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Literature summary for 3.4.22.B69 extracted from

  • Rizzi, L.; Sundararaman, S.; Cendic, K.; Vaiana, N.; Korde, R.; Sinha, D.; Mohmmed, A.; Malhotra, P.; Romeo, S.
    Design and synthesis of protein-protein interaction mimics as Plasmodium falciparum cysteine protease, falcipain-2 inhibitors (2011), Eur. J. Med. Chem., 46, 2083-2090.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
chicken egg white cystatin
-
Plasmodium falciparum
E-64
-
Plasmodium falciparum
leupeptide
-
Plasmodium falciparum
RLLGAP-(cis-4-aminocyclohexane carboxylic acid)-QLVSGI
-
Plasmodium falciparum
RLLGAP-(cis-4-aminocyclohexane carboxylic acid)-QLVSGI-betaAla-betaAla-PW
-
Plasmodium falciparum
RLLGAP-gamma-aminobutyric acid-QLVSGI
-
Plasmodium falciparum
RLLGAP-gamma-aminobutyric acid-QLVSGI-betaAla-betaAla-PW
-
Plasmodium falciparum
RLLGAPV-(cis-4-aminocyclohexane carboxylic acid)-RQLVSGI 63% inhibition at 0.005 mM Plasmodium falciparum
RLLGAPV-(cis-4-aminocyclohexane carboxylic acid)-RQLVSGI-betaAla-betaAla-PW
-
Plasmodium falciparum
RLLGAPV-gamma-aminobutyric acid-RQLVSGI 57% inhibition at 0.005 mM Plasmodium falciparum
RLLGAPV-gamma-aminobutyric acid-RQLVSGI-betaAla-betaAla-PW
-
Plasmodium falciparum

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
Hemoglobin + H2O Plasmodium falciparum
-
?
-
?

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni-NTA column chromatography Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Hemoglobin + H2O
-
Plasmodium falciparum ?
-
?
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
Plasmodium falciparum Z-Phe-Arg + 7-amino-4-methylcoumarin
-
?

Synonyms

Synonyms Comment Organism
FP-2
-
Plasmodium falciparum

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000065
-
chicken egg white cystatin in 100 mM NaOAc, 10 mM dithiothreitol, at 22°C, pH not specified in the publication Plasmodium falciparum
0.002
-
RLLGAPV-(cis-4-aminocyclohexane carboxylic acid)-RQLVSGI in 100 mM NaOAc, 10 mM dithiothreitol, at 22°C, pH not specified in the publication Plasmodium falciparum
0.0025
-
RLLGAPV-gamma-aminobutyric acid-RQLVSGI in 100 mM NaOAc, 10 mM dithiothreitol, at 22°C, pH not specified in the publication Plasmodium falciparum
0.0025
-
RLLGAPV-(cis-4-aminocyclohexane carboxylic acid)-RQLVSGI-betaAla-betaAla-PW in 100 mM NaOAc, 10 mM dithiothreitol, at 22°C, pH not specified in the publication Plasmodium falciparum