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Literature summary for 3.4.23.39 extracted from

  • Gupta, D.; Yedidi, R.S.; Varghese, S.; Kovari, L.C.; Woster, P.M.
    Mechanism-based inhibitors of the aspartyl protease plasmepsin II as potential antimalarial agents (2010), J. Med. Chem., 53, 4234-4247.
    View publication on PubMed
Search for more literature for 3.4.23.39

Cloned(Commentary)

Cloned (Comment) Organism
recombinantly expressed in Escherichia coli Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
N-((S)-1-(((2S,3S)-3-hydroxy-5-oxo-5-(((S)-1-oxo-3-phenyl-1-(prop-2-yn-1-ylamino)propan-2-yl)amino)-1-phenylpentan-2-yl)-amino)-3-methyl-1-oxobutan-2-yl)picolinamide
-
 Plasmodium falciparum
N-((S)-1-(((2S,3S)-5-(((R)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-3-chloro-1-oxopropan-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)-picolinamide
-
 Plasmodium falciparum
N-((S)-1-(((2S,3S)-5-(((S)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-1-oxopent-4-yn-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)-picolinamide
-
 Plasmodium falciparum
N-((S)-1-(((2S,3S)-5-(((S)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-3-cyano-1-oxopropan-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)picolinamide
-
 Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Purification (Commentary)

Purification (Comment) Organism
protein is autoactivated at pH 4.7 Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
EDANS-CO-CH2-CH2-COALERMFLSFP-diaminopimelate-(DABCYL)OH + H2O
-
 Plasmodium falciparum ?
-
 ?

Synonyms

Synonyms Comment Organism
plasmepsin II
-
 Plasmodium falciparum
PLm II
-
 Plasmodium falciparum

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Plasmodium falciparum

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
5
-
 assay at Plasmodium falciparum

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000035
-
 N-((S)-1-(((2S,3S)-5-(((R)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-3-chloro-1-oxopropan-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)-picolinamide pH 5.0, 37°C Plasmodium falciparum
0.000333
-
 N-((S)-1-(((2S,3S)-5-(((S)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-3-cyano-1-oxopropan-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)picolinamide pH 5.0, 37°C Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000022
-
 pH 5.0, 37°C Plasmodium falciparum N-((S)-1-(((2S,3S)-3-hydroxy-5-oxo-5-(((S)-1-oxo-3-phenyl-1-(prop-2-yn-1-ylamino)propan-2-yl)amino)-1-phenylpentan-2-yl)-amino)-3-methyl-1-oxobutan-2-yl)picolinamide
0.000028
-
 pH 5.0, 37°C Plasmodium falciparum N-((S)-1-(((2S,3S)-5-(((R)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-3-chloro-1-oxopropan-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)-picolinamide
0.000141
-
 pH 5.0, 37°C Plasmodium falciparum N-((S)-1-(((2S,3S)-5-(((S)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-1-oxopent-4-yn-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)-picolinamide
0.000333
-
 pH 5.0, 37°C Plasmodium falciparum N-((S)-1-(((2S,3S)-5-(((S)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-3-cyano-1-oxopropan-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)picolinamide