carbonic anhydrase 3Homo sapiens (human)Ki4.570011
Carbonic anhydrase 4Homo sapiens (human)Ki6.510011
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki6.920011
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)Ki6.830011
Carbonic anhydrase 6Homo sapiens (human)Ki4.380011
Carbonic anhydrase 7Homo sapiens (human)Ki6.940011
Carbonic anhydrase 9Homo sapiens (human)Ki3.380011
Cathepsin BHomo sapiens (human)IC5053.666723
Cathepsin BHomo sapiens (human)Ki0.121022
Cathepsin GHomo sapiens (human)IC507.148735
Cathepsin GHomo sapiens (human)Ki0.630011
Cathepsin KHomo sapiens (human)Ki0.001411
Cathepsin SHomo sapiens (human)IC5025.000011
Chain H, Proteasome component PUP1Saccharomyces cerevisiae (brewer's yeast)Ki0.000611
Chain I, Proteasome component PUP3Saccharomyces cerevisiae (brewer's yeast)Ki0.000611
Chain K, Proteasome component PRE2Saccharomyces cerevisiae (brewer's yeast)Ki0.000612
Chain L, Proteasome component C5Saccharomyces cerevisiae (brewer's yeast)Ki0.000612
ChymaseHomo sapiens (human)IC502.360012
Chymotrypsinogen ABos taurus (cattle)Ki2.400011
Chymotrypsinogen BHomo sapiens (human)Ki0.320011
Cysteine protease Trypanosoma brucei rhodesienseIC5050.000011
Cytochrome P450 3A4Homo sapiens (human)IC503.500011
E3 ubiquitin-protein ligase RNF31Homo sapiens (human)IC500.510011
GABA theta subunitRattus norvegicus (Norway rat)IC500.980011
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC500.980011
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC500.980011
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC500.980011
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC500.980011
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC500.980011
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC500.980011
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC500.980011
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC500.980011
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC500.980011
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC500.980011
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC500.980011
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC500.980011
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC500.980011
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC500.980011
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC500.980011
Gamma-secretase subunit PEN-2Homo sapiens (human)IC50200.000011
Geranylgeranyl transferase type-1 subunit betaHomo sapiens (human)IC5017.000011
Glutathione S-transferase omega-1Homo sapiens (human)IC500.150011
Histone deacetylase 1Homo sapiens (human)IC500.620011
Histone deacetylase 2Homo sapiens (human)IC500.800011
Histone deacetylase 3Homo sapiens (human)IC501.180011
Histone deacetylase 6Homo sapiens (human)IC5069.440011
Histone deacetylase 8Homo sapiens (human)IC500.072011
Histone-lysine N-methyltransferase EHMT2Homo sapiens (human)IC503.465022
Histone-lysine N-methyltransferase SUV39H1Homo sapiens (human)IC500.260011
Indoleamine 2,3-dioxygenase 1Homo sapiens (human)IC500.500011
Lon protease homolog, mitochondrialHomo sapiens (human)IC500.183011
Lysosomal protective proteinHomo sapiens (human)IC5019.600012
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000011
Mycothiol S-conjugate amidaseMycobacterium tuberculosis H37RvIC5050.000011
NACHT, LRR and PYD domains-containing protein 3 Mus musculus (house mouse)IC500.120112
Neuraminidase Influenza A virus (A/Wilson-Smith/1933(H1N1))IC5052.600033
Neutrophil elastaseHomo sapiens (human)IC503.550011
Neutrophil elastaseHomo sapiens (human)Ki2.300011
Nuclear factor NF-kappa-B p100 subunit Homo sapiens (human)IC500.085011
Nuclear factor NF-kappa-B p105 subunitHomo sapiens (human)IC500.085011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC5092.100011
Proteasomal ubiquitin receptor ADRM1Homo sapiens (human)IC500.428545
Proteasome subunit alpha type-1Homo sapiens (human)IC500.50221517
Proteasome subunit alpha type-2Homo sapiens (human)IC500.50221517
Proteasome subunit alpha type-3Homo sapiens (human)IC500.50221517
Proteasome subunit alpha type-4Homo sapiens (human)IC500.50221517
Proteasome subunit alpha type-5Homo sapiens (human)IC500.50221517
Proteasome subunit alpha type-6Homo sapiens (human)IC500.50221517
Proteasome subunit alpha type-7Homo sapiens (human)IC500.50221517
Proteasome subunit alpha-type 8Homo sapiens (human)IC500.50221517
Proteasome subunit beta type-1Homo sapiens (human)IC500.46953342
Proteasome subunit beta type-1Saccharomyces cerevisiae S288CIC501.000011
Proteasome subunit beta type-1Homo sapiens (human)Ki8.408366
Proteasome subunit beta type-10Homo sapiens (human)IC500.53441823
Proteasome subunit beta type-11Homo sapiens (human)IC500.50221517
Proteasome subunit beta type-2Homo sapiens (human)IC501.91363545
Proteasome subunit beta type-2Saccharomyces cerevisiae S288CIC501.000011
Proteasome subunit beta type-2Homo sapiens (human)Ki5.578766
Proteasome subunit beta type-3Homo sapiens (human)IC500.50221517
Proteasome subunit beta type-4Homo sapiens (human)IC500.50221517
Proteasome subunit beta type-5Homo sapiens (human)IC506,838.29715775
Proteasome subunit beta type-5Homo sapiens (human)Ki0.012688
Proteasome subunit beta type-6Homo sapiens (human)IC500.49751619
Proteasome subunit beta type-7Homo sapiens (human)IC501.12361619
Proteasome subunit beta type-8Homo sapiens (human)IC500.28352431
Proteasome subunit beta type-8Mus musculus (house mouse)IC500.016811
Proteasome subunit beta type-9Homo sapiens (human)IC500.55932025
Protein farnesyltransferase subunit betaHomo sapiens (human)IC5040.550022
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)IC5032.700033
ProthrombinHomo sapiens (human)Ki13.000011
Pyruvate kinase PKMHomo sapiens (human)IC5022.640011
RanBP-type and C3HC4-type zinc finger-containing protein 1Homo sapiens (human)IC500.510011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC506.187468
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC506.950034
SharpinHomo sapiens (human)IC500.510011
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)Ki25.900011
Substance-K receptorCavia porcellus (domestic guinea pig)IC5050.600011
Substance-P receptorCavia porcellus (domestic guinea pig)IC5050.600011
Transcription factor p65Homo sapiens (human)IC500.085011
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Ki96.600011
UDP-glucuronosyltransferase 1A10Homo sapiens (human)Ki208.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
ATP-dependent Clp protease proteolytic subunitStaphylococcus aureus subsp. aureus NCTC 8325EC5013.550012
Cathepsin GHomo sapiens (human)EC500.013511
NF-kappa-B inhibitor alphaHomo sapiens (human)EC503.100022

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Proteasome subunit beta type-1Homo sapiens (human)Ki500.025022
Proteasome subunit beta type-2Homo sapiens (human)Ki501.075022
Proteasome subunit beta type-5Homo sapiens (human)Ki500.010022
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)Km43.000011
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Km174.000011
UDP-glucuronosyltransferase 1A10Homo sapiens (human)Km225.000011
UDP-glucuronosyltransferase 1A8Homo sapiens (human)Km198.000011
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