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Literature summary for 3.4.11.20 extracted from

  • Harbut, M.B.; Velmourougane, G.; Dalal, S.; Reiss, G.; Whisstock, J.C.; Onder, O.; Brisson, D.; McGowan, S.; Klemba, M.; Greenbaum, D.C.
    Bestatin-based chemical biology strategy reveals distinct roles for malaria M1- and M17-family aminopeptidases (2011), Proc. Natl. Acad. Sci. USA, 108, E526-E534.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.11.20

Cloned(Commentary)

Cloned (Comment) Organism
amino acid residue 192-1085 expressed in Escherichia coli Plasmodium falciparum
His-tagged protein (amino acid residue 79-605) expressed in Escherichia coli Plasmodium falciparum

Crystallization (Commentary)

Crystallization (Comment) Organism
-
 Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
(2S,17S,20S,21R)-21-amino-5-(4-benzoylbenzyl)-2-[4-(hex-5-ynoylamino)butyl]-20-hydroxy-17-(naphthalen-2-ylmethyl)-4,7,16,19-tetraoxo-22-phenyl-9,12-dioxa-3,6,15,18-tetraazadocosan-1-amide
-
 Plasmodium falciparum
N-[(2-[2-[(N-[(2S,3R)-3-amino-4-[4-(benzyloxy)phenyl]-2-hydroxybutanoyl]-L-alanyl)amino]ethoxy]ethoxy)acetyl]-4-benzoylphenylalanyl-N6-hex-5-ynoyl-L-lysinamide
-
 Plasmodium falciparum

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
343000
-
 gel filtration Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-
Plasmodium falciparum Q8IL11
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Plasmodium falciparum

Substrates and Products (Substrate)

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

Subunits

Subunits Comment Organism
homohexamer 343000, gel filtration (357000 calculated) Plasmodium falciparum

Synonyms

Synonyms Comment Organism
aminopeptidase N
-
 Plasmodium falciparum
Leucyl aminopeptidase
-
 Plasmodium falciparum
metallo-aminopeptidase M1
-
 Plasmodium falciparum
Pf-LAP
-
 Plasmodium falciparum
PfA-M1
-
 Plasmodium falciparum

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000029
-
 (2S,17S,20S,21R)-21-amino-5-(4-benzoylbenzyl)-2-[4-(hex-5-ynoylamino)butyl]-20-hydroxy-17-(naphthalen-2-ylmethyl)-4,7,16,19-tetraoxo-22-phenyl-9,12-dioxa-3,6,15,18-tetraazadocosan-1-amide pH 7.5, temperature not specified in the publication Plasmodium falciparum
0.00026
-
 N-[(2-[2-[(N-[(2S,3R)-3-amino-4-[4-(benzyloxy)phenyl]-2-hydroxybutanoyl]-L-alanyl)amino]ethoxy]ethoxy)acetyl]-4-benzoylphenylalanyl-N6-hex-5-ynoyl-L-lysinamide pH 7.5, temperature not specified in the publication Plasmodium falciparum
0.00033
-
 (2S,17S,20S,21R)-21-amino-5-(4-benzoylbenzyl)-2-[4-(hex-5-ynoylamino)butyl]-20-hydroxy-17-(naphthalen-2-ylmethyl)-4,7,16,19-tetraoxo-22-phenyl-9,12-dioxa-3,6,15,18-tetraazadocosan-1-amide pH 7.5, temperature not specified in the publication Plasmodium falciparum
0.004
-
 N-[(2-[2-[(N-[(2S,3R)-3-amino-4-[4-(benzyloxy)phenyl]-2-hydroxybutanoyl]-L-alanyl)amino]ethoxy]ethoxy)acetyl]-4-benzoylphenylalanyl-N6-hex-5-ynoyl-L-lysinamide pH 7.5, temperature not specified in the publication Plasmodium falciparum

General Information

General Information Comment Organism
malfunction inhibition caused swelling of the parasite digestive vacuole and prevented proteolysis of hemoglobin derived oligopeptides, likely starving the parasite resulting in death Plasmodium falciparum
malfunction inhibition is lethal to parasites early in the life cycle, prior to the onset of hemoglobin degradation Plasmodium falciparum