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Literature summary 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

Cloned(Commentary)

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.5.1.98 6-[(2E)-2-[(2-bromo-4-hydroxy-5-methoxyphenyl)methylidene]hydrazino]-N-hydroxy-6-oxohexanamide
-
 Plasmodium falciparum
3.5.1.98 6-[(2E)-2-[(2-bromo-4-hydroxyphenyl)methylidene]hydrazino]-N-hydroxy-6-oxohexanamide
-
 Plasmodium falciparum
3.5.1.98 6-[(2E)-2-[(2-bromo-5-hydroxyphenyl)methylidene]hydrazino]-N-hydroxy-6-oxohexanamide
-
 Plasmodium falciparum
3.5.1.98 7-[(2E)-2-[(2-bromo-4-hydroxy-5-methoxyphenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
3.5.1.98 7-[(2E)-2-[(2-bromo-5-hydroxyphenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
3.5.1.98 7-[(2E)-2-[(2-bromo-5-methoxyphenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
3.5.1.98 7-[(2E)-2-[(2-bromophenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
3.5.1.98 7-[(2E)-2-[(2-bromopyridin-3-yl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
3.5.1.98 7-[(2E)-2-[(2-chlorophenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
3.5.1.98 7-[(2E)-2-[(6-bromo-1,3-benzodioxol-5-yl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
3.5.1.98 7-[(2E)-2-[[4-(dimethylamino)-2-hydroxyphenyl]methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
-
 Plasmodium falciparum
3.5.1.98 8-[(2E)-2-[(2,5-dihydroxyphenyl)methylidene]hydrazino]-N-hydroxy-8-oxooctanamide
-
 Plasmodium falciparum
3.5.1.98 apicidin
-
 Plasmodium falciparum
3.5.1.98 LBH-589
-
 Plasmodium falciparum
3.5.1.98 MS-275
-
 Plasmodium falciparum
3.5.1.98 N-hydroxy-7-[(2E)-2-[(2-hydroxynaphthalen-1-yl)methylidene]hydrazino]-7-oxoheptanamide
-
 Plasmodium falciparum
3.5.1.98 N-hydroxy-7-[(2E)-2-[(3-hydroxyphenyl)methylidene]hydrazino]-7-oxoheptanamide
-
 Plasmodium falciparum
3.5.1.98 N-hydroxy-7-[(2E)-2-[[4-(1H-imidazol-1-yl)phenyl]methylidene]hydrazino]-7-oxoheptanamide
-
 Plasmodium falciparum
3.5.1.98 N-hydroxy-8-oxo-8-[(2E)-2-[(2,4,6-trihydroxyphenyl)methylidene]hydrazino]octanamide
-
 Plasmodium falciparum
3.5.1.98 splitomicin
-
 Plasmodium falciparum
3.5.1.98 suberoylanilide hydroxamic acid SAHA Plasmodium falciparum
3.5.1.98 trichostatin A TSA Plasmodium falciparum
3.5.1.98 [4-[(E)-[[6-(hydroxyamino)-6-oxohexanoyl]hydrazono]methyl]phenyl]boronic acid
-
 Plasmodium falciparum

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.5.1.98 0.03
-
 Ac-Leu-Gly-Lys(Ac)-7-amido-4-methylcoumarin apparent KM Plasmodium falciparum

Localization

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

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
3.5.1.98 Zn2+
-
 Plasmodium falciparum

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
3.5.1.98 51000
-
-
 Plasmodium falciparum

Organism

EC Number Organism UniProt Comment Textmining
3.5.1.98 Plasmodium falciparum Q7K6A1
-
-

Purification (Commentary)

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

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

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

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.5.1.98 0.19
-
 Ac-Leu-Gly-Lys(Ac)-7-amido-4-methylcoumarin
-
 Plasmodium falciparum

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.5.1.98 0.0000006
-
-
 Plasmodium falciparum trichostatin A
3.5.1.98 0.000001
-
-
 Plasmodium falciparum apicidin
3.5.1.98 0.0000018
-
-
 Plasmodium falciparum LBH-589
3.5.1.98 0.000015
-
-
 Plasmodium falciparum N-hydroxy-7-[(2E)-2-[[4-(1H-imidazol-1-yl)phenyl]methylidene]hydrazino]-7-oxoheptanamide
3.5.1.98 0.00002
-
-
 Plasmodium falciparum 7-[(2E)-2-[(6-bromo-1,3-benzodioxol-5-yl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
3.5.1.98 0.000022
-
-
 Plasmodium falciparum 7-[(2E)-2-[(2-bromo-5-methoxyphenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
3.5.1.98 0.000036
-
-
 Plasmodium falciparum 7-[(2E)-2-[(2-bromopyridin-3-yl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
3.5.1.98 0.000037
-
-
 Plasmodium falciparum 7-[(2E)-2-[(2-bromophenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
3.5.1.98 0.000037
-
-
 Plasmodium falciparum 7-[(2E)-2-[[4-(dimethylamino)-2-hydroxyphenyl]methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
3.5.1.98 0.000041
-
-
 Plasmodium falciparum N-hydroxy-7-[(2E)-2-[(2-hydroxynaphthalen-1-yl)methylidene]hydrazino]-7-oxoheptanamide
3.5.1.98 0.000043
-
-
 Plasmodium falciparum N-hydroxy-8-oxo-8-[(2E)-2-[(2,4,6-trihydroxyphenyl)methylidene]hydrazino]octanamide
3.5.1.98 0.000045
-
-
 Plasmodium falciparum [4-[(E)-[[6-(hydroxyamino)-6-oxohexanoyl]hydrazono]methyl]phenyl]boronic acid
3.5.1.98 0.000049
-
-
 Plasmodium falciparum 7-[(2E)-2-[(2-bromo-5-hydroxyphenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
3.5.1.98 0.000059
-
-
 Plasmodium falciparum suberoylanilide hydroxamic acid
3.5.1.98 0.000059
-
-
 Plasmodium falciparum N-hydroxy-7-[(2E)-2-[(3-hydroxyphenyl)methylidene]hydrazino]-7-oxoheptanamide
3.5.1.98 0.000059
-
-
 Plasmodium falciparum 6-[(2E)-2-[(2-bromo-4-hydroxy-5-methoxyphenyl)methylidene]hydrazino]-N-hydroxy-6-oxohexanamide
3.5.1.98 0.000059
-
-
 Plasmodium falciparum 7-[(2E)-2-[(2-bromo-4-hydroxy-5-methoxyphenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
3.5.1.98 0.000089
-
-
 Plasmodium falciparum 6-[(2E)-2-[(2-bromo-5-hydroxyphenyl)methylidene]hydrazino]-N-hydroxy-6-oxohexanamide
3.5.1.98 0.00009
-
-
 Plasmodium falciparum 7-[(2E)-2-[(2-chlorophenyl)methylidene]hydrazino]-N-hydroxy-7-oxoheptanamide
3.5.1.98 0.000106
-
-
 Plasmodium falciparum 6-[(2E)-2-[(2-bromo-4-hydroxyphenyl)methylidene]hydrazino]-N-hydroxy-6-oxohexanamide
3.5.1.98 0.00011
-
-
 Plasmodium falciparum 8-[(2E)-2-[(2,5-dihydroxyphenyl)methylidene]hydrazino]-N-hydroxy-8-oxooctanamide
3.5.1.98 0.00094
-
-
 Plasmodium falciparum MS-275
3.5.1.98 0.01
-
 larger than 0.01 Plasmodium falciparum splitomicin