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3.4.11.3: cystinyl aminopeptidase

This is an abbreviated version!
For detailed information about cystinyl aminopeptidase, go to the full flat file.

Word Map on EC 3.4.11.3

Reaction

Release of an N-terminal amino acid, Cys-/-Xaa-, in which the half-cystine residue is involved in a disulfide loop, notably in oxytocin or vasopressin. Hydrolysis rates on a range of aminoacyl arylamides exceed that for the cystinyl derivative, however =

Synonyms

alpha-Aminoacyl-peptide hydrolase, aminopeptidase, cystyl, AT4 receptor, CAP, CAP-I, CAP-II, CysAP, cysteine aminopeptidase, cystine aminopeptidase, Cystinyl aminopeptidase, cystinylaminopeptidase, cystyl aminopeptidase, cystyl-aminopeptidase, GP160, insulin regulated aminopeptidase, insulin-regulated aminopeptidase, insulin-regulated aminopeptidase IRAP, Insulin-regulated membrane aminopeptidase, Insulin-responsive aminopeptidase, IRAP, IRAP/P-LAP, L-cystine aminopeptidase, LCAP, LeuAP, leucine aminopeptidase/oxytocinase, leucyl-aminopeptidase, leucyl-cystinyl aminopeptidase, LNPEP, M1 aminopeptidase, OTase, oxytocin peptidase, oxytocinase, oxytocinase/insulin-regulated aminopeptidase, oxytocinase/vasopressinase-like leucyl-cystinyl aminopeptidase LNPEP, P-LAP, P-LAP/IRAP, P-LAP/OTase, placental leucil aminopeptidase, Placental leucine aminopeptidase, placental leucine aminopeptidase/oxytocinase, placental leucine aminopeptidase/oxytocinase/insulin-regulated membrane aminopeptidase, vasopressinase, vasopresssinase, Vesicle protein of 165 kDa, Vp165, yscXVI

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.11 Aminopeptidases
                3.4.11.3 cystinyl aminopeptidase

Inhibitors

Inhibitors on EC 3.4.11.3 - cystinyl aminopeptidase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2-[[(1-[[3-(4-hydroxybenzyl)-5-(L-norleucylamino)phenyl]carbonyl]-L-prolyl)amino]methyl]phenyl)acetic acid
-
-
(2-[[(1-[[3-(4-hydroxybenzyl)-5-(L-valylamino)phenyl]carbonyl]-L-prolyl)amino]methyl]phenyl)acetic acid
-
-
(2-[[(N-[[3-(4-hydroxybenzyl)-5-(L-norleucylamino)phenyl]carbonyl]-L-isoleucyl)amino]methyl]phenyl)acetic acid
-
-
(2-[[(N-[[3-(4-hydroxybenzyl)-5-(L-norleucylamino)phenyl]carbonyl]-L-leucyl)amino]methyl]phenyl)acetic acid
-
-
(2-[[(N-[[3-(4-hydroxybenzyl)-5-(L-valylamino)phenyl]carbonyl]-L-isoleucyl)amino]methyl]phenyl)acetic acid
-
-
(2-[[(N-[[3-amino-5-(4-hydroxybenzyl)phenyl]carbonyl]-L-isoleucyl)amino]methyl]phenyl)acetic acid
-
-
1,10-phenanthroline
1,16-bis(4-methyl-2,5-dioxo-3-furyl)hexadecane
-
tyromycin A
1,2-Acyclic oxytocin
-
slight inhibition of oxytocin degradation, marked inhibition of cystine di-beta-naphthylamide degradation
1-methyl-N-[3-(1H-tetrazol-5-yl)phenyl]-1H-indole-6-sulfonamide
2,2'-bipyridine
-
acetic acid-containing chelators potentiate the inhibitory effect of 2,2'-bipyridine. Efficiacy decreases in the order: diethylenetriamine-N,N,N',N'',N''-pentaacetic acid, EDTA, EGTA
2,2'-dipyridyl
-
-
2,4,5-trichloro-N-[3-(1H-tetrazol-5-yl)phenyl]benzene-1-sulfonamide
-
2,4,5-trichloro-N-[3-(1H-tetrazol-5-yl)phenyl]benzenesulfonamide
-
-
2-amino-4-(3,4-dimethoxyphenyl)-7-hydroxy-4H-chromene-3-carbonitrile
-
-
2-amino-4-(3,5-dimethoxyphenyl)-7-hydroxy-4H-chromene-3-carbonitrile
-
-
2-amino-4-[4-(dimethylamino)phenyl]-7-hydroxy-4H-chromene-3-carbonitrile
-
-
2-amino-7-hydroxy-4-(3,4,5-trimethoxyphenyl)-4H-chromene-3-carbonitrile
-
-
2-amino-7-hydroxy-4-(3-methoxyphenyl)-4H-chromene-3-carbonitrile
-
-
2-amino-7-hydroxy-4-(4-methoxyphenyl)-4H-chromene-3-carbonitrile
-
-
2-amino-7-hydroxy-4-(pyridin-4-yl)-4H-chromene-3-carbonitrile
-
-
2-mercaptoethanol
2-methoxyethyl 2-amino-7-hydroxy-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
-
2-[[(1-[[3-(4-hydroxybenzyl)-5-(L-norleucylamino)phenyl]carbonyl]-L-prolyl)amino]methyl]benzoic acid
-
-
2-[[(1-[[3-(4-hydroxybenzyl)-5-(L-valylamino)phenyl]carbonyl]-L-prolyl)amino]methyl]benzoic acid
-
-
2-[[(N-[[3-(4-hydroxybenzyl)-5-(L-norleucylamino)phenyl]carbonyl]-L-isoleucyl)amino]methyl]benzoic acid
-
-
2-[[(N-[[3-(4-hydroxybenzyl)-5-(L-norleucylamino)phenyl]carbonyl]-L-leucyl)amino]methyl]benzoic acid
-
-
2-[[(N-[[3-(4-hydroxybenzyl)-5-(L-valylamino)phenyl]carbonyl]-L-isoleucyl)amino]methyl]benzoic acid
-
-
3,4-dichloro-N-[3-(1H-tetrazol-5-yl)phenyl]benzene-1-sulfonamide
-
3,4-dichloro-N-[3-(1H-tetrazol-5-yl)phenyl]benzenesulfonamide
-
-
3,4-dimethyl-N-[3-(1H-tetrazol-5-yl)phenyl]benzene-1-sulfonamide
-
3,4-dimethyl-N-[3-(1H-tetrazol-5-yl)phenyl]benzenesulfonamide
-
-
3-([(4-bromo-5-chlorothiophen-2-yl)sulfonyl]amino)-N-methylbenzamide
-
-
3-[(4-bromo-5-chlorothiophene-2-sulfonyl)amino]-N-methylbenzamide
-
4,5-dichloro-N-[3-(1H-tetrazol-5-yl)phenyl]thiophene-2-sulfinamide
-
4,5-dichloro-N-[3-(1H-tetrazol-5-yl)phenyl]thiophene-2-sulfonamide
4-amino-3-(L-arginylamino)benzoic acid
-
4-amino-3-(L-tyrosylamino)benzoic acid
-
4-amino-3-[(O-benzyl-L-tyrosyl)amino]benzoic acid
-
4-bromo-2,6-difluoro-N-[3-(1H-tetrazol-5-yl)phenyl]benzene-1-sulfonamide
-
4-bromo-2,6-difluoro-N-[3-(1H-tetrazol-5-yl)phenyl]benzenesulfonamide
-
-
4-bromo-2-fluoro-N-[3-(1H-tetrazol-5-yl)phenyl]benzene-1-sulfonamide
-
4-bromo-2-fluoro-N-[3-(1H-tetrazol-5-yl)phenyl]benzenesulfonamide
-
-
4-bromo-5-chloro-N-methyl-N-[3-(1H-tetrazol-5-yl)phenyl]thiophene-2-sulfonamide
4-bromo-5-chloro-N-[3-(1-methyl-1H-tetrazol-5-yl)phenyl]thiophene-2-sulfonamide
4-bromo-5-chloro-N-[3-(1H-tetrazol-5-yl)phenyl]thiophene-2-carboxamide
-
-
4-bromo-5-chloro-N-[3-(1H-tetrazol-5-yl)phenyl]thiophene-2-sulfonamide
7-chloro-N-[3-(1H-tetrazol-5-yl)phenyl]-1,3-dihydro-2,1,3-benzoxadiazole-4-sulfonamide
-
-
7-chloro-N-[3-(1H-tetrazol-5-yl)phenyl]-2,1,3-benzoxadiazole-4-sulfonamide
-
8-bromo-cGMP
-
-
8-hydroxyquinoline
-
-
amastatin
amino(phenyl)methyl phosphonic acid
-
Ang II
-
-
Ang IV
-
-
angiotensin
-
-
angiotensin 4-8
angiotensin II
angiotensin II(5-8)
-
-
angiotensin III
angiotensin IV
aprotonin
-
-
-
benzyl 2-amino-7-hydroxy-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
-
benzyl N-(3-amino-4-[[(2S)-2-amino-4-phenylbutanoyl]amino]benzoyl)-L-tryptophanate
-
benzyl N-(3-amino-4-[[(2S)-2-amino-4-phenylbutanoyl]amino]benzoyl)-L-valinate
-
benzyl N-(4-amino-3-[[(2S)-2-amino-4-phenylbutanoyl]amino]benzoyl)-L-tryptophanate
-
benzyl N-[3-amino-4-(L-leucylamino)benzoyl]-L-tryptophanate
-
benzyl N-[3-amino-4-(L-norleucylamino)benzoyl]-L-tryptophanate
-
benzyl N-[3-amino-4-(L-norleucylamino)benzoyl]-L-valinate
-
benzyl N-[3-amino-4-([(2S)-2-amino-4-[4-(benzyloxy)phenyl]butanoyl]amino)benzoyl]-L-tryptophanate
-
benzyl N-[3-amino-4-[(O-benzyl-L-tyrosyl)amino]benzoyl]-L-tryptophanate
-
benzyl N-[4-amino-3-(D-norleucylamino)benzoyl]-L-valinate
-
benzyl N-[4-amino-3-(L-norleucylamino)benzoyl]-L-tryptophanate
-
benzyl N-[4-amino-3-(L-tyrosylamino)benzoyl]-L-tryptophanate
-
benzyl N-[4-amino-3-(L-tyrosylamino)benzoyl]-L-valinate
-
benzyl N-[4-amino-3-[(O-benzyl-L-tyrosyl)amino]benzoyl]-L-tryptophanate
-
bestatin
butyl 2-amino-7-hydroxy-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
-
Ca2+
-
slightly
cGMP
-
-
Cloxacillin
-
-
CuCl2
-
0.1 mM, 91% inhibition. 0.01 mM, 87% inhibition
cyclohexylmethyl 2-amino-7-hydroxy-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
50% inhibition at 100 microM
cysteine
diethylenetriamine-N,N,N',N'',N''-pentaacetic acid
-
weak
divalinal
divalinal-angiotensin IV
-
-
ethyl 2,7-diamino-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
50% inhibition at 100 microM
ethyl 2-(acetylamino)-7-hydroxy-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
-
ethyl 2-(acetylamino)-7-hydroxy-4-(quinolin-3-yl)-4H-chromene-3-carboxylate
-
-
ethyl 2-acetamido-7-hydroxy-4-(3-quinolinyl)-4H-chromene-3-carboxylate
HFI-437
ethyl 2-amino-4-(2,4-dichloropyridin-3-yl)-7-hydroxy-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-4-(2-cyanophenyl)-7-hydroxy-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-4-(3,4-dimethoxyphenyl)-7-hydroxy-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-4-(3-chlorophenyl)-7-hydroxy-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-4-(3-cyanophenyl)-7-hydroxy-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-4-(4-bromophenyl)-7-hydroxy-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-4-(4-chlorophenyl)-7-hydroxy-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-4-(4-cyanophenyl)-7-hydroxy-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-4-(5,8-dihydroquinolin-2-yl)-7-hydroxy-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-4-(pyridin-3-yl)-4H-benzo[g]chromene-3-carboxylate
-
-
ethyl 2-amino-4-(pyridin-3-yl)-4H-benzo[h]chromene-3-carboxylate
-
-
ethyl 2-amino-4-[4-(dimethylamino)phenyl]-7-hydroxy-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-6-bromo-7-hydroxy-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
50% inhibition at 100 microM
ethyl 2-amino-6-chloro-7-hydroxy-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-7-(dimethylamino)-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
50% inhibition at 100 microM
ethyl 2-amino-7-(formyloxy)-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
50% inhibition at 100 microM
ethyl 2-amino-7-hydroxy-4-(1,3-thiazol-2-yl)-4H-chromene-3-carboxylate
-
50% inhibition at 100 microM
ethyl 2-amino-7-hydroxy-4-(2-nitrophenyl)-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-7-hydroxy-4-(4-methylphenyl)-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-7-hydroxy-4-(4-nitrophenyl)-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-7-hydroxy-4-(pyridin-2-yl)-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-7-hydroxy-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-7-hydroxy-4-(pyridin-4-yl)-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-7-hydroxy-4-(quinolin-3-yl)-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-7-hydroxy-4-(quinolin-4-yl)-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-7-hydroxy-4-(thiophen-2-yl)-4H-chromene-3-carboxylate
-
50% inhibition at 100 microM
ethyl 2-amino-7-hydroxy-4-phenyl-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-7-hydroxy-4-[4-(pyridin-2-yl)phenyl]-4H-chromene-3-carboxylate
-
-
ethyl 2-amino-7-methoxy-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
50% inhibition at 100 microM
ethyl 2-amino-8-hydroxy-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
-
Fe2+
-
-
HA-08
a macrocyclic IRAP inhibitor
HCO3-
-
-
indomethacin
-
-
iodoacetic acid
L-Arg-vasopressin
-
Ki-value for wild-type, mutants G428E, G428D, G428Q above 0.03 mM
L-Leu-enkephalin
-
-
L-leucine
-
-
L-methionine
-
form I inhibited, form II slightly activated
L-phenylalanine
-
-
L-trans-epoxysuccinyl-leucinamido(4-guanidino)-butane
-
E64
L-tyrosine
-
-
L-Val-L-Tyr-L-Ile-2-aminomethylphenylacetic acid
-
inhibits both IRAP and aminopeptidase N and induces proliferation of stem cells at low concentrations
L-Val-L-Tyr-L-Ile-L-Cys-L-Pro-L-Cys
-
cyclic disulfide, angiotensin IV analog, considerably more stable than angiotensin IV toward enzymatic degradation
L-Val-L-Tyr-L-Ile-L-His-L-Pro-L-cyclohexylalanine
-
-
L-Val-L-Tyr-L-Ile-L-His-L-Pro-L-Phe
Leu-Val-Val-haemorphin 7
-
-
leupeptin
-
0.1 mM, 53% inhibition
LVV hemorphin 7
LVV-H7, IRAP ligands are on the one hand competitive inhibitors of the enzymatic activity of IRAP and on the other hand regulators of its trafficking
LVV-H7
LVV-haemorphin-7
-
-
LVV-hemorphin 7
methyl 2-amino-7-hydroxy-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
-
methyl 3-amino-4-(L-arginylamino)benzoate
-
methyl 3-amino-4-(L-norleucylamino)benzoate
-
methyl 3-amino-4-(L-tyrosylamino)benzoate
-
methyl 3-amino-4-[(O-benzyl-L-tyrosyl)amino]benzoate
-
methyl 3-amino-4-[[(2S)-2-amino-4-phenylbutanoyl]amino]benzoate
-
methyl 4-amino-3-(L-arginylamino)benzoate
-
methyl 4-amino-3-(L-norleucylamino)benzoate
-
methyl 4-amino-3-(L-tyrosylamino)benzoate
-
methyl 4-amino-3-([(2S)-2-amino-4-[4-(benzyloxy)phenyl]butanoyl]amino)benzoate
-
methyl 4-amino-3-[(O-benzyl-L-tyrosyl)amino]benzoate
-
methyl 4-amino-3-[[(2S)-2-amino-4-(4-hydroxyphenyl)butanoyl]amino]benzoate
-
methyl N-(3,4-diaminobenzoyl)-L-tyrosinate
-
methyl N-(3-amino-4-[[(2S)-2-amino-4-phenylbutanoyl]amino]benzoyl)-L-tyrosinate
-
methyl N-(4-amino-3-[[(2S)-2-amino-4-phenylbutanoyl]amino]benzoyl)-L-tyrosinate
-
methyl N-[3-amino-4-(L-arginylamino)benzoyl]-L-tyrosinate
-
methyl N-[3-amino-4-(L-norleucylamino)benzoyl]-L-tyrosinate
-
methyl N-[3-amino-4-(L-tyrosylamino)benzoyl]-L-tyrosinate
-
methyl N-[3-amino-4-[(O-benzyl-L-tyrosyl)amino]benzoyl]-L-tyrosinate
-
methyl N-[4-amino-3-(D-norleucylamino)benzoyl]-D-tyrosinate
-
methyl N-[4-amino-3-(L-arginylamino)benzoyl]-D-tyrosinate
-
methyl N-[4-amino-3-(L-tyrosylamino)benzoyl]-L-threoninate
-
methyl N-[4-amino-3-(L-tyrosylamino)benzoyl]-L-tyrosinate
-
methyl N2-(3,4-diaminobenzoyl)-L-argininate
-
methyl N2-(3,4-diaminobenzoyl)-L-lysinate
-
methyl N2-(3-amino-4-[[(2S)-2-amino-4-phenylbutanoyl]amino]benzoyl)-L-argininate
-
methyl N2-(3-amino-4-[[(2S)-2-amino-4-phenylbutanoyl]amino]benzoyl)-L-lysinate
-
methyl N2-(4-amino-3-[[(2S)-2-amino-4-(4-hydroxyphenyl)butanoyl]amino]benzoyl)-L-lysinate
-
methyl N2-(4-amino-3-[[(2S)-2-amino-4-phenylbutanoyl]amino]benzoyl)-L-lysinate
-
methyl N2-[3-amino-4-(L-arginylamino)benzoyl]-L-lysinate
-
methyl N2-[3-amino-4-(L-leucylamino)benzoyl]-L-lysinate
-
methyl N2-[3-amino-4-(L-norleucylamino)benzoyl]-L-lysinate
-
methyl N2-[3-amino-4-(L-tyrosylamino)benzoyl]-L-lysinate
-
methyl N2-[4-amino-3-(L-norleucylamino)benzoyl]-D-argininate
-
methyl N2-[4-amino-3-(L-norleucylamino)benzoyl]-L-lysinate
-
methyl N2-[4-amino-3-([(2S)-2-amino-4-[4-(benzyloxy)phenyl]butanoyl]amino)benzoyl]-L-lysinate
-
N-(3,4-diaminobenzoyl)-L-tryptophan
-
N-(3-(1H-tetrazol-5-yl)phenyl)-2,3,4-trichlorobenzenesulfonamide
-
N-(3-(1H-tetrazol-5-yl)phenyl)-2,5-bis(trifluoromethyl)-benzenesulfonamide
-
N-(3-(1H-tetrazol-5-yl)phenyl)-2-fluoro-5-(trifluoromethyl)benzenesulfonamide
-
N-(3-(1H-tetrazol-5-yl)phenyl)-3,4-difluorobenzenesulfonamide
-
N-(3-(1H-tetrazol-5-yl)phenyl)-3,5-bis(trifluoromethyl)-benzenesulfonamide
-
N-(3-(1H-tetrazol-5-yl)phenyl)-3-fluoro-4-(trifluoromethyl)benzenesulfonamide
-
N-(3-(1H-tetrazol-5-yl)phenyl)-3-methyl-4-(trifluoromethyl)benzenesulfonamide
-
N-(3-(1H-tetrazol-5-yl)phenyl)-4-methyl-3-(trifluoromethyl)benzenesulfonamide
-
N-(3-amino-4-[[(2S)-2-amino-4-(4-hydroxyphenyl)butanoyl]amino]benzoyl)-L-tryptophan
-
N-(3-amino-4-[[(2S)-2-amino-4-phenylbutanoyl]amino]benzoyl)-L-valine
-
N-(4-amino-3-[[(2R)-2-amino-4-(4-hydroxyphenyl)butanoyl]amino]benzoyl)-L-tryptophan
-
N-alpha-tosyl-L-lysylchloromethane
-
-
N-ethylmaleimide
-
-
N-hexanoyl-L-Tyr-L-Ile
a dipeptide derivative from Ang IV, a strong cognitive enhancer and enzyme inhibitor
N-[3-(1H-tetrazol-5-yl)phenyl]-1-benzothiophene-2-sulfonamide
N-[3-(1H-tetrazol-5-yl)phenyl]-2-benzothiophene-1-sulfonamide
-
N-[3-(1H-tetrazol-5-yl)phenyl]-2-benzothiophene-4-sulfonamide
-
-
N-[3-(1H-tetrazol-5-yl)phenyl]benzenesulfonamide
N-[3-(1H-tetrazol-5-yl)phenyl]biphenyl-4-sulfonamide
-
-
N-[3-(1H-tetrazol-5-yl)phenyl]pyridine-3-sulfonamide
N-[3-(1H-tetrazol-5-yl)phenyl]thiophene-2-sulfonamide
N-[3-(1H-tetrazol-5-yl)phenyl][1,1'-biphenyl]-4-sulfonamide
-
N-[3-amino-4-(L-arginylamino)benzoyl]-L-tryptophan
-
N-[3-amino-4-(L-norleucylamino)benzoyl]-L-tryptophan
-
N-[3-amino-4-(L-norleucylamino)benzoyl]-L-valine
-
N-[3-amino-4-(L-tyrosylamino)benzoyl]-L-tryptophan
-
N-[4-amino-3-(D-norleucylamino)benzoyl]-L-valine
-
N-[4-amino-3-(L-arginylamino)benzoyl]-L-tryptophan
-
N-[4-amino-3-(L-arginylamino)benzoyl]-L-valine
-
N-[4-amino-3-(L-norleucylamino)benzoyl]-L-tryptophan
-
N-[4-amino-3-(L-tyrosylamino)benzoyl]-L-tryptophan
-
N-[4-amino-3-(L-tyrosylamino)benzoyl]-L-valine
-
N-[[3-(4-hydroxybenzyl)-5-(L-valylamino)phenyl]carbonyl]-L-isoleucine
-
-
N-[[3-(4-hydroxybenzyl)-5-(L-valylamino)phenyl]carbonyl]-L-isoleucyl-L-histidyl-L-prolyl-L-phenylalanine
-
-
N2-(2- 8[(1-amino-3-phenylpropyl)(hydroxy)phosphoryl]methyl]-4-methylpentanoyl)-L-lysyl-L-histidyl-L-histidyl-L-alanyl-L-phenylalanyl-L-seryl-L-phenylalanyl-L-lysine
i.e. DG025, an antigenic peptide precursor analogue, enzyme binding structure determination and analysis. The canonical orientation of the two N-terminal residues of DG025 is defined by the transition state nature of the ligand and the hydrophobic and aromatic interactions of the hPhe residue in the S1 specificity pocket of the enzyme (and in particular with Phe544). The remaining of the peptide extends toward the base of the cavity, where it is sandwiched between domains II and IV
N2-(4-amino-3-[[(2S)-2-amino-4-phenylbutanoyl]amino]benzoyl)-L-ornithine
-
N2-[4-amino-3-(L-leucylamino)benzoyl]-L-lysine
-
N2-[4-amino-3-(L-phenylalanylamino)benzoyl]-L-lysine
-
N2-[4-amino-3-(L-tyrosylamino)benzoyl]-L-lysine
-
NaCN
-
-
p-chloromercuribenzoate
p-hydroxymercuribenzoate
-
-
pepstatin A
-
0.1 mM, 70% inhibition
Polyphloretin phosphate
-
-
porcine ACTH(1-39)
-
-
-
propyl 2-amino-7-hydroxy-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
-
prostaglandin E-1
prostaglandin E2
prostaglandin F-2alpha
puromycin
-
0.1 mM, 36% inhibition. 0.01 mM, 5% inhibition
S-Benzyl-L-cysteinyl-L-prolyl-L-leucyl-glycinamide
-
-
S-benzylcysteine
-
and S-benzylcysteine containing peptides
Somatostatin
-
-
tert-butyl 2-amino-7-hydroxy-4-(pyridin-3-yl)-4H-chromene-3-carboxylate
-
-
tosylphenylalanine-chloromethane
-
-
Urea
-
-
ZnCl2
-
0.1 mM, 98% inhibition. 0.01 mM, 77% inhibition
[(5R)-6-amino-5-benzyl-2-(2,2-diphenylethyl)-3,6-dioxohexyl][(1R)-1-amino-3-phenylpropyl]phosphinic acid
i.e. DG026, a phosphinic pseudotripeptide that acts as very potent inhibitor of IRAP. DG026 is able to selectively downregulate IRAP-dependent cross-presentation by dendritic cells but leave ERAP1-dependent cross-presentation unaffected. Enzyme binding structure determination and analysis, overview
[2-amino-7-hydroxy-4-(pyridin-3-yl)-4H-chromen-3-yl](phenyl)methanone
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50% inhibition at 100 microM
[2-[([[3-(4-hydroxybenzyl)-5-(L-valylamino)phenyl]carbonyl]amino)methyl]phenyl]acetic acid
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[2-[([[3-amino-5-(4-hydroxybenzyl)phenyl]carbonyl]amino)methyl]phenyl]acetic acid
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additional information
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