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Literature summary for 3.5.1.98 extracted from

  • Vannini, A.; Volpari, C.; Filocamo, G.; Casavola, E.C.; Brunetti, M.; Renzoni, D.; Chakravarty, P.; Paolini, C.; De Francesco, R.; Gallinari, P.; Steinkuhler, C.; Di Marco, S.
    Crystal structure of a eukaryotic zinc-dependent histone deacetylase, human HDAC8, complexed with a hydroxamic acid inhibitor (2004), Proc. Natl. Acad. Sci. USA, 101, 15064-15069.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine knock-down of isoform HDAC8 expression by RNAi inhibits growth of human lung, colon, and cervical cancer cell lines Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
molecular modeling of isoform HDAC8 in complex with inhibitor N-hydroxy-4-(methyl[(5-pyridin-2-yl-2-thienyl)sulfonyl]amino)benzamide Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information knock-down of isoform HDAC8 expression by RNAi inhibits growth of human lung, colon, and cervical cancer cell lines Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
apicidin
-
Homo sapiens
N-hydroxy-4-(methyl[(5-pyridin-2-yl-2-thienyl)sulfonyl]amino)benzamide
-
Homo sapiens
pyridin-3-ylmethyl (4-[[(2-aminophenyl)amino]carbonyl]benzyl)carbamate i.e. MS27-275 Homo sapiens
suberoylanilide hydroxamic acid
-
Homo sapiens
trichostatin A
-
Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
K+ presence of two potassium ions in the structure of isoform HDAC8, one of which interacts with the key catalytic residues. Direct role of potassium in fold stabilization Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9BY41 isoforms HDAC1, HDAC3, HDAC8
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000006
-
isoform HDAC3 Homo sapiens trichostatin A
0.0000007
-
isoform HDAC3 Homo sapiens apicidin
0.0000015
-
isoform HDAC1 Homo sapiens trichostatin A
0.000002
-
isoform HDAC1 Homo sapiens apicidin
0.000044
-
isoform HDAC3 Homo sapiens N-hydroxy-4-(methyl[(5-pyridin-2-yl-2-thienyl)sulfonyl]amino)benzamide
0.000086
-
isoform HDAC1 Homo sapiens N-hydroxy-4-(methyl[(5-pyridin-2-yl-2-thienyl)sulfonyl]amino)benzamide
0.000106
-
isoform HDAC3 Homo sapiens suberoylanilide hydroxamic acid
0.000119
-
isoform HDAC1 Homo sapiens suberoylanilide hydroxamic acid
0.000175
-
isoform HDAC8 Homo sapiens N-hydroxy-4-(methyl[(5-pyridin-2-yl-2-thienyl)sulfonyl]amino)benzamide
0.000185
-
isoform HDAC1 Homo sapiens pyridin-3-ylmethyl (4-[[(2-aminophenyl)amino]carbonyl]benzyl)carbamate
0.000201
-
isoform HDAC3 Homo sapiens pyridin-3-ylmethyl (4-[[(2-aminophenyl)amino]carbonyl]benzyl)carbamate
0.00049
-
isoform HDAC8 Homo sapiens trichostatin A
0.001
-
isoform HDAC8 Homo sapiens apicidin
0.004
-
isoform HDAC8 Homo sapiens suberoylanilide hydroxamic acid
0.01
-
isoform HDAC8 Homo sapiens pyridin-3-ylmethyl (4-[[(2-aminophenyl)amino]carbonyl]benzyl)carbamate