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Literature summary extracted from

  • Velmourougane, G.; Harbut, M.B.; Dalal, S.; McGowan, S.; Oellig, C.A.; Meinhardt, N.; Whisstock, J.C.; Klemba, M.; Greenbaum, D.C.
    Synthesis of new (-)-bestatin-based inhibitor libraries reveals a novel binding mode in the S1 pocket of the essential malaria M1 metalloaminopeptidase (2011), J. Med. Chem., 54, 1655-1666.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.11.20 expressed in Escherichia coli Plasmodium falciparum

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.4.11.20
-
 Plasmodium falciparum

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.11.20 bestatin
-
 Plasmodium falciparum
3.4.11.20 N-[(2S,3R)-3-amino-2-hydroxy-4-(4-methoxyphenyl)butanoyl]-L-leucine
-
 Plasmodium falciparum
3.4.11.20 N-[(2S,3R)-3-amino-2-hydroxy-4-(naphthalen-2-yl)butanoyl]-L-leucine
-
 Plasmodium falciparum
3.4.11.20 N-[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-norleucine
-
 Plasmodium falciparum
3.4.11.20 N-[(2S,3R)-3-amino-2-hydroxyheptanoyl]-L-leucine
-
 Plasmodium falciparum
3.4.11.20 N-[(2S,3R)-3-amino-4-[4-(benzyloxy)phenyl]-2-hydroxybutanoyl]-L-leucine
-
 Plasmodium falciparum
3.4.11.20 N2-[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-N6-[(benzyloxy)carbonyl]-L-lysine
-
 Plasmodium falciparum

Organism

EC Number Organism UniProt Comment Textmining
3.4.11.20 Plasmodium falciparum
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.11.20
-
 Plasmodium falciparum

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.11.20 L-leucyl-7-amido-4-methylcoumarin + H2O
-
 Plasmodium falciparum L-leucine + 7-amino-4-methylcoumarin
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.11.20 M1 metalloaminopeptidase
-
 Plasmodium falciparum
3.4.11.20 malaria M1 metalloaminopeptidase
-
 Plasmodium falciparum

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.11.20 0.000043
-
 N-[(2S,3R)-3-amino-2-hydroxy-4-(4-methoxyphenyl)butanoyl]-L-leucine pH 7.5, temperature not specified in the publication Plasmodium falciparum
3.4.11.20 0.00019
-
 bestatin pH 7.5, temperature not specified in the publication Plasmodium falciparum
3.4.11.20 0.00049
-
 N-[(2S,3R)-3-amino-4-[4-(benzyloxy)phenyl]-2-hydroxybutanoyl]-L-leucine pH 7.5, temperature not specified in the publication Plasmodium falciparum
3.4.11.20 0.0009
-
 N-[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-norleucine pH 7.5, temperature not specified in the publication Plasmodium falciparum
3.4.11.20 0.00145
-
 N2-[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-N6-[(benzyloxy)carbonyl]-L-lysine pH 7.5, temperature not specified in the publication Plasmodium falciparum
3.4.11.20 0.003
-
 N-[(2S,3R)-3-amino-2-hydroxy-4-(naphthalen-2-yl)butanoyl]-L-leucine pH 7.5, temperature not specified in the publication Plasmodium falciparum
3.4.11.20 0.0053
-
 N-[(2S,3R)-3-amino-2-hydroxyheptanoyl]-L-leucine pH 7.5, temperature not specified in the publication Plasmodium falciparum