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Synonyms
kallikrein, prekallikrein, plasma kallikrein, urinary kallikrein, kininogenase, plasma prekallikrein, plasma pk, pancreatic kallikrein, klk13, klkb1,
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factor XII + H2O
?
activation of the factor XII, bound to negatively charged surfaces
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?, ir
kininogen + H2O
bradykinin + fragments of kininogen
high-molecular weight kininogen
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?, ir
kininogen + H2O
bradykinin + ?
kininogen + H2O
bradykinin + fragments of kininogen
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-
-
-
?
N-benzyloxycarbonyl-Ala-Lys-Arg-4-methylcoumarin 7-amide
N-benzyloxycarbonyl-Ala-Lys-Arg + 7-amino-4-methylcoumarin
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-
-
-
?
o-aminobenzoyl-GEFIKKSSFQ-N-(2,4-dinitrophenyl)-ethylene diamine + H2O
o-aminobenzoyl-GEFIK + KSSFQ-N-(2,4-dinitrophenyl)-ethylene diamine
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synthetic fluorogenic substrate
67% of product formation, identification by mass spectroscopy
?
o-aminobenzoyl-GEFIKKSSFQ-N-(2,4-dinitrophenyl)-ethylene diamine + H2O
o-aminobenzoyl-GEFIKK + SSFQ-N-(2,4-dinitrophenyl)-ethylene diamine
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synthetic fluorogenic substrate
33% of product formation, identification by mass spectroscopy
?
o-aminobenzoyl-GEFIKKSSFTNVTQ-N-(2,4-dinitrophenyl)-ethylene diamine + H2O
o-aminobenzoyl-GEFIK + KSSFTNVTQ-N-(2,4-dinitrophenyl)-ethylene diamine
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synthetic fluorogenic substrate
62% of product formation, identification by mass spectroscopy
?
o-aminobenzoyl-GEFIKKSSFTNVTQ-N-(2,4-dinitrophenyl)-ethylene diamine + H2O
o-aminobenzoyl-GEFIKK + SSFTNVTQ-N-(2,4-dinitrophenyl)-ethylene diamine
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synthetic fluorogenic substrate
38% of product formation, identification by mass spectroscopy
?
o-aminobenzoyl-IKKSSF-N-(2,4-dinitrophenyl)-ethylene diamine + H2O
o-aminobenzoyl-IKK + SSF-N-(2,4-dinitrophenyl)-ethylene diamine
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synthetic fluorogenic substrate
identification by mass spectroscopy
?
Prorenin + H2O
Renin + ?
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rat prorenin, very low activity
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ir
additional information
?
-
Prorenin + H2O
Renin + ?
activation of prorenin
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ir
Prorenin + H2O
Renin + ?
activation of prorenin, involved in the renin-angiotensin system
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ir
kininogen + H2O
bradykinin + ?
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-
-
?
kininogen + H2O
bradykinin + ?
-
-
-
-
?
additional information
?
-
belongs to the peptidase family S1, plasma kallikrein subfamily
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?
additional information
?
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-
substrate specificity requirements, very low activity with the equivalent of rat prorenin to the cleavage site and with the peptide o-aminobenzoyl-NVTSPVQ-N-(2,4-dinitrophenyl)-ethylene diamine, activation of rat prorenin requires a different enzyme and/or mechanism
-
?
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1-benzyl-1H-pyrazole-4-carboxylic acid 4-carbamimidoyl-benzylamide
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ASP-440, small molecule inhibitor of plasma kallikrein
2-[3'-acetyl-5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxybiphenyl-3-yl]butanedioic acid
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-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-2',6-dihydroxybiphenyl-3-yl]butanedioic acid
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-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-2'-fluoro-6-hydroxybiphenyl-3-yl]butanedioic acid
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-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3',6-dihydroxybiphenyl-3-yl]butanedioic acid
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-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-carbamoyl-6-hydroxybiphenyl-3-yl]butanedioic acid
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inhibitor with the best potency and selectivity profile for plasma kallikrein versus related serine proteases. This compound is highly stable in vivo and could be further developed for the treatment and inflammatory or coagulation disorders. Pharmacokinetic data
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-chloro-6-hydroxybiphenyl-3-yl]butanedioic acid
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-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-cyano-6-hydroxybiphenyl-3-yl]butanedioic acid
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-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-4'-chloro-6-hydroxybiphenyl-3-yl]butanedioic acid
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-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-2'-methoxybiphenyl-3-yl]butanedioic acid
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-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-2'-methylbiphenyl-3-yl]butanedioic acid
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-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-methoxybiphenyl-3-yl]butanedioic acid
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2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-methylbiphenyl-3-yl]butanedioic acid
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-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-4'-methoxybiphenyl-3-yl]butanedioic acid
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-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-4'-methylbiphenyl-3-yl]butanedioic acid
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2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxybiphenyl-3-yl]butanedioic acid
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bicyclic peptide Ac-CiS1F2[Aze]3Y4[HArg]5Cii[Ala(PsiCH2-NH)]6H7Q8D9L10Ciii
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-
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bicyclic peptide Ac-CiS1W2P3A4R5CiiL6H7Q8D9L10Ciii
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-
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diisopropylfluorophosphate
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-
human IgG1 monoclonal antibody DX-2930
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potently and specifically inhibits plasma kallikrein
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Soybean trypsin inhibitor
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-
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0.000006
2-[3'-acetyl-5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
0.000013
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-2',6-dihydroxybiphenyl-3-yl]butanedioic acid
-
-
0.000012
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-2'-fluoro-6-hydroxybiphenyl-3-yl]butanedioic acid
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-
0.000003
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3',6-dihydroxybiphenyl-3-yl]butanedioic acid
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-
0.0000005
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-carbamoyl-6-hydroxybiphenyl-3-yl]butanedioic acid
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-
0.000003 - 0.000065
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-chloro-6-hydroxybiphenyl-3-yl]butanedioic acid
0.00001
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-cyano-6-hydroxybiphenyl-3-yl]butanedioic acid
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-
0.000037
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-4'-chloro-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
0.000006
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-2'-methoxybiphenyl-3-yl]butanedioic acid
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-
0.000006
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-2'-methylbiphenyl-3-yl]butanedioic acid
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-
0.000005
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-methoxybiphenyl-3-yl]butanedioic acid
-
-
0.000004
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-methylbiphenyl-3-yl]butanedioic acid
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-
0.000027
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-4'-methoxybiphenyl-3-yl]butanedioic acid
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-
0.000018
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-4'-methylbiphenyl-3-yl]butanedioic acid
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-
0.0000008
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxybiphenyl-3-yl]butanedioic acid
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-
0.00000017
human IgG1 monoclonal antibody DX-2930
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at pH 7.5 and 30°C
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0.000003
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-chloro-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
0.000065
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-chloro-6-hydroxybiphenyl-3-yl]butanedioic acid
-
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
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Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
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Paquin, J.; Benjannet, S.; Sawyer, N.; Lazure, C.; Chretien, M.; Seidah, N.G.
Rat plasma kallikrein: purification, NH2-terminal sequencing and development of a specific radioimmunoassay
Biochim. Biophys. Acta
999
103-110
1989
Rattus norvegicus
brenda
Boeckmann, B.; Bairoch, A.; Apweiler, R.; Blatter, M.C.; Estreicher, A.; Gasteiger, E.; Martin M.J.; Michoud, K.; O'Donovan, C.; Phan, I.; Pilbout, S.; Schneider, M.
The SWISS-PROT protein knowledgebase and its supplement TrEMBL
Nucleic Acids Res.
31
365-370
2003
Homo sapiens (P03952), Mus musculus (P26262), Rattus norvegicus (P14272)
brenda
Almeida, P.C.; Chagas, J.R.; Cezari, M.H.; Juliano, M.A.; Juliano, L.
Hydrolysis by plasma kallikrein of fluorogenic peptides derived from prorenin processing site
Biochim. Biophys. Acta
1479
83-90
2000
Homo sapiens, Rattus norvegicus
brenda
Neth, P.; Arnhold, M.; Sidarovich, V.; Bhoola, K.D.; Fink, E.
Expression of the plasma prekallikrein gene: utilization of multiple transcription start sites and alternative promoter regions
Biol. Chem.
386
101-109
2005
Homo sapiens, Rattus norvegicus
brenda
Young, W.B.; Rai, R.; Shrader, W.D.; Burgess-Henry, J.; Hu, H.; Elrod, K.C.; Sprengeler, P.A.; Katz, B.A.; Sukbuntherng, J.; Mordenti, J.
Small molecule inhibitors of plasma kallikrein
Bioorg. Med. Chem. Lett.
16
2034-2036
2006
Rattus norvegicus
brenda
Phipps, J.A.; Clermont, A.C.; Sinha, S.; Chilcote, T.J.; Bursell, S.E.; Feener, E.P.
Plasma kallikrein mediates angiotensin II type 1 receptor-stimulated retinal vascular permeability
Hypertension
53
175-181
2009
Rattus norvegicus
brenda
Liu, J.; Gao, B.B.; Clermont, A.C.; Blair, P.; Chilcote, T.J.; Sinha, S.; Flaumenhaft, R.; Feener, E.P.
Hyperglycemia-induced cerebral hematoma expansion is mediated by plasma kallikrein
Nat. Med.
17
206-210
2011
Rattus norvegicus
brenda
Kenniston, J.; Faucette, R.; Martik, D.; Comeau, S.; Lindberg, A.; Kopacz, K.; Conley, G.; Chen, J.; Viswanathan, M.; Kastrapeli, N.; Cosic, J.; Mason, S.; DiLeo, M.; Abendroth, J.; Kuzmic, P.; Ladner, R.; Edwards, T.; TenHoor, C.; Adelman, B.; Nixon, A.;
Inhibition of plasma kallikrein by a highly specific active site blocking antibody
J. Biol. Chem.
289
23596-23608
2014
Macaca fascicularis, Mus musculus, Rattus norvegicus, Homo sapiens (P03952), Homo sapiens
brenda
Teufel, D.P.; Bennett, G.; Harrison, H.; van Rietschoten, K.; Pavan, S.; Stace, C.; Le Floch, F.; Van Bergen, T.; Vermassen, E.; Barbeaux, P.; Hu, T.T.; Feyen, J.H.M.; Vanhove, M.
Stable and long-lasting, novel bicyclic peptide plasma kallikrein inhibitors for the treatment of diabetic macular edema
J. Med. Chem.
61
2823-2836
2018
Rattus norvegicus
brenda