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(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
-
hPhe-PSI[PO2CH2]-Phe
phosphinic dipeptide analog
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-3-aminobenzamide
highly effective against the malaria parasites, IC50 values of 233 nM
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-4-aminobenzamide
highly effective against the malaria parasites, IC50 values of 283 nM
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-pivalamide
most effective inhibitor of isoform M1 and one of the more potent inhibitors of isoform M17 tested, the most effective compound against 3D7 malaria parasites, with an IC50 of 227 nM
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
-
tert-butyl (1-(4-(1H-Pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)carbamate
compound shows good in vitro inhibitory properties, but IC50 for parasite growth is only 783 nM, suggesting that compounds substituted with the N-Boc group are either less capable of cellular penetration or less stable than the corresponding N-acyl derivatives
tosedostat
i.e. (2S)-({(2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoyl}amino)(phenyl)ethanoic acid, crystal 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
-
1,10-phenanthroline
1 mM, 80% inhibition
1-hydroxy-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid (4-phenyl-butyl)-amide
-
-
1-hydroxy-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid 4-fluoro-benzylamide
-
-
2-(4-benzyl-piperidine-1-carbonyl)-4-methyl-pentanoic acid hydroxyamide
-
-
2-benzyl-3-(3,4-dihydro-1H-isoquinolin-2-yl)-N-hydroxy-3-oxo-propionamide
-
-
2-benzyl-3-(4-benzyl-piperazin-1-yl)-N-hydroxy-3-oxo-propionamide
-
-
2-benzyl-3-(4-benzyl-piperidin-1-yl)-N-hydroxy-3-oxo-propionamide
-
-
2-benzyl-N-(2,2-diphenyl-ethyl)-N'-hydroxy-malonamide
-
-
2-benzyl-N-(4-chloro-benzyl)-N'-hydroxy-malonamide
-
-
2-benzyl-N-(4-fluoro-benzyl)-N'-hydroxy-malonamide
-
-
2-benzyl-N-biphenyl-3-ylmethyl-N'-hydroxy-malonamide
-
-
2-benzyl-N-hydroxy-N'-(2-methyl-benzyl)-malonamide
-
-
2-benzyl-N-hydroxy-N'-(3-phenoxy-benzyl)-malonamide
-
-
2-benzyl-N-hydroxy-N'-(3-phenyl-propyl)-malonamide
-
-
2-benzyl-N-hydroxy-N'-(4-phenyl-butyl)-malonamide
-
-
2-benzyl-N-hydroxy-N'-indan-2-yl-malonamide
-
-
2-benzyl-N-hydroxy-N'-naphthalen-1-ylmethyl-malonamide
-
-
2-benzyl-N-hydroxy-N'-phenethyl-malonamide
-
-
2N-dibenzyl-N'-hydroxy-malonamide
-
-
3-(3,4-dihydro-1H-isoquinolin-2-yl)-N-hydroxy-3-oxo-2-(3-phenoxy-benzyl)-propionamide
-
-
3-(4-benzyl-piperidin-1-yl)-N-hydroxy-3-oxo-2-(3-phenoxybenzyl)-propionamide
-
-
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-3-aminobenzamide
highly effective against the malaria parasites, IC50 values of 233 nM
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-4-aminobenzamide
highly effective against the malaria parasites, IC50 values of 283 nM
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-pivalamide
most effective inhibitor of isoform M1 and one of the more potent inhibitors of isoform M17 tested, the most effective compound against 3D7 malaria parasites, with an IC50 of 227 nM
N-(4-chloro-benzyl)-N'-hydroxy-2-(3-phenoxy-benzyl)-malonamide
-
-
N-(4-chloro-benzyl)-N'-hydroxy-2-isobutyl-malonamide
-
-
N-(4-fluoro-benzyl)-N'-hydroxy-2-isobutyl-malonamide
-
-
N-(4-fluoro-benzyl)-N'-hydroxy-2-[1-phenyl-meth-(E)-ylidene]-malonamide
-
-
N-(4-fluoro-benzyl)-N'-hydroxy-2-[1-phenyl-meth-(Z)-ylidene]-malonamide
-
-
N-benzyl-N'-hydroxy-2-(3-phenoxy-benzyl)-malonamide
-
-
N-benzyl-N'-hydroxy-2-isobutyl-malonamide
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
N-hydroxy-2-(3-phenoxy-benzyl)-N'-(3-phenyl-propyl)-malonamide
-
-
N-hydroxy-2-(3-phenoxy-benzyl)-N'-(4-phenyl-butyl)-malonamide
-
-
N-hydroxy-2-(3-phenoxy-benzyl)-N'-(4-trifluoromethyl-benzyl)-malonamide
-
-
N-hydroxy-2-isobutyl-N'-(1,2,3,4-tetrahydro-naphthalen-1-yl)-malonamide
-
-
N-hydroxy-2-isobutyl-N'-(3-phenoxy-benzyl)-malonamide
-
-
N-hydroxy-2-isobutyl-N'-(3-phenyl-propyl)-malonamide
-
-
N-hydroxy-2-isobutyl-N'-(4-phenyl-butyl)-malonamide
-
-
N-hydroxy-2-isobutyl-N'-naphthalen-1-ylmethyl-malonamide
-
-
N-hydroxy-2-isobutyl-N'-phenethyl-malonamide
-
-
N-hydroxy-N'-(4-phenyl-butyl)-2-[1-phenyl-meth-(Z)-ylidene]-malonamide
-
-
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
-
N-[(2S,3R)-3-amino-2-hydroxy-4-(4-methoxyphenyl)butanoyl]-L-leucine
-
-
N-[(2S,3R)-3-amino-2-hydroxy-4-(naphthalen-2-yl)butanoyl]-L-leucine
-
-
N-[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-norleucine
-
-
N-[(2S,3R)-3-amino-2-hydroxyheptanoyl]-L-leucine
-
-
N-[(2S,3R)-3-amino-4-[4-(benzyloxy)phenyl]-2-hydroxybutanoyl]-L-leucine
-
-
N2-[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-N6-[(benzyloxy)carbonyl]-L-lysine
-
-
tert-butyl (1-(4-(1H-Pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)carbamate
compound shows good in vitro inhibitory properties, but IC50 for parasite growth is only 783 nM, suggesting that compounds substituted with the N-Boc group are either less capable of cellular penetration or less stable than the corresponding N-acyl derivatives
tosedostat
i.e. (2S)-([(2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoyl]amino)(phenyl)ethanoic acid, crystal structure
Zn2+
0.1 mM, 80% inhibition
bestatin
-
-
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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
0.000025
bestatin
pH and temperature not specified in the publication
0.000013
hPhe-PSI[PO2CH2]-Phe
pH and temperature not specified in the publication
0.000014
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-3-aminobenzamide
pH 8.0, 37°C
0.000011
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-4-aminobenzamide
pH 8.0, 37°C
0.000028
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-pivalamide
pH 8.0, 37°C
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
0.00003
tert-butyl (1-(4-(1H-Pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)carbamate
pH 8.0, 37°C
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
0.00012 - 0.0038
bestatin
0.00048
bestatin methyl ester
0.0055
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-3-aminobenzamide
pH 8.0, 37°C
0.0074
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-4-aminobenzamide
pH 8.0, 37°C
0.0007
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-pivalamide
pH 8.0, 37°C
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
0.000043
N-[(2S,3R)-3-amino-2-hydroxy-4-(4-methoxyphenyl)butanoyl]-L-leucine
-
pH 7.5, temperature not specified in the publication
0.003
N-[(2S,3R)-3-amino-2-hydroxy-4-(naphthalen-2-yl)butanoyl]-L-leucine
-
pH 7.5, temperature not specified in the publication
0.0009
N-[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-norleucine
-
pH 7.5, temperature not specified in the publication
0.0053
N-[(2S,3R)-3-amino-2-hydroxyheptanoyl]-L-leucine
-
pH 7.5, temperature not specified in the publication
0.00049
N-[(2S,3R)-3-amino-4-[4-(benzyloxy)phenyl]-2-hydroxybutanoyl]-L-leucine
-
pH 7.5, temperature not specified in the publication
0.00145
N2-[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-N6-[(benzyloxy)carbonyl]-L-lysine
-
pH 7.5, temperature not specified in the publication
0.0008
tert-butyl (1-(4-(1H-Pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)carbamate
pH 8.0, 37°C
0.00012
bestatin
pH 7.5, 37°C
0.00019
bestatin
-
pH 7.5, temperature not specified in the publication
0.0038
bestatin
pH 5.5, 37°C
0.00048
bestatin methyl ester
pH 7.5, 37°C
0.00048
bestatin methyl ester
pH 5.5, 37°C
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0.01
1-hydroxy-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid (4-phenyl-butyl)-amide
Plasmodium falciparum
-
IC50 above 0.01 mM, in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.01
1-hydroxy-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid 4-fluoro-benzylamide
Plasmodium falciparum
-
IC50 above 0.01 mM, in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000406
2-(4-benzyl-piperidine-1-carbonyl)-4-methyl-pentanoic acid hydroxyamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000253
2-benzyl-3-(3,4-dihydro-1H-isoquinolin-2-yl)-N-hydroxy-3-oxo-propionamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.00176
2-benzyl-3-(4-benzyl-piperazin-1-yl)-N-hydroxy-3-oxo-propionamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000206
2-benzyl-3-(4-benzyl-piperidin-1-yl)-N-hydroxy-3-oxo-propionamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.005363
2-benzyl-N-(2,2-diphenyl-ethyl)-N'-hydroxy-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.00017
2-benzyl-N-(4-chloro-benzyl)-N'-hydroxy-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000027
2-benzyl-N-(4-fluoro-benzyl)-N'-hydroxy-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.001168
2-benzyl-N-biphenyl-3-ylmethyl-N'-hydroxy-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000041
2-benzyl-N-hydroxy-N'-(2-methyl-benzyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.002515
2-benzyl-N-hydroxy-N'-(3-phenoxy-benzyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000125
2-benzyl-N-hydroxy-N'-(3-phenyl-propyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000046
2-benzyl-N-hydroxy-N'-(4-phenyl-butyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.001931
2-benzyl-N-hydroxy-N'-indan-2-yl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000107
2-benzyl-N-hydroxy-N'-naphthalen-1-ylmethyl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.001011
2-benzyl-N-hydroxy-N'-phenethyl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000125
2N-dibenzyl-N'-hydroxy-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000966
3-(3,4-dihydro-1H-isoquinolin-2-yl)-N-hydroxy-3-oxo-2-(3-phenoxy-benzyl)-propionamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000248
3-(4-benzyl-piperidin-1-yl)-N-hydroxy-3-oxo-2-(3-phenoxybenzyl)-propionamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.00013
N-(4-chloro-benzyl)-N'-hydroxy-2-(3-phenoxy-benzyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000904
N-(4-chloro-benzyl)-N'-hydroxy-2-isobutyl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.003896
N-(4-fluoro-benzyl)-N'-hydroxy-2-isobutyl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.00033
N-(4-fluoro-benzyl)-N'-hydroxy-2-[1-phenyl-meth-(E)-ylidene]-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000006
N-(4-fluoro-benzyl)-N'-hydroxy-2-[1-phenyl-meth-(Z)-ylidene]-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000164
N-benzyl-N'-hydroxy-2-(3-phenoxy-benzyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000495
N-benzyl-N'-hydroxy-2-isobutyl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000527
N-hydroxy-2-(3-phenoxy-benzyl)-N'-(3-phenyl-propyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000225
N-hydroxy-2-(3-phenoxy-benzyl)-N'-(4-phenyl-butyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000231
N-hydroxy-2-(3-phenoxy-benzyl)-N'-(4-trifluoromethyl-benzyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000109
N-hydroxy-2-isobutyl-N'-(1,2,3,4-tetrahydro-naphthalen-1-yl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000045
N-hydroxy-2-isobutyl-N'-(3-phenoxy-benzyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.00079
N-hydroxy-2-isobutyl-N'-(3-phenyl-propyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.001149
N-hydroxy-2-isobutyl-N'-(4-phenyl-butyl)-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000091
N-hydroxy-2-isobutyl-N'-naphthalen-1-ylmethyl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000885
N-hydroxy-2-isobutyl-N'-phenethyl-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
0.000013
N-hydroxy-N'-(4-phenyl-butyl)-2-[1-phenyl-meth-(Z)-ylidene]-malonamide
Plasmodium falciparum
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25°C
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Flipo, M.; Beghyn, T.; Leroux, V.; Florent, I.; Deprez, B.P.; Deprez-Poulain, R.F.
Novel selective inhibitors of the zinc plasmodial aminopeptidase PfA-M1 as potential antimalarial agents
J. Med. Chem.
50
1322-1334
2007
Plasmodium falciparum, Plasmodium falciparum FcB1
brenda
Ragheb, D.; Dalal, S.; Bompiani, K.M.; Ray, W.K.; Klemba, M.
Distribution and biochemical properties of an M1-family aminopeptidase in Plasmodium falciparum indicate a role in vacuolar hemoglobin catabolism
J. Biol. Chem.
286
27255-27265
2011
Plasmodium falciparum (Q8IEK1), Plasmodium falciparum
brenda
Velmourougane, G.; Harbut, M.B.; Dalal, S.; McGowan, S.; Oellig, C.A.; Meinhardt, N.; Whisstock, J.C.; Klemba, M.; Greenbaum, D.C.
Synthesis of new (-)-bestatin-based inhibitor libraries reveals a novel binding mode in the S1 pocket of the essential malaria M1 metalloaminopeptidase
J. Med. Chem.
54
1655-1666
2011
Plasmodium falciparum
brenda
Azimzadeh, O.; Sow, C.; Geze, M.; Nyalwidhe, J.; Florent, I.
Plasmodium falciparum PfA-M1 aminopeptidase is trafficked via the parasitophorous vacuole and marginally delivered to the food vacuole
Malar. J.
9
189
2010
Plasmodium falciparum (O96935), Plasmodium falciparum
brenda
McGowan, S.; Oellig, C.A.; Birru, W.A.; Caradoc-Davies, T.T.; Stack, C.M.; Lowther, J.; Skinner-Adams, T.; Mucha, A.; Kafarski, P.; Grembecka, J.; Trenholme, K.R.; Buckle, A.M.; Gardiner, D.L.; Dalton, J.P.; Whisstock, J.C.
Structure of the Plasmodium falciparum M17 aminopeptidase and significance for the design of drugs targeting the neutral exopeptidases
Proc. Natl. Acad. Sci. USA
107
2449-2454
2010
Plasmodium falciparum (Q8IL11), Plasmodium falciparum
brenda
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
Proc. Natl. Acad. Sci. USA
108
E526-E534
2011
Plasmodium falciparum, Plasmodium falciparum (Q8IL11)
brenda
Mistry, S.N.; Drinkwater, N.; Ruggeri, C.; Sivaraman, K.K.; Loganathan, S.; Fletcher, S.; Drag, M.; Paiardini, A.; Avery, V.M.; Scammells, P.J.; McGowan, S.
Two-pronged attack: dual inhibition of Plasmodium falciparum M1 and M17 metalloaminopeptidases by a novel series of hydroxamic acid-based inhibitors
J. Med. Chem.
57
9168-9183
2014
Plasmodium falciparum (O96935), Plasmodium falciparum (Q8IL11), Plasmodium falciparum, Plasmodium falciparum isolate FcB1/Columbia (O96935)
brenda
Dalal, S.; Ragheb, D.R.; Klemba, M.
Engagement of the S1, S1' and S2' subsites drives efficient catalysis of peptide bond hydrolysis by the M1-family aminopeptidase from Plasmodium falciparum
Mol. Biochem. Parasitol.
183
70-77
2012
Plasmodium falciparum
brenda
Gonzalez-Bacerio, J.; Osuna, J.; Ponce, A.; Fando, R.; Figarella, K.; Mendez, Y.; Charli, J.L.; Chavez, M.D.
High-level expression in Escherichia coli, purification and kinetic characterization of Plasmodium falciparum M1-aminopeptidase
Protein Expr. Purif.
104C
103-114
2014
Plasmodium falciparum (Q8IEK1)
brenda
Drinkwater, N.; Bamert, R.S.; Kannan Sivaraman, K.; Paiardini, A.; McGowan, S.
X-ray crystal structures of an orally available aminopeptidase inhibitor, tosedostat, bound to anti-malarial drug targets PfA-M1 and PfA-M17
Proteins
83
789-795
2015
Plasmodium falciparum (O96935), Plasmodium falciparum (Q8IL11), Plasmodium falciparum, Plasmodium falciparum isolate FcB1/Columbia (O96935)
brenda