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3.4.14.1: dipeptidyl-peptidase I

This is an abbreviated version!
For detailed information about dipeptidyl-peptidase I, go to the full flat file.

Word Map on EC 3.4.14.1

Reaction

Release of an N-terminal dipeptide, Xaa-Yaa-/-Zaa-, except when Xaa is Arg or Lys, or Yaa or Zaa is Pro =

Synonyms

Cat C, CATC, cathepsin C, cathepsin J, CTSC, DAP I, DDPI, dipeptide arylamidase I, dipeptidyl aminopeptidase I, dipeptidyl peptidase I, dipeptidyl peptidase I/cathepsin C, dipeptidyl transferase, DPAP1, DPAP2, DPP I, DPP-I, DPPI, EC 3.4.4.9, hDPPI, PBANKA_146070, PFL2290w

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.14 Dipeptidyl-peptidases and tripeptidyl-peptidases
                3.4.14.1 dipeptidyl-peptidase I

Inhibitors

Inhibitors on EC 3.4.14.1 - dipeptidyl-peptidase I

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide
-
-
(4R)-N-[(1S)-1-cyano-2-phenylethyl]-4-(methylsulfanyl)-4-phenyl-L-prolinamide
-
-
(4R)-N-[(1S)-1-cyano-2-phenylethyl]-4-fluoro-4-phenyl-L-prolinamide
-
-
(4S)-4-chloro-N-[(1S)-1-cyano-2-phenylethyl]-L-prolinamide
-
-
(4S)-N-(1-cyanocyclopropyl)-4-(methylsulfanyl)-L-prolinamide
-
-
(4S)-N-(1-cyanocyclopropyl)-4-fluoro-L-prolinamide
-
-
(4S)-N-[(1R,2S)-2-benzyl-1-cyanocyclopropyl]-4-(methylsulfanyl)-L-prolinamide
-
-
(4S)-N-[(1R,2S)-2-benzyl-1-cyanocyclopropyl]-4-fluoro-L-prolinamide
-
-
(4S)-N-[(1S)-1-cyano-2-phenylethyl]-4-(ethylsulfanyl)-L-prolinamide
-
-
(4S)-N-[(1S)-1-cyano-2-phenylethyl]-4-(methylsulfanyl)-L-prolinamide
-
-
(4S)-N-[(1S)-1-cyano-2-phenylethyl]-4-fluoro-L-prolinamide
-
-
(4S)-N-[(1S)-1-cyano-2-phenylethyl]-4-methoxy-L-prolinamide
-
-
(4S)-N-[(1S)-1-cyano-2-phenylethyl]-4-methyl-L-prolinamide
-
-
(4S)-N-[(1S,2R)-2-benzyl-1-cyanocyclopropyl]-4-(methylsulfanyl)-L-prolinamide
-
-
(4S)-N-[(1S,2R)-2-benzyl-1-cyanocyclopropyl]-4-fluoro-L-prolinamide
-
-
(4S)-N-[(1S,2S)-1-cyano-2-phenylcyclopropyl]-4-fluoro-L-prolinamide
-
-
1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(2-naphthyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide
-
IC50: 19 nM
1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(benzo[b]-thiophen-3-yl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide
-
IC50: 22 nM
1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(indol-3-yl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide
-
IC50: 21 nM
1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(m-fluorophenyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide
-
IC50: 31 nM, competitive inhibition, selective for DPP I over other cysteine and serine proteases, noncytotoxic
1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(m-methoxyphenyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide
-
IC50: 39 nM
1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(p-chlorophenyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide
-
IC50: 45 nM
3-chloro-2-hydroxypropyl (2Z)-2-(2-aminoacetamido)-3-phenylprop-2-enoate
-
3-[4-(1-amino-1-cyclopentylethyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
3-[4-(1-amino-2-phenylethyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
-
3-[4-(1-aminocyclohexyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
-
3-[4-(1-aminocyclohexyl)-1H-1,2,3-triazol-1-yl]-2-oxoheptyl 2,6-dimethylbenzoate
-
-
3-[4-(1-aminoethyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
-
3-[4-(2-aminopentan-2-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
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-
3-[4-(2-aminopropan-2-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
-
3-[4-(2-methylpyrrolidin-2-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
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-
3-[4-(3-aminopentan-3-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
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-
3-[4-(4-aminoheptan-4-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
-
3-[4-[(1R)-1-amino-1-cyclopentylethyl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
-
3-[4-[(1S)-1-amino-1-cyclohexylethyl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
-
3-[4-[(1S)-1-amino-1-cyclopentylethyl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
-
3-[4-[4-(methylamino)heptan-4-yl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
-
5,5'-dithiobis(2-nitrobenzoic acid)
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1.5 mM, 81% residual activity
5-aminopentanoic acid ethyl ester
-
-
Ala-4(I)Phe-diazomethyl ketone
-
irreversible inhibitor
antipain
Arg-NH2
-
inhibition of the reaction with Gly-Gly-ethyl ester or Gly-L-Phe-NH2
benzoyl-Arg-NH2
-
inhibition of the reaction with Gly-Gly-ethyl ester or Gly-L-Phe-NH2
beta-Ala-NH2
-
inhibition of the reaction with Gly-Gly-ethyl ester or Gly-L-Phe-NH2
beta-alanine ethyl ester
-
-
Boc-Gly-DELTA(Z)Phe-AbuPO(OMe)2
-
-
Butylamine
-
reaction with Gly-Gly-ethyl ester, Gly-Gly-NH2 or Gly-Phe-NH2
cystatin
-
-
-
ethylamine
-
-
fluoride
-
fluoride preparations inhibit activity of cathepsin C in saliva
FY01
-
FY01 is a selective reagent for DPPI and can efficiently label its target in an activity-dependent manner in both crude tissue extracts and intact cells
gamma-aminobutyryl ethyl ester
-
-
Glu-alpha-methyl ester
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inhibition of the reaction with Gly-Gly-ethyl ester, weak inhibition of reaction with Gly-L-Phe-NH2
glucagon
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competitive inhibition of His-Ser-2-naphthylamide hydrolysis
Gly-beta-Ala-NH2
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inhibition of the reaction with Gly-Gly-ethyl ester or Gly-L-Phe-NH2
Gly-DELTA(Z)Phe-AlaPO(OEt)2-trifluoroacetic acid
-
-
Gly-DELTAZPhe-Gly-DELTAEPhe-Gly
-
-
Gly-DELTAZPhe-Gly-DELTAEPhe-Gly-OMe
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-
Gly-DELTAZPhe-Gly-DELTAEPhe-Phe
-
-
Gly-DELTAZPhe-Gly-DELTAEPhe-Phe-OMe
-
-
Gly-Gly-NH2
-
inhibition of the reaction with Gly-Gly-ethyl ester or Gly-L-Phe-NH2
Gly-NH2
-
inhibition of the reaction with Gly-Gly-ethyl ester or Gly-L-Phe-NH2
Gly-Phe-CHN2
presence down-regulates mast cell intracellular DPPI and chymase activities. Inhibitor Gly-Phe-CHN2 also inhibits the LTB4-activated neutrophils and neutrophil-elastase activities
Gly-Phe-NH2
-
competitive inhibition of His-Ser-2-naphthylamide hydrolysis
glycinamide
-
reaction with Gly-Gly-ethyl ester, Gly-Gly-NH2 or Gly-Phe-NH2
glycine ethyl ester
-
-
Guanidinium chloride
-
reversible, significantly decreases the Km-value of substrate hydrolysis, without changing the maximal velocity
Hexylamine
-
-
iodoacetamide
iodoacetate
L-trans-epoxy-succinyl-leucylamido(4-guanidino)-butane
-
-
Leu-NH2
-
inhibition of the reaction with Gly-Gly-ethyl ester or Gly-L-Phe-NH2
leupeptin
Lys-NH2
-
inhibition of the reaction with Gly-Gly-ethyl ester, weak inhibition of reaction with Gly-L-Phe-NH2
methylamine
-
-
N-(1-cyano-2,2-dimethylcyclopropyl)-3-thiophen-2-yl-L-alaninamide
-
-
N-(1-cyano-2-phenylcyclopropyl)-3-thiophen-2-yl-L-alaninamide
-
-
N-(1-cyanocyclobutyl)-3-thiophen-2-yl-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-thiophen-2-yl-L-alaninamide
-
-
N-(2-cyanopropan-2-yl)-3-thiophen-2-yl-L-alaninamide
-
-
N-(cyanomethyl)-3-thiophen-2-yl-L-alaninamide
-
-
N-ethylmaleimine
-
1 mM, 46.4% residual activity
N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-norvalinamide
-
-
N-[(1R,2R)-1-cyano-2-phenylcyclopropyl]-3-thiophen-2-yl-L-alaninamide
-
-
N-[(1S)-1-cyano-2,2-dimethylpropyl]-3-thiophen-2-yl-L-alaninamide
-
-
N-[(1S)-1-cyano-2,2-diphenylethyl]-3-thiophen-2-yl-L-alaninamide
-
-
N-[(1S)-1-cyano-2-(1H-indol-3-yl)ethyl]-3-thiophen-2-yl-L-alaninamide
-
-
N-[(1S)-1-cyano-2-(1H-indol-3-yl)ethyl]-L-methioninamide
-
-
N-[(1S)-1-cyano-2-(1H-indol-3-yl)ethyl]-L-valinamide
-
-
N-[(1S)-1-cyano-2-(1H-indol-3-yl)ethyl]-S-ethyl-L-cysteinamide
-
-
N-[(1S)-1-cyano-2-(1H-indol-3-yl)ethyl]-S-ethyl-L-homocysteinamide
-
-
N-[(1S)-1-cyano-2-(4-fluorophenyl)ethyl]-L-prolinamide
-
-
N-[(1S)-1-cyano-2-(5-phenylthiophen-2-yl)ethyl]-3-thiophen-2-yl-L-alaninamide
-
-
N-[(1S)-1-cyano-2-(naphthalen-2-yl)ethyl]-3-thiophen-2-yl-L-alaninamide
-
-
N-[(1S)-1-cyano-2-cyclohexylethyl]-3-thiophen-2-yl-L-alaninamide
-
-
N-[(1S)-1-cyano-2-methylpropyl]-3-thiophen-2-yl-L-alaninamide
-
-
N-[(1S)-1-cyano-2-phenylethyl]-3-thiophen-2-yl-L-alaninamide
-
-
N-[(1S)-1-cyano-2-phenylethyl]-L-prolinamide
-
-
N-[(1S)-1-cyano-2-[4-(methylsulfanyl)phenyl]ethyl]-L-prolinamide
-
-
N-[(1S)-1-cyano-3-phenylpropyl]-3-thiophen-2-yl-L-alaninamide
-
-
N-[(1S)-2-(1,3-benzothiazol-2-yl)-1-cyanoethyl]-3-thiophen-2-yl-L-alaninamide
-
-
N-[(1S,2S)-1-cyano-2-phenylcyclopropyl]-3-thiophen-2-yl-L-alaninamide
-
-
N-[2-(1H-indol-3-yl)ethyl]-L-methioninamide
-
-
N2-(morpholin-4-ylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-leucinamide
-
-
p-Hydroxymercuriphenyl sulfonate
-
-
PCMB
-
-
pentylamine
-
-
Phe-NH2
-
inhibition of the reaction with Gly-Gly-ethyl ester or Gly-L-Phe-NH2
prop-2-en-1-yl 2-(2-amino-3-phenylpropanamido)prop-2-enoate
-
Propylamine
-
-
SAK2
-
peptide vinyl sulfone, covalent inhibitor
sodium deoxycholate
-
-
Trp-NH2
-
inhibition of the reaction with Gly-Gly-ethyl ester or Gly-L-Phe-NH2
additional information
-