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3.4.25.1: proteasome endopeptidase complex

This is an abbreviated version!
For detailed information about proteasome endopeptidase complex, go to the full flat file.

Word Map on EC 3.4.25.1

Reaction

cleavage of peptide bonds with very broad specificity =

Synonyms

20 S proteasome, 206 proteasome, 20S CP, 20S protease core, 20S proteasome, 26 S proteasome, 26S protease, 26S proteasome, 26S proteasome complex, 27 kDa prosomal protein, 30 kDa prosomal protein, beta1-PF1404, c20S, Component Y8, constitutive proteasome 20S, EC 3.4.22.21, EC 3.4.24.5, EC 3.4.99.46, GPRO-28, HsBPROS26, HSN3, i20S, immunoproteasome 20S, ingensin, KIPase, large multicatalytic protease, macropain, multi-subunit protease complex, multicatalytic endopeptidase complex, Multicatalytic endopeptidase complex C7, multicatalytic protease, multicatalytic proteinase, p27K, PROS-27, PROS-30, PROS-Dm25, PROS-Dm28.1, PROS-Dm29, PROS-Dm35, Pros26.4, prosome, proteasome, proteasome 19S, proteasome 20S, Proteasome component C13, Proteasome component C2, Proteasome component C3, Proteasome component C5, Proteasome component C8, Proteasome component C9, Proteasome component DD4, Proteasome component DD5, Proteasome component pts1, proteasome subunit alpha-type 7-like, PSMA5, Psma8, RING12 protein, RN3, Scl1, SCL1 suppressor protein, SFRICE_003436, T20S, TAS-F22/FAFP98, TAS-G64, TCPR29, tricorn protease, tricorn proteinase, XC3

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.25 Threonine endopeptidases
                3.4.25.1 proteasome endopeptidase complex

Inhibitors

Inhibitors on EC 3.4.25.1 - proteasome endopeptidase complex

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(-)-epigallocatechin-3-gallate
-
i.e. EGCG, inhibits the proteasomal chymotrypsin-like activity
(2E)-3-(4-tert-butylphenyl)-1-[4-(4-nitrophenyl)piperazin-1-yl]prop-2-en-1-one
-
-
(2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,4,5-triethoxybenzoate)
-
inhibits 48% of MDA-MB-231 cell proliferation at 0.05 mM
(2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,4,5-trihydroxybenzoate)
-
-
(2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,5-diethoxybenzoate)
-
70-79% inhibition in MDA-MB-231 cells at 0.025-0.050 mM
(2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,5-dihydroxybenzoate)
-
-
(acetato-kappaO)[2,4-diiodo-6-({[(pyridin-2-yl-kappaN)methyl]amino-kappaN}methyl)phenolato-kappaO]copper
-
a copper complex, causes selective 20S proteasomal inhibition and apoptosis induction in several lines of cancer cells
1-[1-(1-[(2,4-dioxoimidazolidin-1-ylimino)-methyl]-2-phenyl-ethylcarbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-(1H-indol)
2-(2-bromo-4-tert-butylphenoxy)-1-[4-(4-nitrophenyl)piperazin-1-yl]ethanone
-
-
2-(2-chlorophenyl)-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]quinoline-4-carboxamide
-
-
2-(4-tert-butylphenoxy)-1-[4-(4-methoxy-2-nitrophenyl)piperazin-1-yl]ethanone
-
-
2-methyl-5-[4-(phenylamino)phthalazin-1-yl]-N-(tetrahydrofuran-2-ylmethyl)benzenesulfonamide
-
-
3,4-dichloroisocoumarin
4-(4-methoxyphenyl)-N-(4-nitrophenyl)piperazine-1-carbothioamide
-
-
4-hydroxy-2-nonenal
-
specific subunits of the 20S proteasome are targeted for modification by 4-hydroxy-2-nonenal (0.5 mM)
4-tert-butyl-N-[4-(diethylsulfamoyl)phenyl]benzamide
-
-
4-tert-butyl-N-[4-(dipropylsulfamoyl)phenyl]benzamide
-
-
4-tert-butyl-N-[4-[di(prop-2-en-1-yl)sulfamoyl]phenyl]benzamide
-
-
acetyl-Ala-Pro-norleucine-Leu-Asp-aldehyde
acetyl-DPSD-CHO
-
-
acetyl-Leu-Leu-Arg
-
IC50: 0.85 mM for chymotrypsin-like activity, 0.0056 mM for trypsin-like activity
acetyl-Leu-Leu-norleucinal
-
competitive
adamantaneacetyl-(6-aminohexanoyl)3-(leucyl)3-vinylmethyl sulfone
-
-
AEBSF
-
25% inhibition of hydrolysis of acetyl-norleucine-Leu-Pro-norleucine-Leu-Asp-7-amino-4-methylcoumarin, 22% inhibition of hydrolysis of acetyl-norleucine-GPLD-7-amido-4-methylcoumarin, 19% inhibition of hydrolysis of acetyl-GPLL-7-amido-4-methylcoumarin, 21% inhibition of hydrolysis of acetyl-Ala-Pro-norleucine-Leu-Leu-7-amido-4-methylcoumarin, 26% inhibition of hydrolysis of succinyl-LLVY-7-amido-4-methylcoumarin, 98% inhibition of hydrolysis of tert-butyloxycarbonyl-LRR-7-amino-4-methylcoumarin
ALLN
-
-
antipain
Aprotinin
-
0.0133 mg/ml, 53.62% inhibition
ATP
-
inhibits trypsin-like, peptidylglutamyl peptide hydrolase, and branched-chain amino acid preferring activities
belactosin A
-
isolated from a Streptomyces sp. strain
Belactosin C
-
isolated from a Streptomyces sp. strain
benzyloxycarbonyl-Ala-Ala-Phe-CH2Cl
-
-
benzyloxycarbonyl-GPAF aldehyde
-
-
benzyloxycarbonyl-GPFL aldehyde
-
-
benzyloxycarbonyl-IE-(Ot-Bu)-AL aldehyde
-
0.002 mg/ml, 75% inhibition of chymotrypsin-like activity, hydrolysis of benzyloxycarbonyl-GGL-4-nitroanilide. 0.002 mM, 8% inhibition of peptidyl-glutamyl-peptide-hydrolyzing activity, hydrolysis of benzyloxycarbonyl-LLE-2-naphthylamide
benzyloxycarbonyl-Leu-Gly-Arg
-
IC50: 0.11 mM for chymotrypsin-like activity, 0.0066 mM for trypsin-like activity
benzyloxycarbonyl-Leu-Leu
-
0.1 mM, 84% inhibition of hydrolysis of succinyl-Leu-leu-Val-Tyr-7-amido-4-methylcoumarin, 43% inhibition of hydrolysis of tert-butyloxycarbonyl-Phe-Ser-Arg-7-amido-4-methylcoumarin, 20% inhibition of hydrolysis of benzyloxycarbonyl-Leu-Leu-Leu-7-amido-4-methylcoumarin, 86% inhibition of hydrolysis of benzyloxycarbonyl-Leu-Leu-Glu-7-amido-4-methylcoumarin
Benzyloxycarbonyl-Leu-Leu-Arg
-
IC50: 0.056 mM for chymotrypsin-like activity, 0.0014 mM for trypsin-like activity
benzyloxycarbonyl-Leu-Leu-CH2Cl
-
-
benzyloxycarbonyl-Leu-Leu-Leu-CHO
-
reversible inhibitor, modulation by sodium ion
benzyloxycarbonyl-Leu-Ser-Arg
-
IC50: 0.017 mM for chymotrypsin-like activity, 0.0017 mM for trypsin-like activity
benzyloxycarbonyl-Leu-Thr-Arg
-
IC50: 0.065 mM for chymotrypsin-like activity, 0.0021 mM for trypsin-like activity
benzyloxycarbonyl-LLF aldehyde
-
-
benzyloxycarbonyl-LLL aldehyde
-
0.001 mg/ml, 69% inhibition of chymotrypsin-like activity, hydrolysis of benzyloxycarbonyl-GGL-4-nitroanilide
benzyloxycarbonyl-Phe-Ser-Arg
-
IC50: 0.0089 mM for chymotrypsin-like activity, 0.002 mM for trypsin-like activity
benzyloxycarbonyl-Pro-norleucine-Leu-Asp-aldehyde
bortezomib
calpeptin
-
inhibits calpain-like activity
carbobenzoxy-L-leucyl-L-leucyl-leucinal
-
MG-132
carfilzomib
CEP-18770
cetyltrimethylammonium bromide
-
-
chloro[2,4-diiodo-6-({[(pyridin-2-yl-kappaN)methyl]amino-kappaN}methyl)phenolato-kappaO]copper
-
a copper complex, causes selective 20S proteasomal inhibition and apoptosis induction in several lines of cancer cells
chymostatin
Cl-
-
inhibits peptidylglutamyl peptide hydrolase activity
clasto-lactacystin beta-lactone
-
complete inhibition of the chymotrypsin-like activity at 0.01 mM, complete inhibition of the trypsin-like activity at 0.02 mM, and complete inhibition of caspase-activity of the 26S proteasome at 0.02 mM
clastolactacystin-beta-lactone
-
-
cystatin
-
0.0133 mg/mL 46.38% inhibition
-
c[Ala-Leu-Leu-Glu(Leu-vinyl ester)]
-
-
c[Gly-Leu-Leu-Glu(Leu-vinyl ester)]
-
-
c[Ser-Leu-Leu-Glu(Leu-vinyl ester)]
-
-
c[Val-Leu-Leu-Glu(Leu-vinyl ester)]
-
-
delanzomib
-
slow-binding inhibitor, kinetic analysis
dibromo[(dimethylamino)methanedithiolato(2-)-kappa2S1,S1]aurate(3-)
-
proteasome inhibition and apoptosis induction are completely blocked by addition of dithiothreitol or N-acetyl-L-cysteine, showing that process of oxidation is required for proteasome inhibition
diisopropylfluorophosphate
-
-
E-64
-
0.0133 mg/ml, 71.15% inhibition
E-64-d
-
0.1 mM, 30% inhibition of hydrolysis of succinyl-Leu-leu-Val-Tyr-7-amido-4-methylcoumarin, no inhibition of hydrolysis of tert-butyloxycarbonyl-Phe-Ser-Arg-7-amido-4-methylcoumarin, benzyloxycarbonyl-Leu-Leu-Leu-7-amido-4-methylcoumarin, benzyloxycarbonyl-Leu-Leu-Glu-7-amido-4-methylcoumarin
epoxomicin
epoxomycin
ethanol
-
ethanol-induced proteasome inhibition in liver cells
glial fibrillary acidic protein
-
human recombinant GFP-tagged, accumulation of the intermediate filament protein, glial fibrillary acidic protein, GFAP, in astrocytes of Alexander disease impairs proteasome function in astrocytes, also oligomers of R239C mutant GFAP inhibit the proteasome system in Alexander disease astrocytes to an even higher extent compared to the wild-type GFAP. The small heat shock protein chaperone alphaB-crystallin reverses the inhibition by shifting the size of the mutant protein from larger oligomers to smaller oligomers and monomers. The proteasome cannot efficiently degrade unassembled R239C GFAP, and the interaction of R239C GFAP with proteasomes actually inhibits proteasomal protease activity in a non-competitive manner, detailed overview
-
glidobactin A
-
GlbA
H-Ala-Leu-Leu-Glu(Leu-vinyl ester)-NH2
-
-
H-Gly-Leu-Leu-Glu(Leu-vinyl ester)-NH2
-
-
H-Ser-Leu-Leu-Glu(Leu-vinyl ester)-NH2
-
-
H-Val-Leu-Leu-Glu(Leu-vinyl ester)-NH2
-
-
hepatitis B virus X protein
-
-
-
histone H3
-
activity with benzyloxycarbonyl-LAF-4-aminobenzoate, 87%, benzyloxycarbonyl-dALR-4-aminobenzoate, 43%, or benzyloxycarbonyl-LLE-2-naphthylamide, 81% as substrates
-
iodoacetic acid
-
1.0 mM, 54.04 mM inhibition
ixazomib
-
slow-binding inhibitor, kinetic analysis
lactacystin
leupeptin
marizomib
-
-
MG-132
MG115
MLN9708
Mn2+
-
inhibits peptidylglutamyl peptide hydrolase activity
mutant huntingtin
-
mutant huntingtin filamentous aggregates can inhibit 26S proteasome activity, but only when not recruited inclusion bodies
-
N,N'-bis(4-methoxyphenyl)tricyclo[3.3.1.13,7]decane-1,3-dicarboxamide
-
-
N-(1-hydroxy-2-methylpropan-2-yl)-5-[4-[(3-hydroxyphenyl)amino]phthalazin-1-yl]-2-methylbenzenesulfonamide
-
-
N-(2-methyl-1,3-thiazole-5-carbonyl)-5-phenyl-L-norvalyl-N-[(1E,3S)-1-(methanesulfonyl)-5-methylhex-1-en-3-yl]-L-homoserinamide
-
compound has low nanomolar activity at killing parasite in the 72 h treatment with exceptionally low toxicity against human foreskin fibroblast resulting in greatly enhanced selectivity ratio. Compound has no toxicity to HepG2 cells even after 72 h treatment with doses as high as 10 microM
N-(3-hydroxy-2-oxopropyl)-5-[4-[(3-hydroxyphenyl)amino]phthalazin-1-yl]-2-methylbenzenesulfonamide
-
-
N-(4-methoxyphenyl)-3-(4-methylphenyl)tricyclo[3.3.1.13,7]decane-1-carboxamide
-
-
N-(tert-butoxycarbonyl)-L-alanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide
-
-
N-(tert-butoxycarbonyl)-L-alanyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide
-
-
N-(tert-butoxycarbonyl)-L-isoleucyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide
-
-
N-(tert-butoxycarbonyl)-L-phenylalanyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
-
60.06% inhibition at 0.01 mM
N-(tert-butoxycarbonyl)-L-phenylalanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide
-
-
N-(tert-butoxycarbonyl)-O-methyl-L-tyrosyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
-
89.7% inhibition at 0.01 mM
N-(tert-butoxycarbonyl)-O-methyl-L-tyrosyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
-
69.7% inhibition at 0.01 mM
N-(tert-butoxycarbonyl)glycyl-N1-benzyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-L-glutamamide
-
shows significant inhibition of 20S proteasome chymotrypsin-like, b5 activity
N-(tert-butoxycarbonyl)glycyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide
-
shows significant inhibition of 20S proteasome chymotrypsin-like, b5 activity
N-(tert-butoxycarbonyl)glycyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide
-
-
N-acetyl-Leu-Leu-norleucinal
-
-
N-acetyl-leucyl-leucyl-norleucinal
-
MG132, 0.03 mM
N-carbobenzoxy-L-leucyl-L-norvalinal
-
-
N-Cbz-Leu-Leu-leucinal
-
MG132
N-ethylmaleimide
N-methoxysuccinyl-Glu-Val-Lys-Phe-H
-
modified
N-tert-butyl-5-[4-[(3-hydroxyphenyl)amino]phthalazin-1-yl]-2-methylbenzenesulfonamide
-
-
N-tosylphenylalanylchloromethylketone
-
-
N-[(1S)-1-benzyl-2-[[(1S)-1-(furan-2-ylcarbonyl)-3-methylbutyl]amino]-2-oxoethyl]-Na-(tert-butoxycarbonyl)-L-phenylalaninamide
-
inhibits chymotrypsin-like activity of the 26S proteasome
N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
58.5% inhibition at 0.01 mM
N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
-
73.4% inhibition at 0.01 mM
N-[(benzyloxy)carbonyl]-L-phenylalanyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
-
82.2% inhibition at 0.01 mM
N-[4-(acetylsulfamoyl)phenyl]-2-(4-ethoxyphenyl)quinoline-4-carboxamide
-
-
N-[4-(acetylsulfamoyl)phenyl]-2-(4-ethylphenyl)quinoline-4-carboxamide
-
-
N-[4-(azepan-1-ylsulfonyl)phenyl]-4-tert-butylbenzamide
-
-
N-[4-(benzylsulfamoyl)phenyl]-2-methylbenzamide
-
-
N-[4-(benzylsulfamoyl)phenyl]-2-[4-(thiophen-2-yl)phenyl]quinoline-4-carboxamide
-
-
N2-(decylcarbamoyl)-N-[(3E,5S,8S,9E)-2,7-dioxo-5-(propan-2-yl)-1,6-diazacyclododeca-3,9-dien-8-yl]-L-valinamide
-
rational design and synthesis of a syringolin A-based lipophilic derivative, which proves to be a very potent syrbactin-based proteasome inhibitor
N2-(tert-butoxycarbonyl)-N-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-3-[(naphthalen-2-ylmethyl)amino]-3-oxo-D-alaninamide
-
-
N2-(tert-butoxycarbonyl)-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide
-
-
N2-(tert-butoxycarbonyl)-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide
-
-
Nalpha-(tert-butoxycarbonyl)-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
7.7% inhibition at 0.01 mM
Nalpha-(tert-butoxycarbonyl)-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
-
16.5% inhibition at 0.01 mM
Nalpha-(tert-butoxycarbonyl)-N-[(2S)-1-[[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-O-methyl-L-tyrosinamide
-
73% inhibition at 0.01 mM
Nalpha-[(2S)-2-[2-(tert-butoxycarbonyl)hydrazinyl]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
-
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-(4-methoxyphenyl)butanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
-
84.8% inhibition at 0.01 mM
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
47.5% inhibition at 0.01 mM
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
-
67.1% inhibition at 0.01 mM
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
-
14.9% inhibition at 0.01 mM
Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
5.7% inhibition at 0.01 mM
Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
-
13.6% inhibition at 0.01 mM
Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-[[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]amino]-3-(4-methoxyphenyl)-1-oxopropan-2-yl]-O-methyl-L-tyrosinamide
-
60.5% inhibition at 0.01 mM
Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-[[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
-
36.4% inhibition at 0.01 mM
NH4+
-
-
NH4Cl
-
lysosomal inhibitor
NLVS
-
irreversible inhibitor
NMDA
-
exposure causes the disassembly of 26S proteasomes and dissociation of E3, i.e. KCMF1, HUWE1, and UBE3A
NPI-0052
NPLLLVS
IC50: 0.04 mM, inhibition of hydrolysis of Gly-Gly-Arg-7-amido-4-methylcoumarin. IC50: 0.007 mM, inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin, most potent inhibitor for hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin
NPLLNVS
IC50: 0.063 mM, inhibition of hydrolysis of Gly-Gly-Arg-7-amido-4-carbamoylcoumarin. IC50: 0.077 mM, inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin
ONX0912
-
a selective, irreversible inhibitor of the chymotrypsin-like activity of constitutive proteasome 20S and immunoproteasome 20S. ONX0912 exerts toxicity in Waldenstroem macroglobulinemia cells, by reducing bone marrow-derived interleukin-6 and insulin-like growth factor 1 secretion, thus inhibiting BM-induced p-Akt and phosphorylated extracellular signal-related kinase activation in Waldenstroem macroglobulinemia cells, overview. ONX0912 acts synergistically with bortezomib
p-chloromercuribenzoic acid
p65/relA
-
inhibits the degradation of IkappaBalpha by the proteasome
-
PA28
-
inhibition of the protease activities of the of the 20S- and 26S proteasome in all larvaeal stages, overview
-
Pentamidine
-
-
pepstatin
-
0.0133 mg/ml 76.09% inhibition
phenylmethylsulfonyl fluoride
PI 1
-
0.03 mM
prion protein
-
recombinant mouse aggregated beta-PrP binds directly to human 20S and 26S proteasomes, i.e. its 20S core particle, overview. Conversion of cellular prion protein, PrPC, to toxic beta-sheet isoforms, PrPSc, which inhibit the ubiquitin-proteasome system and lead to accumulation of the system substrates, are associated with the prion diseases. PrP aggregates inhibit by stabilising the closed conformation of the substrate entry channel. The 20S proteasome is not inhibited when the gate in the alpha-ring is open due to a truncation mutation or by association with PA26/PA28. Modelling of location of aggregated beta-sheet rich PrP binding to the 20S proteasome and inhibition mechanism, detailed overview
-
pro-epigallocatechin-3-gallate
-
i.e. pro-EGCG, inhibitory efficacy is greatly improved from 42% inhibition to 89% inhibition when combined with 3,5-dinitrocatechol
PS-341
PSI
-
0.1 mM, 93% inhibition of hydrolysis of succinyl-Leu-leu-Val-Tyr-7-amido-4-methylcoumarin, no inhibition of hydrolysis of tert-butyloxycarbonyl-Phe-Ser-Arg-7-amido-4-methylcoumarin and benzyloxycarbonyl-Leu-Leu-Leu-7-amido-4-methylcoumarin, complete inhibition of hydrolysis of benzyloxycarbonyl-Leu-Leu-Glu-7-amido-4-methylcoumarin
quercetin
-
-
syringolin A
syringolin A methyl ester
-
-
-
syringolin B
-
SylB, synthesis and inhibitory potency, overview
TLCK
-
0.133 mg/ml, 79.57% inhibition
YLLLVS
IC50: 0.048 mM, inhibition of hydrolysis of Gly-Gly-Arg-7-amido-4-methylcoumarin. IC50: 0.033 mM, inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin
Yu101
Z-b-Ala-Val-Ser-Leu-vinyl ester
-
-
Z-beta-Ala-Leu-Leu-Leu-vinyl ester
-
-
Z-Gly-Leu-Leu-Leu-vinyl ester
-
-
Z-Gly-Val-Ser-Leu-vinyl ester
-
-
Z-NH-(CH2)3-CO-Leu-Leu-Leu-vinyl ester
-
-
Z-NH-(CH2)3-CO-Val-Ser-Leu-vinyl ester
-
-
Z-NH-(CH2)4-CO-Leu-Leu-Leu-vinyl ester
-
-
Z-NH-(CH2)4-CO-Val-Ser-Leu-vinyl ester
-
-
Z-NH-(CH2)5-CO-Leu-Leu-Leu-vinyl ester
-
-
Z-NH-(CH2)5-CO-Val-Ser-Leu-vinyl ester
-
-
Z-NH-(CH2)6-CO-Leu-Leu-Leu-vinyl ester
-
-
Z-NH-(CH2)6-CO-Val-Ser-Leu-vinyl ester
-
-
Z-NH-(CH2)7-CO-Leu-Leu-Leu-vinyl ester
-
-
Z-NH-(CH2)7-CO-Val-Ser-Leu-vinyl ester
-
-
Zn2+
-
inhibits peptidylglutamyl peptide hydrolase activity
[Au(ESDT)]2
[AuBr2(ESDT)]
[Cu(HLI)(LI)]OAc
-
a copper complex, HLI is the ligand 2,4-diiodo-6-((pyridine-2-ylmethylamino)methyl)phenol, causes selective 20S proteasomal inhibition and apoptosis induction in several lines of cancer cells
-
additional information
-