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Literature summary for 3.5.1.98 extracted from

  • Patel, V.; Mazitschek, R.; Coleman, B.; Nguyen, C.; Urgaonkar, S.; Cortese, J.; Barker, R.H.; Greenberg, E.; Tang, W.; Bradner, J.E.; Schreiber, S.L.; Duraisingh, M.T.; Wirth, D.F.; Clardy, J.
    Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum (2009), J. Med. Chem., 52, 2185-2187.
    View publication on PubMedView publication on EuropePMC
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Cloned(Commentary)

Cloned (Comment) Organism
into the pAc5.1 expression vector for expression in S2 insect cells Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
6-[(2E)-2-[(2-bromo-4-hydroxy-5-methoxyphenyl)methylidene]hydrazino]-N-hydroxy-6-oxohexanamide
-
 Plasmodium falciparum
6-[(2E)-2-[(2-bromo-4-hydroxyphenyl)methylidene]hydrazino]-N-hydroxy-6-oxohexanamide
-
 Plasmodium falciparum
6-[(2E)-2-[(2-bromo-5-hydroxyphenyl)methylidene]hydrazino]-N-hydroxy-6-oxohexanamide
-
 Plasmodium falciparum
7-[(2E)-2-[(2-bromo-4-hydroxy-5-methoxyphenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
7-[(2E)-2-[(2-bromo-5-hydroxyphenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
7-[(2E)-2-[(2-bromo-5-methoxyphenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
7-[(2E)-2-[(2-bromophenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
7-[(2E)-2-[(2-bromopyridin-3-yl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
7-[(2E)-2-[(2-chlorophenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
7-[(2E)-2-[(6-bromo-1,3-benzodioxol-5-yl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
7-[(2E)-2-[[4-(dimethylamino)-2-hydroxyphenyl]methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
8-[(2E)-2-[(2,5-dihydroxyphenyl)methylidene]hydrazino]-N-hydroxy-8-oxooctanamide
-
 Plasmodium falciparum
apicidin
-
 Plasmodium falciparum
LBH-589
-
 Plasmodium falciparum
MS-275
-
 Plasmodium falciparum
N-hydroxy-7-[(2E)-2-[(2-hydroxynaphthalen-1-yl)methylidene]hydrazino]-7-oxoheptanamide
-
 Plasmodium falciparum
N-hydroxy-7-[(2E)-2-[(3-hydroxyphenyl)methylidene]hydrazino]-7-oxoheptanamide
-
 Plasmodium falciparum
N-hydroxy-7-[(2E)-2-[[4-(1H-imidazol-1-yl)phenyl]methylidene]hydrazino]-7-oxoheptanamide
-
 Plasmodium falciparum
N-hydroxy-8-oxo-8-[(2E)-2-[(2,4,6-trihydroxyphenyl)methylidene]hydrazino]octanamide
-
 Plasmodium falciparum
splitomicin
-
 Plasmodium falciparum
suberoylanilide hydroxamic acid SAHA Plasmodium falciparum
trichostatin A TSA Plasmodium falciparum
[4-[(E)-[[6-(hydroxyamino)-6-oxohexanoyl]hydrazono]methyl]phenyl]boronic acid
-
 Plasmodium falciparum

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.03
-
 Ac-Leu-Gly-Lys(Ac)-7-amido-4-methylcoumarin apparent KM Plasmodium falciparum

Localization

Localization Comment Organism GeneOntology No. Textmining
nucleus
-
 Plasmodium falciparum 5634
-

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+
-
 Plasmodium falciparum

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
51000
-
-
 Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum Q7K6A1
-
-

Purification (Commentary)

Purification (Comment) Organism
using an engineered HPC4 epitope tag at the C-terminus Plasmodium falciparum

Source Tissue

Source Tissue Comment Organism Textmining
gametocyte expressed in gametocytes and mature blood stages of the malaria parasite life cycle Plasmodium falciparum
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ac-Leu-Gly-Lys(Ac)-7-amido-4-methylcoumarin + H2O
-
 Plasmodium falciparum Ac-Leu-Gly-Lys-7-amido-4-methylcoumarin + acetate
-
 ?

Synonyms

Synonyms Comment Organism
class I histone deacetylase
-
 Plasmodium falciparum
pfHDAC-1
-
 Plasmodium falciparum

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.19
-
 Ac-Leu-Gly-Lys(Ac)-7-amido-4-methylcoumarin
-
 Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000006
-
-
 Plasmodium falciparum trichostatin A
0.000001
-
-
 Plasmodium falciparum apicidin
0.0000018
-
-
 Plasmodium falciparum LBH-589
0.000015
-
-
 Plasmodium falciparum N-hydroxy-7-[(2E)-2-[[4-(1H-imidazol-1-yl)phenyl]methylidene]hydrazino]-7-oxoheptanamide
0.00002
-
-
 Plasmodium falciparum 7-[(2E)-2-[(6-bromo-1,3-benzodioxol-5-yl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
0.000022
-
-
 Plasmodium falciparum 7-[(2E)-2-[(2-bromo-5-methoxyphenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
0.000036
-
-
 Plasmodium falciparum 7-[(2E)-2-[(2-bromopyridin-3-yl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
0.000037
-
-
 Plasmodium falciparum 7-[(2E)-2-[(2-bromophenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
0.000037
-
-
 Plasmodium falciparum 7-[(2E)-2-[[4-(dimethylamino)-2-hydroxyphenyl]methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
0.000041
-
-
 Plasmodium falciparum N-hydroxy-7-[(2E)-2-[(2-hydroxynaphthalen-1-yl)methylidene]hydrazino]-7-oxoheptanamide
0.000043
-
-
 Plasmodium falciparum N-hydroxy-8-oxo-8-[(2E)-2-[(2,4,6-trihydroxyphenyl)methylidene]hydrazino]octanamide
0.000045
-
-
 Plasmodium falciparum [4-[(E)-[[6-(hydroxyamino)-6-oxohexanoyl]hydrazono]methyl]phenyl]boronic acid
0.000049
-
-
 Plasmodium falciparum 7-[(2E)-2-[(2-bromo-5-hydroxyphenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
0.000059
-
-
 Plasmodium falciparum suberoylanilide hydroxamic acid
0.000059
-
-
 Plasmodium falciparum N-hydroxy-7-[(2E)-2-[(3-hydroxyphenyl)methylidene]hydrazino]-7-oxoheptanamide
0.000059
-
-
 Plasmodium falciparum 6-[(2E)-2-[(2-bromo-4-hydroxy-5-methoxyphenyl)methylidene]hydrazino]-N-hydroxy-6-oxohexanamide
0.000059
-
-
 Plasmodium falciparum 7-[(2E)-2-[(2-bromo-4-hydroxy-5-methoxyphenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
0.000089
-
-
 Plasmodium falciparum 6-[(2E)-2-[(2-bromo-5-hydroxyphenyl)methylidene]hydrazino]-N-hydroxy-6-oxohexanamide
0.00009
-
-
 Plasmodium falciparum 7-[(2E)-2-[(2-chlorophenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
0.000106
-
-
 Plasmodium falciparum 6-[(2E)-2-[(2-bromo-4-hydroxyphenyl)methylidene]hydrazino]-N-hydroxy-6-oxohexanamide
0.00011
-
-
 Plasmodium falciparum 8-[(2E)-2-[(2,5-dihydroxyphenyl)methylidene]hydrazino]-N-hydroxy-8-oxooctanamide
0.00094
-
-
 Plasmodium falciparum MS-275
0.01
-
 larger than 0.01 Plasmodium falciparum splitomicin