Information on EC 3.4.23.B14 - plasmepsin IV

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The expected taxonomic range for this enzyme is: Plasmodium

EC NUMBER
COMMENTARY hide
3.4.23.B14
preliminary BRENDA-supplied EC number
RECOMMENDED NAME
GeneOntology No.
plasmepsin IV
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REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
cleavage of hemoglobin. In the S3 and S2 subsites, the plasmepsin 4 orthologs all prefer hydrophobic amino acid residues, Phe or Ile, but reject charged residues such as Lys or Asp. In S2' and S3' subsites these plasmepsins tolerate both hydrophobic and hydrophilic residues
show the reaction diagram
cleavage of hemoglobin. In the S3 and S2 subsites, the plasmepsin 4 orthologs all prefer hydrophobic amino acid residues, Phe or Ile, but reject charged residues such as Lys or Asp. In S2' and S3' subsites these plasmepsins tolerate both hydrophobic and hydrophilic residues.
show the reaction diagram
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
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CAS REGISTRY NUMBER
COMMENTARY hide
429673-77-8
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
rodent malaria parasite, wild-type line1037cl1 gene pm4
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Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
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PM4 deficiency results in significantly less virulence than that for the parental parasite. Enzyme-deficient parasites fail to induce experimental cerebral malaria in susceptible mice, and resistant mice are able to clear infections
physiological function
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
denatured human hemoglobin + H2O
?
show the reaction diagram
preferred over native human hemoglobin. PvPM4 acts synergistically with cysteine proteases vivapain-2 and vivapain-3 in the hydrolysis of hemoglobin
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?
haemoglobin + H2O
?
show the reaction diagram
Hemoglobin + H2O
?
show the reaction diagram
KEFAFF(NO2)ALK + H2O
KEFAF + F(NO2)ALK
show the reaction diagram
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-
?
KEFNFF(NO2)ALK + H2O
KEFNF + F(NO2)ALK
show the reaction diagram
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-
-
?
KEFVFF(NO2)ALK + H2O
KEFVF + F(NO2)ALK
show the reaction diagram
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-
?
KPAEFF(NO2)RL + H2O
KPAEF + F(NO2)RL
show the reaction diagram
KPDEFF(NO2)RL + H2O
KPDEF + F(NO2)RL
show the reaction diagram
KPFEFF(NO2)RL + H2O
KPFEF + F(NO2)RL
show the reaction diagram
KPIAFF(NO2)RL + H2O
KPIAF + F(NO2)RL
show the reaction diagram
KPIDFF(NO2)RL + H2O
KPIDF + F(NO2)RL
show the reaction diagram
KPIEFF(NO2)AL + H2O
KPIEF + F(NO2)AL
show the reaction diagram
KPIEFF(NO2)EL + H2O
KPIEF + F(NO2)EL
show the reaction diagram
KPIEFF(NO2)KL + H2O
KPIEF + F(NO2)KL
show the reaction diagram
KPIEFF(NO2)RD + H2O
KPIEF + F(NO2)RD
show the reaction diagram
KPIEFF(NO2)RI + H2O
KPIEF + F(NO2)RI
show the reaction diagram
KPIEFF(NO2)RL + H2O
KPIEF + F(NO2)RL
show the reaction diagram
KPIEFF(NO2)RR + H2O
KPIEF + F(NO2)RR
show the reaction diagram
KPIEFF(NO2)RS + H2O
KPIEF + F(NO2)RS
show the reaction diagram
KPIEFF(NO2)RV + H2O
KPIEF + F(NO2)RV
show the reaction diagram
KPIEFF(NO2)SL + H2O
KPIEF + F(NO2)SL
show the reaction diagram
KPIEFF(NO2)VL + H2O
KPIEF + F(NO2)VL
show the reaction diagram
KPIEFZRL + H2O
KPIEF + ZRL
show the reaction diagram
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-
-
?
KPIKFF(NO2)RL + H2O
KPIKF + F(NO2)RL
show the reaction diagram
KPILFF(NO2)RL + H2O
KPILEF + F(NO2)RL
show the reaction diagram
KPKEFF(NO2)RL + H2O
KPKEF + F(NO2)RL
show the reaction diagram
KPSEFF(NO2)RL + H2O
KPSEF + F(NO2)RL
show the reaction diagram
Lys-Pro-Ile-Nle-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Nle-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
native human gemoglobin + H2O
?
show the reaction diagram
poor substrate
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?
spectrin + H2O
?
show the reaction diagram
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?
additional information
?
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NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
haemoglobin + H2O
?
show the reaction diagram
Q8IM16
human haemoglobin. The enzyme may play a crucial role in the critical process which yields nutrients from parasite growth, the enzyme may have the potential to initiate the vacuolar haemoglobin digestion pathway
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?
additional information
?
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INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1R,2R,3R,4R)-1,4-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-1,4-bis[5-(4-tert-butylphenyl)-1,3,4-oxadiazol-2-yl]butane-2,3-diol
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(2R,3R,4R)-2-benzyloxy-3,4-dihydroxy-N-[(1S,2R)-2-hydroxyindan-1-yl]-4-[(2R)-3-oxo-1-oxa-4-aza-cyclotridec-2-yl]butyramide
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(2R,3R,4R)-2-benzyloxy-3,4-dihydroxy-N-[(1S,2R)-2-hydroxyindan-1-yl]-4-[(2R,11E)-3-oxo-1-oxa-4-aza-cyclo-tridec-11-en-2-yl]butyramide
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(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(1,3-benzodioxol-5-yl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
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(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5-(5-methyl-1,3,4-oxadiazol-2-yl)pentanamide
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(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5-[5-(2-phenylethyl)-1,3,4-oxadiazol-2-yl]pentanamide
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(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
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(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-5-[5-(4-tert-butylphenyl)-1,3,4-oxadiazol-2-yl]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]pentanamide
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(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-6-[2-[(4-tert-butylphenyl)carbonyl]hydrazino]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxohexanamide
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(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-N'1,N'6-bis[(4-tert-butylphenyl)carbonyl]-3,4-dihydroxyhexanedihydrazide
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(2R,3R,4R,5R)-5-(5-benzyl-1,3,4-oxadiazol-2-yl)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]pentanamide
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(2R,3R,4R,5R)-5-benzyloxy-3,4-dihydroxy-6-oxo-1-oxa-7-aza-cyclohexadec-2-carboxylic acid [(1S,2R)-2-hydroxyindan-1-yl]-amide
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(2R,3R,4R,5R,14E)-5-benzyloxy-3,4-dihydroxy-6-oxo-1-oxa-7-aza-cyclohexadec-14-ene-2-carboxylic acid [(1S,2R)-2-hydroxyindan-1-yl]-amide
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(2S,5S,14S,17S,18S)-N-(2-amino-2-oxoethyl)-17-benzyl-18-hydroxy-14-[[N-(3-methylbutanoyl)-L-valyl]amino]-2-(1-methylethyl)-3,8,15,20-tetraoxo-1,4,9,16-tetraazacycloicosane-5-carboxamide
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(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-([N-[(naphthalen-2-yloxy)acetyl]isoleucyl]amino)heptanamide
(3S,4S)-pyrrolidine-3,4-diyl bis(3,3-dimethylbutanoate)
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(3S,4S)-pyrrolidine-3,4-diyl bis(3-methylbutanoate)
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(3S,4S)-pyrrolidine-3,4-diyl bis(naphthalen-1-ylacetate)
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(3S,4S)-pyrrolidine-3,4-diyl bis(naphthalen-2-ylacetate)
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(3S,4S)-pyrrolidine-3,4-diyl bis(phenylacetate)
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(3S,4S)-pyrrolidine-3,4-diyl dibenzoate
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(3S,4S)-pyrrolidine-3,4-diyl dicyclohexanecarboxylate
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(4R)-3-[(2S,3S)-2-hydroxy-3-[[(3-hydroxy-2-methylphenyl)carbonyl]amino]-4-phenylbutanoyl]-5,5-dimethyl-N-(2-methylbenzyl)-1,3-thiazolidine-4-carboxamide
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(4R)-3-[(2S,3S)-3-[[(2,6-dimethylphenoxy)acetyl]amino]-2-hydroxy-4-phenylbutanoyl]-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
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(4R)-N-tert-butyl-3-[(2S,3S)-2-hydroxy-3-([N-[(isoquinolin-5-yloxy)acetyl]-S-methyl-L-cysteinyl]amino)-4-phenylbutanoyl]-1,3-thiazolidine-4-carboxamide
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(4R)-N-tert-butyl-3-[(2S,3S)-2-hydroxy-3-[[(3-hydroxy-2-methylphenyl)carbonyl]amino]-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
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(5-[[(1H-indol-3-ylacetyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-aminobenzoate
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(5-[[(1H-indol-3-ylacetyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-nitrobenzoate
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(5-[[(phenylcarbonyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-aminobenzoate
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(5-[[(phenylcarbonyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-nitrobenzoate
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(6-[[(phenylcarbonyl)oxy]methyl]-2,5,6,7-tetrahydro-1H-azepin-4-yl)methyl 4-aminobenzoate
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(6-[[(phenylcarbonyl)oxy]methyl]-2,5,6,7-tetrahydro-1H-azepin-4-yl)methyl 4-nitrobenzoate
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(6S,9S,12R,13S,17S,20R,21S)-13,21-dihydroxy-2,17-dimethyl-6,9-bis(1-methylethyl)-4,7,10,15,18-pentaoxo-12,20-bis(trifluoromethyl)-5,8,11,16,19-pentaazatricosan-23-oic acid
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2,3,4,7-tetrahydro-1H-azepine-3,5-diyldimethanediyl bis(4-aminobenzoate)
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2,3,4,7-tetrahydro-1H-azepine-3,5-diyldimethanediyl bis(4-nitrobenzoate)
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2,3,4,7-tetrahydro-1H-azepine-3,5-diyldimethanediyl dibenzoate
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4-(1-benzofuran-2-yl)-Na-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
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acetyl-Val-Val-Sta-Ala-Sta
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isobutyl-Val-Val-Sta-Ala-Sta
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Iva-Val-Val-Sta-Ala-Sta
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KNI-727
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IC50: 0.00074 mM
L-lysyl-L-prolyl-L-norleucyl-N-[(1S)-1-([[(1S)-1-[[(1S)-4-amino-1-[[(1R)-1-carboxy-2-methylbutyl]carbamoyl]pent-4-en-1-yl]carbamoyl]-3-methylbutyl]amino]methyl)pentyl]-L-serinamide
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L-lysyl-L-prolyl-L-phenylalanyl-N-[(1S)-1-benzyl-2-[[(1S)-1-benzyl-2-[[(1S)-2-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-1-(hydroxymethyl)-2-oxoethyl]amino]-2-oxoethyl]amino]ethyl]-L-norleucinamide
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Lac-Val-Sta-Ala-Sta
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Lys-Pro-Ile-Glu-Phe-Phe-Ala-Leu
Lys-Pro-Ile-Ile-Phe-Phe-Arg-Leu
Lys-Pro-Ile-Nle-Phe-Phe-Arg-Leu
Lys-Pro-Phe-Nle-Phe-Phe-Ser-Arg
Lys-Pro-Phe-Nle-Phe-Phe-Ser-Ser
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
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N,N'-(3S,4S)-pyrrolidine-3,4-diylbis(N-benzyl-2-phenylacetamide)
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N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucine
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
N-acetyl-L-Leu-L-Leu-L-norleucinal
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N-acetyl-Leu-Leu-Met-CHO
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calpaicin inhibitor II
N-acetyl-Leu-Leu-norleucinal
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calpaicin inhibitor I
N-benzyl-2-bromo-N-[[4-([[2-(2,4-dichlorophenyl)ethyl](3-phenylpropyl)amino]methyl)pyrrolidin-3-yl]methyl]-4,5-dimethoxybenzamide
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N-benzyl-2-bromo-N-[[4-([[2-(2,4-dichlorophenyl)ethyl][2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]amino]methyl)pyrrolidin-3-yl]methyl]-4,5-dimethoxybenzamide
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N-[(1R)-1-[[(1S,2S)-4-[[(1S)-5-amino-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)pentyl]amino]-1-benzyl-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
N-[(1S,2S)-1-benzyl-3-[(4R)-4-(tert-butylcarbamoyl)-5,5-dimethyl-1,3-thiazolidin-3-yl]-2-hydroxy-3-oxopropyl]-N2-[(cyclohexa-1,3-dien-1-yloxy)acetyl]-L-valinamide
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N-[(1S,2S)-1-benzyl-3-[(4R)-4-(tert-butylcarbamoyl)-5,5-dimethyl-1,3-thiazolidin-3-yl]-2-hydroxy-3-oxopropyl]-N2-[(isoquinolin-5-yloxy)acetyl]-L-valinamide
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N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-([4-[4-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)phenoxy]phenyl]carbonyl)isoleucinamide
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-[[4-(4-[[(1R)-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)-3-methylbutyl]carbamoyl]phenoxy)phenyl]carbonyl]isoleucinamide
N-[(4-[2-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-2-oxoethyl]phenyl)acetyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-alanyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucine
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-alaninamide
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
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N-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-4-oxobutanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
N-[4-[([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)oxy]butanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
N1-[(1S,2S)-1-benzyl-3-[(4R)-4-(tert-butylcarbamoyl)-5,5-dimethyl-1,3-thiazolidin-3-yl]-2-hydroxy-3-oxopropyl]-N2-[(isoquinolin-5-yloxy)acetyl]-L-aspartamide
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Pepstatin
pepstatin A
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-L-lysinate
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N6-(tert-butoxycarbonyl)-L-lysinate
ritonavir
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IC50: 1800 nM
Ro 40-4388
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Ro40-5576
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saquinavir
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IC50: 375 nM
tert-butyl [(1S)-1-[[(3S,7S,10S,19S)-19-[(2-amino-2-oxoethyl)carbamoyl]-7-benzyl-6-hydroxy-3-(1-methylethyl)-2,9,16-trioxo-1,4,8,15-tetraazacyclononadecan-10-yl]carbamoyl]-2-methylpropyl]carbamate
[5-([[(4-bromophenyl)carbonyl]oxy]methyl)-2,3,4,7-tetrahydro-1H-azepin-3-yl]methyl 4-aminobenzoate
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[6-([[(4-aminophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl naphthalene-1-carboxylate
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[6-([[(4-nitrophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl 4-bromobenzoate
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[6-([[(4-nitrophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl naphthalene-1-carboxylate
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additional information
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KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.035
KEFAFF(NO2)ALK
-
pH 4.7, 37°C
0.02
KEFNFF(NO2)ALK
-
pH 4.7, 37°C
0.011
KEFVFF(NO2)ALK
-
pH 4.7, 37°C
0.017 - 0.05
KPAEFF(NO2)RL
0.029 - 0.063
KPDEFF(NO2)RL
0.009 - 0.014
KPFEFF(NO2)RL
0.005 - 0.012
KPIAFF(NO2)RL
0.01 - 0.023
KPIDFF(NO2)RL
0.0116 - 0.028
KPIEFF(NO2)AL
0.008 - 0.0518
KPIEFF(NO2)EL
0.017 - 0.025
KPIEFF(NO2)KL
0.0146 - 0.044
KPIEFF(NO2)RD
0.0165 - 0.034
KPIEFF(NO2)RI
0.0092 - 0.02
KPIEFF(NO2)RL
0.0037 - 0.0296
KPIEFF(NO2)RR
0.0054 - 0.043
KPIEFF(NO2)RS
0.021 - 0.046
KPIEFF(NO2)RV
0.017 - 0.043
KPIEFF(NO2)SL
0.0044 - 0.023
KPIEFF(NO2)VL
0.036
KPIEFZRL
-
pH 4.7, 37°C
0.0123 - 0.029
KPIKFF(NO2)RL
0.008 - 0.0166
KPILFF(NO2)RL
0.007 - 0.0429
KPKEFF(NO2)RL
0.012 - 0.041
KPSEFF(NO2)RL
0.007 - 0.016
Lys-Pro-Ile-Nle-Phe-Phe(NO2)-Arg-Leu
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
13
KEFAFF(NO2)ALK
Plasmodium falciparum
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pH 4.7, 37°C
20
KEFNFF(NO2)ALK
Plasmodium falciparum
-
pH 4.7, 37°C
6
KEFVFF(NO2)ALK
Plasmodium falciparum
-
pH 4.7, 37°C
3.4 - 35
KPAEFF(NO2)RL
1.2 - 12
KPDEFF(NO2)RL
5.1 - 31
KPFEFF(NO2)RL
5.2 - 20
KPIAFF(NO2)RL
3 - 29
KPIDFF(NO2)RL
8.7 - 37
KPIEFF(NO2)AL
5.4 - 42
KPIEFF(NO2)EL
5 - 14.7
KPIEFF(NO2)KL
14.6 - 29
KPIEFF(NO2)RD
10 - 20
KPIEFF(NO2)RI
6.1 - 50
KPIEFF(NO2)RL
3.7 - 26.1
KPIEFF(NO2)RR
5.4 - 22.7
KPIEFF(NO2)RS
3 - 11.9
KPIEFF(NO2)RV
2 - 20.8
KPIEFF(NO2)SL
0.9 - 13
KPIEFF(NO2)VL
5
KPIEFZRL
Plasmodium falciparum
-
pH 4.7, 37°C
1.9 - 5.4
KPIKFF(NO2)RL
6 - 20.5
KPILFF(NO2)RL
0.01 - 0.9
KPKEFF(NO2)RL
2.4 - 18.5
KPSEFF(NO2)RL
6 - 67
Lys-Pro-Ile-Nle-Phe-Phe(NO2)-Arg-Leu
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000035
(1R,2R,3R,4R)-1,4-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-1,4-bis[5-(4-tert-butylphenyl)-1,3,4-oxadiazol-2-yl]butane-2,3-diol
-
-
0.0002
(2R,3R,4R)-2-benzyloxy-3,4-dihydroxy-N-[(1S,2R)-2-hydroxyindan-1-yl]-4-[(2R)-3-oxo-1-oxa-4-aza-cyclotridec-2-yl]butyramide
-
-
0.0068
(2R,3R,4R)-2-benzyloxy-3,4-dihydroxy-N-[(1S,2R)-2-hydroxyindan-1-yl]-4-[(2R,11E)-3-oxo-1-oxa-4-aza-cyclo-tridec-11-en-2-yl]butyramide
-
-
0.000397
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(1,3-benzodioxol-5-yl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
0.01
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5-(5-methyl-1,3,4-oxadiazol-2-yl)pentanamide
-
-
0.012
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5-[5-(2-phenylethyl)-1,3,4-oxadiazol-2-yl]pentanamide
-
-
0.002
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
0.0012
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-5-[5-(4-tert-butylphenyl)-1,3,4-oxadiazol-2-yl]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]pentanamide
-
-
0.014
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-6-[2-[(4-tert-butylphenyl)carbonyl]hydrazino]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxohexanamide
-
-
0.000478
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-N'1,N'6-bis[(4-tert-butylphenyl)carbonyl]-3,4-dihydroxyhexanedihydrazide
-
-
0.002
(2R,3R,4R,5R)-5-(5-benzyl-1,3,4-oxadiazol-2-yl)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]pentanamide
-
-
0.0022
(2R,3R,4R,5R)-5-benzyloxy-3,4-dihydroxy-6-oxo-1-oxa-7-aza-cyclohexadec-2-carboxylic acid [(1S,2R)-2-hydroxyindan-1-yl]-amide
-
-
0.002
(2R,3R,4R,5R,14E)-5-benzyloxy-3,4-dihydroxy-6-oxo-1-oxa-7-aza-cyclohexadec-14-ene-2-carboxylic acid [(1S,2R)-2-hydroxyindan-1-yl]-amide
-
-
0.00000052
(2S,5S,14S,17S,18S)-N-(2-amino-2-oxoethyl)-17-benzyl-18-hydroxy-14-[[N-(3-methylbutanoyl)-L-valyl]amino]-2-(1-methylethyl)-3,8,15,20-tetraoxo-1,4,9,16-tetraazacycloicosane-5-carboxamide
-
-
0.000017 - 0.0013
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-([N-[(naphthalen-2-yloxy)acetyl]isoleucyl]amino)heptanamide
0.00011
(4R)-3-[(2S,3S)-2-hydroxy-3-[[(3-hydroxy-2-methylphenyl)carbonyl]amino]-4-phenylbutanoyl]-5,5-dimethyl-N-(2-methylbenzyl)-1,3-thiazolidine-4-carboxamide
-
-
0.000015
(4R)-3-[(2S,3S)-3-[[(2,6-dimethylphenoxy)acetyl]amino]-2-hydroxy-4-phenylbutanoyl]-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.00074
(4R)-N-tert-butyl-3-[(2S,3S)-2-hydroxy-3-([N-[(isoquinolin-5-yloxy)acetyl]-S-methyl-L-cysteinyl]amino)-4-phenylbutanoyl]-1,3-thiazolidine-4-carboxamide
-
-
0.003
(4R)-N-tert-butyl-3-[(2S,3S)-2-hydroxy-3-[[(3-hydroxy-2-methylphenyl)carbonyl]amino]-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.0159
(5-[[(1H-indol-3-ylacetyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-aminobenzoate
-
plasmepsin IV
0.0434
(5-[[(1H-indol-3-ylacetyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-nitrobenzoate
-
plasmepsin IV
0.0072
(5-[[(phenylcarbonyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-aminobenzoate
-
plasmepsin IV
0.0386
(5-[[(phenylcarbonyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-nitrobenzoate
-
plasmepsin IV
0.0099
(6-[[(phenylcarbonyl)oxy]methyl]-2,5,6,7-tetrahydro-1H-azepin-4-yl)methyl 4-aminobenzoate
-
plasmepsin IV
0.029
(6-[[(phenylcarbonyl)oxy]methyl]-2,5,6,7-tetrahydro-1H-azepin-4-yl)methyl 4-nitrobenzoate
-
plasmepsin IV
0.000023
(6S,9S,12R,13S,17S,20R,21S)-13,21-dihydroxy-2,17-dimethyl-6,9-bis(1-methylethyl)-4,7,10,15,18-pentaoxo-12,20-bis(trifluoromethyl)-5,8,11,16,19-pentaazatricosan-23-oic acid
-
-
0.0032
2,3,4,7-tetrahydro-1H-azepine-3,5-diyldimethanediyl bis(4-aminobenzoate)
-
plasmepsin IV
0.0221
2,3,4,7-tetrahydro-1H-azepine-3,5-diyldimethanediyl bis(4-nitrobenzoate)
-
plasmepsin IV
0.211
2,3,4,7-tetrahydro-1H-azepine-3,5-diyldimethanediyl dibenzoate
-
plasmepsin IV
0.000041
4-(1-benzofuran-2-yl)-Na-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
0.0000002
acetyl-Val-Val-Sta-Ala-Sta
-
pH 4.7
0.0000001
Iva-Val-Va-Sta-Ala-Sta
-
pH 4.7
0.000022
L-lysyl-L-prolyl-L-norleucyl-N-[(1S)-1-([[(1S)-1-[[(1S)-4-amino-1-[[(1R)-1-carboxy-2-methylbutyl]carbamoyl]pent-4-en-1-yl]carbamoyl]-3-methylbutyl]amino]methyl)pentyl]-L-serinamide
-
-
0.000000026
L-lysyl-L-prolyl-L-phenylalanyl-N-[(1S)-1-benzyl-2-[[(1S)-1-benzyl-2-[[(1S)-2-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-1-(hydroxymethyl)-2-oxoethyl]amino]-2-oxoethyl]amino]ethyl]-L-norleucinamide
-
-
0.000025
Lac-Val-Sta-Ala-Sta
-
pH 4.7
0.00000011 - 0.0000022
Lys-Pro-Ile-Glu-Phe-Phe-Ala-Leu
0.00000053 - 0.0000058
Lys-Pro-Ile-Ile-Phe-Phe-Arg-Leu
0.00000006 - 0.00000041
Lys-Pro-Ile-Nle-Phe-Phe-Arg-Leu
0.00000014 - 0.0000006
Lys-Pro-Phe-Nle-Phe-Phe-Ser-Arg
0.000000026 - 0.00000071
Lys-Pro-Phe-Nle-Phe-Phe-Ser-Ser
0.00005
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
pH 4.7
0.0000014 - 0.00026
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucine
0.0000006 - 0.000021
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
0.000002 - 0.00003
N-[(1R)-1-[[(1S,2S)-4-[[(1S)-5-amino-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)pentyl]amino]-1-benzyl-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
0.00016
N-[(1S,2S)-1-benzyl-3-[(4R)-4-(tert-butylcarbamoyl)-5,5-dimethyl-1,3-thiazolidin-3-yl]-2-hydroxy-3-oxopropyl]-N2-[(cyclohexa-1,3-dien-1-yloxy)acetyl]-L-valinamide
-
-
0.000025 - 0.003
N-[(1S,2S)-1-benzyl-3-[(4R)-4-(tert-butylcarbamoyl)-5,5-dimethyl-1,3-thiazolidin-3-yl]-2-hydroxy-3-oxopropyl]-N2-[(isoquinolin-5-yloxy)acetyl]-L-valinamide
0.0000007 - 0.000058
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-([4-[4-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)phenoxy]phenyl]carbonyl)isoleucinamide
0.0000003 - 0.00025
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-[[4-(4-[[(1R)-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)-3-methylbutyl]carbamoyl]phenoxy)phenyl]carbonyl]isoleucinamide
0.0000005 - 0.000038
N-[(4-[2-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-2-oxoethyl]phenyl)acetyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
0.00000009 - 0.000017
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-alanyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
0.0000045 - 0.000044
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucine
0.00000024 - 0.0000025
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-alaninamide
0.0000005 - 0.00001
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
0.000707
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
-
0.0000021 - 0.00016
N-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-4-oxobutanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
0.00000014 - 0.000006
N-[4-[([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)oxy]butanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
0.0071
N1-[(1S,2S)-1-benzyl-3-[(4R)-4-(tert-butylcarbamoyl)-5,5-dimethyl-1,3-thiazolidin-3-yl]-2-hydroxy-3-oxopropyl]-N2-[(isoquinolin-5-yloxy)acetyl]-L-aspartamide
-
-
0.000000015 - 0.0000023
pepstatin A
0.0000015 - 0.000087
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-L-lysinate
0.0000014 - 0.000019
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N6-(tert-butoxycarbonyl)-L-lysinate
0.00001
Ro 40-4388
-
-
0.00001
Ro40-4388
-
pH 4.7
0.000015
Ro40-5576
-
pH 4.7
-
0.00000029 - 0.00052
tert-butyl [(1S)-1-[[(3S,7S,10S,19S)-19-[(2-amino-2-oxoethyl)carbamoyl]-7-benzyl-6-hydroxy-3-(1-methylethyl)-2,9,16-trioxo-1,4,8,15-tetraazacyclononadecan-10-yl]carbamoyl]-2-methylpropyl]carbamate
0.0057
[5-([[(4-bromophenyl)carbonyl]oxy]methyl)-2,3,4,7-tetrahydro-1H-azepin-3-yl]methyl 4-aminobenzoate
-
plasmepsin IV
0.0015
[6-([[(4-aminophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl naphthalene-1-carboxylate
-
plasmepsin IV
0.0688
[6-([[(4-nitrophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl 4-bromobenzoate
-
plasmepsin IV
0.0039
[6-([[(4-nitrophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl naphthalene-1-carboxylate
-
plasmepsin IV
additional information
additional information
-
the Ki-value for isobutyl-Val-Val-Sta-Ala-Sta is below 0.1 nM
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0412
(3S,4S)-pyrrolidine-3,4-diyl bis(3,3-dimethylbutanoate)
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.168
(3S,4S)-pyrrolidine-3,4-diyl bis(3-methylbutanoate)
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.00009
(3S,4S)-pyrrolidine-3,4-diyl bis(naphthalen-1-ylacetate)
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.0008
(3S,4S)-pyrrolidine-3,4-diyl bis(naphthalen-2-ylacetate)
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.0074
(3S,4S)-pyrrolidine-3,4-diyl bis(phenylacetate)
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.0538
(3S,4S)-pyrrolidine-3,4-diyl dibenzoate
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.134
(3S,4S)-pyrrolidine-3,4-diyl dicyclohexanecarboxylate
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.00074
KNI-727
Plasmodium falciparum
-
IC50: 0.00074 mM
0.0015
N,N'-(3S,4S)-pyrrolidine-3,4-diylbis(N-benzyl-2-phenylacetamide)
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.00035
N-benzyl-2-bromo-N-[[4-([[2-(2,4-dichlorophenyl)ethyl](3-phenylpropyl)amino]methyl)pyrrolidin-3-yl]methyl]-4,5-dimethoxybenzamide
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.00018
N-benzyl-2-bromo-N-[[4-([[2-(2,4-dichlorophenyl)ethyl][2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]amino]methyl)pyrrolidin-3-yl]methyl]-4,5-dimethoxybenzamide
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.000001
Pepstatin
Plasmodium falciparum
-
IC50: about 1 nM
0.0018
ritonavir
Plasmodium falciparum
-
IC50: 1800 nM
0.000375
saquinavir
Plasmodium falciparum
-
IC50: 375 nM
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
3.5 - 5.5
broad
4.5
-
assay at
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
PSM4 is inactive at pH 2.2
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
TEMPERATURE RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
PSM4 is inactive at 0 °C
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
a fertilized zygote capable of moving spontaneously, the enzyme is located at the apical surface
Manually annotated by BRENDA team
additional information
-
presence of PgPM4 in the different life cycle stages, e.g. in asexual blood stage, overview
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
of asexual stage malaria parasites
-
Manually annotated by BRENDA team
-
ookinete-secreted plasmepsin 4
-
Manually annotated by BRENDA team
additional information
-
co-localization of PgPM4 with chitinase, PgCHT2
-
Manually annotated by BRENDA team
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37000
x * 44000, SDs-PAGE of preprotein, x * 37000, SDS-PAGE of mature protein
44000
x * 44000, SDs-PAGE of preprotein, x * 37000, SDS-PAGE of mature protein
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
x * 44000, SDs-PAGE of preprotein, x * 37000, SDS-PAGE of mature protein
additional information
-
PSM4 is unusable for structural studies by hydrogen/deuterium exchange coupled to mass spectrometry, DXMS, since the method requires the use of proteases working at acidic pH and low temperatures
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
proteolytic modification
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
hanging-drop vapor-diffusion method, crystals of PmPM4 in complex with the small-molecule inhibitor AG1776. The crystals are orthorhombic, with space group P2(1)2(1)2 and unit-cell parameters a = 95.88 A, b = 112.58 A, c = 90.40 A, two molecules per asymmetric unit
-
hanging-drop vapor-diffusion method, crystal structure of plasmepsin 4 bound to the allophenylnorstatine-based compound KNI-764 at 3.3 A resolution. The PmPM4–inhibitor complex crystallized in the ortho-rhombic space group P2(1)2(1)2, with unit-cell parameters a = 95.9 A, b = 112.6 A, c = 90.4 A, with two molecules in the asymmetric unit
-
pKa calculations for PM IV complexed with the inhibitor KNI-764. Residue Asp214 is protonated, while residue Asp34 is deprotonated. In the colmplex, the hydroxyl group interacts with the OD2 oxygen atom of Asp34 through a hydrogen bond. The hydroxyl group also presents a hydrogen bond interaction with acid aspartic protonated Asp214. The amino groups of Gly78 and Ser79 residues interact with KNI-764 forming hydrogen bonds at 2.02 and 2.20 A. The hydroxyl group of Thr217 forms hydrogen bonds with the inhibitor at 2.06 A
analysis of 3D model of PM4 shows a typical aspartic protease structure with bi-lobed, compact and distinct peptide binding cleft
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37
highly stable under acidic and neutral conditions
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
expression in Escherichia coli
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
construction of 1092cl4 and 1092cl6, two parasite lines deficient in expressing PM4, by gene disruption, and of mutant lines 688cl2 and 688cl3. PM4 deficiency results in significantly less virulence than that for the parental parasite. Enzyme-deficient parasites fail to induce experimental cerebral malaria in susceptible mice, and resistant mice are able to clear infections. The mutant acts as vaccine, immunity through antibody-mediated parasite clearance in the spleen, virulence-attenuated phenotypes, overview
Renatured/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
bacterially expressed recombinant PvPM4 is insoluble, but it is easily refolded into a soluble protein
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
analysis
-
PSM4 is unusable for structural studies by hydrogen/deuterium exchange coupled to mass spectrometry, DXMS, since the method requires the use of proteases working at acidic pH and low temperatures, in contrast to PSM2, EC 3.4.23.39
medicine