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Literature summary for 3.4.14.1 extracted from

  • Deu, E.; Leyva, M.; Albrow, V.; Rice, M.; Ellman, J.; Bogyo, M.
    Functional studies of plasmodium falciparum dipeptidyl aminopeptidase i using small molecule inhibitors and active site probes (2010), Chem. Biol., 17, 808-819.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.14.1

Inhibitors

Inhibitors Comment Organism Structure
3-[4-(1-amino-1-cyclopentylethyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
 Plasmodium falciparum
3-[4-(1-amino-2-phenylethyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
 Plasmodium falciparum
3-[4-(1-aminocyclohexyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
 Plasmodium falciparum
3-[4-(1-aminocyclohexyl)-1H-1,2,3-triazol-1-yl]-2-oxoheptyl 2,6-dimethylbenzoate
-
 Plasmodium falciparum
3-[4-(1-aminoethyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
 Plasmodium falciparum
3-[4-(2-aminopentan-2-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
 Plasmodium falciparum
3-[4-(2-aminopropan-2-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
 Plasmodium falciparum
3-[4-(2-methylpyrrolidin-2-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
 Plasmodium falciparum
3-[4-(3-aminopentan-3-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
 Plasmodium falciparum
3-[4-(4-aminoheptan-4-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
 Plasmodium falciparum
3-[4-[(1R)-1-amino-1-cyclopentylethyl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
 Plasmodium falciparum
3-[4-[(1S)-1-amino-1-cyclohexylethyl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
 Plasmodium falciparum
3-[4-[(1S)-1-amino-1-cyclopentylethyl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
 Plasmodium falciparum
3-[4-[4-(methylamino)heptan-4-yl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
-
 Plasmodium falciparum
Ala-4(I)Phe-diazomethyl ketone irreversible inhibitor Plasmodium falciparum
SAK2 peptide vinyl sulfone, covalent inhibitor Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(Pro-Arg)2-Rho + 2 H2O
-
 Plasmodium falciparum rhodamine + 2 Pro-Arg
-
 ?

Synonyms

Synonyms Comment Organism
dipeptidyl aminopeptidase I
-
 Plasmodium falciparum
DPAP1
-
 Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000019
-
 determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C Plasmodium falciparum 3-[4-[(1R)-1-amino-1-cyclopentylethyl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
0.000186
-
 determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C Plasmodium falciparum 3-[4-(1-amino-1-cyclopentylethyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
0.00041
-
 determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C Plasmodium falciparum 3-[4-(3-aminopentan-3-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
0.00041
-
 determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C Plasmodium falciparum 3-[4-(2-aminopentan-2-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
0.00042
-
 determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C Plasmodium falciparum 3-[4-(2-methylpyrrolidin-2-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
0.00056
-
 determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C Plasmodium falciparum 3-[4-(1-aminocyclohexyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
0.0007
-
 determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C Plasmodium falciparum 3-[4-(1-aminoethyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
0.0007
-
 determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C Plasmodium falciparum 3-[4-[(1S)-1-amino-1-cyclohexylethyl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
0.0007
-
 determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C Plasmodium falciparum 3-[4-(4-aminoheptan-4-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
0.0011
-
 determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C Plasmodium falciparum 3-[4-(2-aminopropan-2-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
0.0077
-
 determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C Plasmodium falciparum 3-[4-[4-(methylamino)heptan-4-yl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
0.011
-
 determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C Plasmodium falciparum 3-[4-(1-aminocyclohexyl)-1H-1,2,3-triazol-1-yl]-2-oxoheptyl 2,6-dimethylbenzoate
0.014
-
 determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C Plasmodium falciparum 3-[4-[(1S)-1-amino-1-cyclopentylethyl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
0.074
-
 determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C Plasmodium falciparum 3-[4-(1-amino-2-phenylethyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one

General Information

General Information Comment Organism
physiological function inhibition results in the formation of an immature trophozoite that leads to parasite death Plasmodium falciparum