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Literature summary for 3.4.22.34 extracted from

  • Ovat, A.; Muindi, F.; Fagan, C.; Brouner, M.; Hansell, E.; Dvorak, J.; Sojka, D.; Kopacek, P.; McKerrow, J.H.; Caffrey, C.R.; Powers, J.C.
    Aza-peptidyl Michael acceptor and epoxide inhibitors--potent and selective inhibitors of Schistosoma mansoni and Ixodes ricinus legumains (asparaginyl endopeptidases) (2009), J. Med. Chem., 52, 7192-7210.
    View publication on PubMed
Search for more literature for 3.4.22.34

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Pichia pastoris Schistosoma mansoni
expressed in Pichia pastoris Ixodes ricinus

Inhibitors

Inhibitors Comment Organism Structure
Boc-azaAsn-CH=CH-COOEt
-
 Ixodes ricinus
Boc-Piz-Ala-Ala-azaAsn-CH=CH-CON(Bzl)2
-
 Ixodes ricinus
Boc-Piz-Ala-Ala-azaAsn-CH=CH-CON(Bzl)2
-
 Schistosoma mansoni
Boc-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
-
 Ixodes ricinus
Boc-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
-
 Schistosoma mansoni
Boc-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH3)CH2-1-naphthyl
-
 Ixodes ricinus
Boc-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH3)CH2-1-naphthyl
-
 Schistosoma mansoni
Boc-Piz-Ala-Ala-azaAsn-CH=CH-COOBzl
-
 Ixodes ricinus
Boc-Piz-Ala-Ala-azaAsn-CH=CH-COOBzl
-
 Schistosoma mansoni
Boc-Piz-Ala-Ala-azaAsn-CH=CH-COOEt
-
 Ixodes ricinus
Boc-Piz-Ala-Ala-azaAsn-CH=CH-COOEt
-
 Schistosoma mansoni
Boc-Piz-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
-
 Ixodes ricinus
Boc-Piz-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
-
 Schistosoma mansoni
Cbz-Ala-Ala-azaAsn-CH=CH-COOEt
-
 Ixodes ricinus
Cbz-Ala-Ala-azaAsn-CH=CH-COOEt
-
 Schistosoma mansoni
Cbz-Ala-Ile-azaAsn-CH=CH-COOEt
-
 Ixodes ricinus
Cbz-Ala-Ile-azaAsn-CH=CH-COOEt
-
 Schistosoma mansoni
CBZ-Ala-Phe-azaAsn-CH=CH-CO-tetrahydroisoquinoline
-
 Ixodes ricinus
CBZ-Ala-Phe-azaAsn-CH=CH-CONHCH2-furyl
-
 Ixodes ricinus
Cbz-Ala-Val-azaAsn-CH=CH-CO-tetrahydroquinoline
-
 Ixodes ricinus
Cbz-Ala-Val-azaAsn-CH=CH-CO-tetrahydroquinoline
-
 Schistosoma mansoni
Cbz-Ala-Val-azaAsn-CH=CH-CONHCH2-1-naphthyl
-
 Ixodes ricinus
Cbz-Ala-Val-azaAsn-CH=CH-CONHCH2-1-naphthyl
-
 Schistosoma mansoni
Cbz-Ala-Val-azaAsn-CH=CH-COOEt
-
 Ixodes ricinus
Cbz-Ala-Val-azaAsn-CH=CH-COOEt
-
 Schistosoma mansoni
Cbz-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
-
 Ixodes ricinus
Cbz-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
-
 Schistosoma mansoni
Cbz-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH3)CH2-1-naphthyl
-
 Ixodes ricinus
Cbz-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH3)CH2-1-naphthyl
-
 Schistosoma mansoni
Cbz-Piz-Ala-Ala-azaAsn-CH=CH-COOEt
-
 Ixodes ricinus
Cbz-Piz-Ala-Ala-azaAsn-CH=CH-COOEt
-
 Schistosoma mansoni
Cbz-Piz-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
-
 Ixodes ricinus
Cbz-Piz-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
-
 Schistosoma mansoni
Cbz-Piz-Ala-azaAsn-CH=CH-CO-tetrahydroquinoline
-
 Ixodes ricinus
Cbz-Piz-Ala-azaAsn-CH=CH-CO-tetrahydroquinoline
-
 Schistosoma mansoni
Mu-Ala-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
-
 Ixodes ricinus
Mu-Ala-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
-
 Schistosoma mansoni
Mu-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
-
 Ixodes ricinus
Mu-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
-
 Schistosoma mansoni
Mu-Ala-Ala-azaAsn-CH=CH-CONHCH2CH2CH2Ph
-
 Schistosoma mansoni
Mu-Ala-Ala-azaAsn-CH=CH-COOEt
-
 Ixodes ricinus
Mu-Ala-Ala-azaAsn-CH=CH-COOEt
-
 Schistosoma mansoni
Mu-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
-
 Ixodes ricinus
Mu-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
-
 Schistosoma mansoni
Mu-Ala-Ala-azaAsn-EP(S,S)-CONHCH2-1-naphthyl
-
 Ixodes ricinus
Mu-Ala-Ala-azaAsn-EP(S,S)-CONHCH2-1-naphthyl
-
 Schistosoma mansoni
Mu-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
-
 Ixodes ricinus
Mu-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
-
 Schistosoma mansoni
Pip-Ala-Ala-azaAsn-CH=CH-CON(Bzl)-CH2-1-naphthyl
-
 Ixodes ricinus
Pip-Ala-Ala-azaAsn-CH=CH-CON(Bzl)-CH2-1-naphthyl
-
 Schistosoma mansoni
Pip-Ala-Ala-azaAsn-CH=CH-CON(Bzl)2
-
 Ixodes ricinus
Pip-Ala-Ala-azaAsn-CH=CH-CON(Bzl)2
-
 Schistosoma mansoni
Pip-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
-
 Ixodes ricinus
Pip-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
-
 Schistosoma mansoni
Pip-Ala-Ala-azaAsn-CH=CH-CONHCH2CH2Ph
-
 Ixodes ricinus
Pip-Ala-Ala-azaAsn-CH=CH-CONHCH2CH2Ph
-
 Schistosoma mansoni
Pip-Ala-Ala-azaAsn-CH=CH-COOEt
-
 Ixodes ricinus
Pip-Ala-Ala-azaAsn-CH=CH-COOEt
-
 Schistosoma mansoni
Pip-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
-
 Ixodes ricinus
Pip-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
-
 Schistosoma mansoni
Pip-Ala-Ala-azaAsn-EP(S,S)-CONHCH2-1-naphthyl
-
 Ixodes ricinus
Pip-Ala-Ala-azaAsn-EP(S,S)-CONHCH2-1-naphthyl
-
 Schistosoma mansoni
Pip-Ala-Ala-azaAsn-EP(S,S)-COOEt
-
 Ixodes ricinus
Pip-Ala-Ala-azaAsn-EP(S,S)-COOEt
-
 Schistosoma mansoni
Pip-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
-
 Ixodes ricinus
Pip-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
-
 Schistosoma mansoni
Piz-Ala-Ala-azaAsn-CH=CH-CON(Bzl)2
-
 Ixodes ricinus
Piz-Ala-Ala-azaAsn-CH=CH-CON(Bzl)2
-
 Schistosoma mansoni
Piz-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
-
 Ixodes ricinus
Piz-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
-
 Schistosoma mansoni
Piz-Ala-Ala-azaAsn-CH=CH-CON(CH3)CH2-1-naphthyl
-
 Ixodes ricinus
Piz-Ala-Ala-azaAsn-CH=CH-CON(CH3)CH2-1-naphthyl
-
 Schistosoma mansoni
Piz-Ala-Ala-azaAsn-CH=CH-COOBzl
-
 Ixodes ricinus
Piz-Ala-Ala-azaAsn-CH=CH-COOBzl
-
 Schistosoma mansoni
Piz-Ala-Ala-azaAsn-CH=CH-COOEt
-
 Ixodes ricinus
Piz-Ala-Ala-azaAsn-CH=CH-COOEt
-
 Schistosoma mansoni
Piz-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
-
 Ixodes ricinus
Piz-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
-
 Schistosoma mansoni

Organism

Organism UniProt Comment Textmining
Ixodes ricinus
-
-
-
Schistosoma mansoni
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Schistosoma mansoni
-
 Ixodes ricinus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Cbz-Ala-Ala-azaAsn-7-amido-4-methyl-coumarin + H2O
-
 Schistosoma mansoni ?
-
 ?
Cbz-Ala-Ala-azaAsn-7-amido-4-methyl-coumarin + H2O
-
 Ixodes ricinus ?
-
 ?

Synonyms

Synonyms Comment Organism
Asparaginyl endopeptidase
-
 Schistosoma mansoni
Asparaginyl endopeptidase
-
 Ixodes ricinus
legumain
-
 Schistosoma mansoni
legumain
-
 Ixodes ricinus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000014
-
 pH 6.8, 25°C Ixodes ricinus Cbz-Piz-Ala-Ala-azaAsn-CH=CH-COOEt
0.00000023
-
 pH 6.8, 25°C Ixodes ricinus Mu-Ala-Ala-azaAsn-CH=CH-COOEt
0.00000035
-
 pH 6.8, 25°C Ixodes ricinus Cbz-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH3)CH2-1-naphthyl
0.00000037
-
 pH 6.8, 25°C Ixodes ricinus Cbz-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
0.00000052
-
 pH 6.8, 25°C Ixodes ricinus Cbz-Ala-Ile-azaAsn-CH=CH-COOEt
0.0000017
-
 pH 6.8, 25°C Ixodes ricinus Mu-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
0.0000024
-
 pH 6.8, 25°C Ixodes ricinus Pip-Ala-Ala-azaAsn-CH=CH-CON(Bzl)-CH2-1-naphthyl
0.0000026
-
 pH 6.8, 25°C Ixodes ricinus Piz-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
0.0000033
-
 pH 6.8, 25°C Ixodes ricinus Mu-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
0.0000038
-
 pH 6.8, 25°C Ixodes ricinus Piz-Ala-Ala-azaAsn-CH=CH-CON(CH3)CH2-1-naphthyl
0.0000045
-
 pH 6.8, 25°C Ixodes ricinus Cbz-Ala-Ala-azaAsn-CH=CH-COOEt
0.000005
-
 pH 6.8, 25°C Ixodes ricinus Boc-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
0.000006
-
 pH 6.8, 25°C Ixodes ricinus Mu-Ala-Ala-azaAsn-EP(S,S)-CONHCH2-1-naphthyl
0.0000075
-
 pH 6.8, 25°C Ixodes ricinus Boc-Piz-Ala-Ala-azaAsn-CH=CH-COOBzl
0.000008
-
 pH 6.8, 25°C Ixodes ricinus Pip-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
0.0000085
-
 pH 6.8, 25°C Ixodes ricinus Piz-Ala-Ala-azaAsn-CH=CH-COOEt
0.0000085
-
 pH 6.8, 25°C Ixodes ricinus Boc-Piz-Ala-Ala-azaAsn-CH=CH-COOEt
0.0000085
-
 pH 6.8, 25°C Ixodes ricinus Pip-Ala-Ala-azaAsn-EP(S,S)-CONHCH2-1-naphthyl
0.000011
-
 pH 6.8, 25°C Ixodes ricinus Piz-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
0.000012
-
 pH 6.8, 25°C Ixodes ricinus Pip-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
0.000013
-
 pH 6.8, 25°C Ixodes ricinus Cbz-Ala-Val-azaAsn-CH=CH-CO-tetrahydroquinoline
0.000013
-
 pH 6.8, 25°C Ixodes ricinus Piz-Ala-Ala-azaAsn-CH=CH-COOBzl
0.000015
-
 pH 6.8, 25°C Ixodes ricinus Pip-Ala-Ala-azaAsn-CH=CH-COOEt
0.000017
-
 pH 6.8, 25°C Ixodes ricinus Pip-Ala-Ala-azaAsn-CH=CH-CON(Bzl)2
0.00002
-
 pH 6.8, 25°C Ixodes ricinus Boc-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH3)CH2-1-naphthyl
0.00003
-
 pH 6.8, 25°C Ixodes ricinus Boc-Piz-Ala-Ala-azaAsn-CH=CH-CON(Bzl)2
0.00003
-
 pH 6.8, 25°C Ixodes ricinus Pip-Ala-Ala-azaAsn-EP(S,S)-COOEt
0.000031
-
 pH 6.8, 25°C Ixodes ricinus Piz-Ala-Ala-azaAsn-CH=CH-CON(Bzl)2
0.000031
-
 pH 6.8, 25°C Schistosoma mansoni Cbz-Ala-Ala-azaAsn-CH=CH-COOEt
0.00004
-
 pH 6.8, 25°C Schistosoma mansoni Piz-Ala-Ala-azaAsn-CH=CH-CON(CH3)CH2-1-naphthyl
0.000045
-
 pH 6.8, 25°C Schistosoma mansoni Mu-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
0.000045
-
 pH 6.8, 25°C Schistosoma mansoni Boc-Piz-Ala-Ala-azaAsn-CH=CH-COOBzl
0.000045
-
 pH 6.8, 25°C Schistosoma mansoni Boc-Piz-Ala-Ala-azaAsn-CH=CH-CON(Bzl)2
0.00005
-
 pH 6.8, 25°C Schistosoma mansoni Cbz-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
0.000057
-
 pH 6.8, 25°C Schistosoma mansoni Pip-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
0.000058
-
 pH 6.8, 25°C Schistosoma mansoni Boc-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH3)CH2-1-naphthyl
0.00006
-
 pH 6.8, 25°C Schistosoma mansoni Mu-Ala-Ala-azaAsn-EP(S,S)-CONHCH2-1-naphthyl
0.000065
-
 pH 6.8, 25°C Ixodes ricinus Mu-Ala-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
0.000065
-
 pH 6.8, 25°C Ixodes ricinus Cbz-Ala-Val-azaAsn-CH=CH-COOEt
0.000068
-
 pH 6.8, 25°C Schistosoma mansoni Boc-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
0.00007
-
 pH 6.8, 25°C Schistosoma mansoni Piz-Ala-Ala-azaAsn-CH=CH-CON(CH2-1-naphthyl)2
0.00007
-
 pH 6.8, 25°C Schistosoma mansoni Cbz-Piz-Ala-Ala-azaAsn-CH=CH-COOEt
0.00007
-
 pH 6.8, 25°C Schistosoma mansoni Cbz-Piz-Ala-Ala-azaAsn-CH=CH-CON(CH3)CH2-1-naphthyl
0.000072
-
 pH 6.8, 25°C Schistosoma mansoni Pip-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
0.00008
-
 pH 6.8, 25°C Schistosoma mansoni Pip-Ala-Ala-azaAsn-CH=CH-COOEt
0.00008
-
 pH 6.8, 25°C Schistosoma mansoni Pip-Ala-Ala-azaAsn-CH=CH-CON(Bzl)2
0.00008
-
 pH 6.8, 25°C Schistosoma mansoni Boc-Piz-Ala-Ala-azaAsn-CH=CH-COOEt
0.00008
-
 pH 6.8, 25°C Schistosoma mansoni Boc-Piz-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
0.00009
-
 pH 6.8, 25°C Schistosoma mansoni Piz-Ala-Ala-azaAsn-CH=CH-CON(Bzl)2
0.00009
-
 pH 6.8, 25°C Schistosoma mansoni Mu-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
0.0001
-
 pH 6.8, 25°C Schistosoma mansoni Pip-Ala-Ala-azaAsn-CH=CH-CON(Bzl)-CH2-1-naphthyl
0.0001
-
 pH 6.8, 25°C Schistosoma mansoni Cbz-Ala-Val-azaAsn-CH=CH-COOEt
0.000101
-
 pH 6.8, 25°C Schistosoma mansoni Mu-Ala-Ala-azaAsn-CH=CH-COOEt
0.000103
-
 pH 6.8, 25°C Schistosoma mansoni Mu-Ala-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
0.000138
-
 pH 6.8, 25°C Schistosoma mansoni Cbz-Ala-Val-azaAsn-CH=CH-CO-tetrahydroquinoline
0.00015
-
 pH 6.8, 25°C Ixodes ricinus Pip-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
0.00015
-
 pH 6.8, 25°C Schistosoma mansoni Piz-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
0.00016
-
 pH 6.8, 25°C Schistosoma mansoni Pip-Ala-Ala-azaAsn-EP(S,S)-CONHCH2-1-naphthyl
0.00022
-
 pH 6.8, 25°C Schistosoma mansoni Pip-Ala-Ala-azaAsn-EP(S,S)-COOEt
0.00025
-
 pH 6.8, 25°C Schistosoma mansoni Piz-Ala-Ala-azaAsn-CH=CH-COOBzl
0.00027
-
 pH 6.8, 25°C Ixodes ricinus Boc-Piz-Ala-Ala-azaAsn-EP(S,S)-CON(Bzl)2
0.00028
-
 pH 6.8, 25°C Schistosoma mansoni Cbz-Ala-Ile-azaAsn-CH=CH-COOEt
0.0003
-
 pH 6.8, 25°C Schistosoma mansoni Piz-Ala-Ala-azaAsn-CH=CH-COOEt
0.00035
-
 pH 6.8, 25°C Ixodes ricinus Cbz-Ala-Val-azaAsn-CH=CH-CONHCH2-1-naphthyl
0.0004
-
 pH 6.8, 25°C Ixodes ricinus Pip-Ala-Ala-azaAsn-CH=CH-CONHCH2CH2Ph
0.0005
-
 pH 6.8, 25°C Ixodes ricinus Cbz-Ala-Val-azaAsn-CH=CH-CO-tetrahydroquinoline
0.0005
-
 pH 6.8, 25°C Ixodes ricinus CBZ-Ala-Phe-azaAsn-CH=CH-CO-tetrahydroisoquinoline
0.0006
-
 pH 6.8, 25°C Schistosoma mansoni Pip-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
0.0006
-
 pH 6.8, 25°C Ixodes ricinus Mu-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
0.00075
-
 pH 6.8, 25°C Schistosoma mansoni Mu-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
0.00075
-
 pH 6.8, 25°C Schistosoma mansoni Cbz-Piz-Ala-azaAsn-CH=CH-CO-tetrahydroquinoline
0.00075
-
 pH 6.8, 25°C Schistosoma mansoni Cbz-Piz-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
0.00075
-
 pH 6.8, 25°C Schistosoma mansoni Pip-Ala-Ala-azaAsn-CH=CH-CONHCH2CH2Ph
0.00075
-
 pH 6.8, 25°C Ixodes ricinus Boc-azaAsn-CH=CH-COOEt
0.0008
-
 pH 6.8, 25°C Ixodes ricinus Cbz-Piz-Ala-azaAsn-CH=CH-CO-tetrahydroisoquinoline
0.00085
-
 pH 6.8, 25°C Ixodes ricinus Cbz-Piz-Ala-azaAsn-CH=CH-CO-tetrahydroquinoline
0.00105
-
 pH 6.8, 25°C Schistosoma mansoni Cbz-Ala-Val-azaAsn-CH=CH-CONHCH2-1-naphthyl
0.00145
-
 pH 6.8, 25°C Schistosoma mansoni Mu-Ala-Ala-azaAsn-CH=CH-CONHCH2CH2CH2Ph
0.0018
-
 pH 6.8, 25°C Ixodes ricinus CBZ-Ala-Phe-azaAsn-CH=CH-CONHCH2-furyl