3.4.14.4: dipeptidyl-peptidase III
This is an abbreviated version!
For detailed information about dipeptidyl-peptidase III, go to the full flat file.
Word Map on EC 3.4.14.4
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3.4.14.4
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exopeptidase
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tynorphin
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enkephalin-degrading
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leu-enkephalin
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nudix
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spinorphin
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hexxh
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map2k5
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medicine
- 3.4.14.4
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exopeptidase
- tynorphin
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enkephalin-degrading
- leu-enkephalin
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nudix
- spinorphin
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hexxh
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map2k5
- medicine
Reaction
release of an N-terminal dipeptide from a peptide comprising four or additional information residues, with broad specificity. Also acts on dipeptidyl 2-naphthylamides. =
Synonyms
BT_1846, Cabys_2252, dipeptdiyl peptidase III, dipeptidyl aminopeptidase III, dipeptidyl arylamidase III, dipeptidyl peptidase III, dipeptidyl-peptidase III, dipeptidyl-peptide hydrolase, dipeptidylpeptidase III, DPP III, DPP-3, DPP-III, DPP3, DPPIII, enkephalinase B, NUDT3, peptidase, dipeptidyl, III, PG_0317, PHYPA_007037, red cell angiotensinase
ECTree
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Inhibitors
Inhibitors on EC 3.4.14.4 - dipeptidyl-peptidase III
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1,3-di-[5-(2-imidazolinyl)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
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1,3-di-[5-(2-imidazolinyl)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
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1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-furyl)-cyclobutane dihydrochloride
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1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-thienyl)-cyclobutane dihydrochloride
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1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-thienyl)-cyclobutanedihydrochloride
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1,3-di-[5-(N-amidino)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
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1,3-di-[5-(N-amidino)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
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1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
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1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-o-chlorophenylcyclobutane dihydrochloride
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1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
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1-ethyl-3(3-dimethyl-amino-propyl)-carbodiimide*HCl
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1.0 mM inhibitor, 29% inhibition, 5.0 mM inhibitor, 64% inhibition
2,2'-dithiodipyridine
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1.0 mM inhibitor, 32% inhibition, 2.5 mM inhibitor, 98% inhibition
2,4,6-trinitrobenzene sufonic acid trihydrate
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1.0 mM inhibitor, 52% inhibition, 2.5 mM inhibitor, 89% inhibition
2-(3H-imidazol-4-yl)-1H-benzoimidazole-5-carboxamidine hydrochloride
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complete inhibition at 0.1 mM
2-(3H-imidazol-4-yl)-1H-benzoimidazole-5-imidazolinylamidine hydrochloride
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complete inhibition at 0.1 mM
3,3'-dithiobis(6-nitrobenzoic acid)
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13% residual activity at 2.5 mM, beta-mercaptoethanol and dithiothreitlol completely restores enzyme activity
4,4'-dithiodipyridine
inactivation of wild-type dipeptidyl peptidase III after incubation at pH 8.0 at 25°C, after 5 min incubation loss of 30% enzyme activity, after 15 min incubation loss of 62% enzyme activity
amino([(5-([(2R)-1-methoxy-3-(6-methylphenanthridin-8-yl)-1-oxopropan-2-yl]carbamoyl)-1H-pyrrol-2-yl)carbonyl]amino)methaniminium chloride
0.035 mM, 45% inhibition
amino[((5-[(2-([(2R)-1-methoxy-3-(6-methylphenanthridin-8-yl)-1-oxopropan-2-yl]amino)-2-oxoethyl)carbamoyl]-1H-pyrrol-2-yl)carbonyl)amino]methaniminium chloride
0.06 mM, 33% inhibition
benzamidine HCl
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1.0 mM inhibitor, 29% inhibition, 5.0 mM inhibitor, 61% inhibition
dimethyl sulfoxide
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inhibitory effect with more than 5% (v/v) dimethyl sulfoxide
E-64
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i.e. L-trans-epoxysuccinyl-leucylamido(4-guanidino)butane, 10% inhibition at 0.1 mM
EGTA
96% inhibition in the presence of 1 mM EGTA, but 110% activity in the presence of the two inhibitors 1 mM EGTA and 1 mM Zn2+
iodoacetic acid
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1.0 mM inhibitor, 25% inhibition, 5.0 mM inhibitor, 48% inhibition
L-Leu-L-Trp-L-Met-L-Arg-L-Phe-L-Ala
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competitive inhibitor, complete inhibition at 1 mM
L-tryptophyl-L-methionyl-L-alpha-aspartyl-L-phenylalaninamide
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competitive inhibition
Leu-enkephalin
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i.e. L-Tyr-Gly-Gly-L-Phe-L-Leu, 92% inhibition at 1 mM, competitive inhibitor
Met-enkephalin
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i.e. L-Tyr-Gly-Gly-L-Phe-L-Met, 61% inhibition at 0.5 mM, competitive inhibitor
methyl N-[5-(carbamimidoylcarbamoyl)-1H-pyrrole-2-carbonyl]-3-[[(pyren-1-yl)methyl]amino]-D-alaninate
0.01 mM, 36% inhibition. Compound is not hydrolysed by enzyme, although the binding affinity is comparable with that of Arg-Arg-2-naphthylamide
N-hydroxy-succinimide
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1.0 mM inhibitor, 30% inhibition, 5.0 mM inhibitor, 51% inhibition
p-aminophenyl mercuric acetate
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1.0 mM inhibitor, 42% inhibition, 2.5 mM inhibitor, 94% inhibition
p-hydroxymercuriphenyl-sulfonic acid
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1.0 mM inhibitor, 22% inhibition, 2.5 mM inhibitor, 96% inhibition
p-nitrocatecholsulfate
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1.0 mM inhibitor, 37% inhibition, 5.0 mM inhibitor, 58% inhibition
Pb(CH3COO)2
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1.0 mM inhibitor, 53% inhibition, 2.5 mM inhibitor, 97% inhibition
Soybean trypsin inhibitor
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1.0 mM inhibitor, 64% inhibition, 2.5 mM inhibitor, 76% inhibition
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6-(4,5-dihydro-1H-imidazol-2-yl)-2-[(E)-2-phenylethenyl]-1H-benzimidazole
0.01 mM, 97.8% inhibition
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1.0 mM inhibitor, 27% inhibition, 5.0 mM inhibitor, 42% inhibition
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1.0 mM inhibitor, 29% inhibition, 2.5 mM inhibitor, 88% inhibition, 5.0 mM inhibitor, 96% inhibition
o-phenanthroline
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1.0 mM inhibitor, 46% inhibition, 2.5 mM inhibitor, 85% inhibition, 5.0 mM inhibitor, 96% inhibition
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reactivation by reduced glutathione or mercaptoethanol
Zn2+
19% inhibition in the presence of 0.1 mM Zn2+, 99.8% inhibition in the presence of 1 mM Zn2+
activities in phosphate buffers are singnificantly lower than in Tris-Hcl buffer
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additional information
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activities in phosphate buffers are singnificantly lower than in Tris-Hcl buffer
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additional information
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structural requirements for inhibition by hemorphin-like peptides
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