BRENDA - Enzyme Database show
show all sequences of 1.14.11.B1

Lysine-specific demethylase 1-mediated demethylation of histone H3 lysine 9 contributes to interleukin 1beta-induced microsomal prostaglandin E synthase 1 expression in human osteoarthritic chondrocytes

El Mansouri, F.; Nebbaki, S.; Kapoor, M.; Afif, H.; Martel-Pelletier, J.; Pelletier, J.; Benderdour, M.; Fahmi, H.; Arthritis Res. Ther. 16, R113 (2014)

Data extracted from this reference:

Activating Compound
Activating Compound
Commentary
Organism
Structure
additional information
interleukin-1beta enhances recruitment of LSD1 to mPGES-1 promoter
Homo sapiens
Cloned(Commentary)
Commentary
Organism
gene KDM1A, real-time PCR enzyme expression analysis
Homo sapiens
Engineering
Amino acid exchange
Commentary
Organism
additional information
the enzyme is knocked out by expression of specific siRNA for LSD1 in chondrocytes
Homo sapiens
Inhibitors
Inhibitors
Commentary
Organism
Structure
Pargyline
-
Homo sapiens
Tranylcypromine
-
Homo sapiens
Localization
Localization
Commentary
Organism
GeneOntology No.
Textmining
chromatin
-
Homo sapiens
785
-
mitochondrion
enzyme LSD1 is present at the proximal region of the microsomal PGES-1 promoter
Homo sapiens
5739
-
Metals/Ions
Metals/Ions
Commentary
Organism
Structure
Fe2+
required
Homo sapiens
Natural Substrates/ Products (Substrates)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
histone H3 N6,N6-dimethyl-L-lysine9 + 2-oxoglutarate + O2
Homo sapiens
-
histone H3 N6-methyl-L-lysine9 + succinate + formaldehyde + CO2
-
-
?
histone H3 N6-methyl-L-lysine9 + 2-oxoglutarate + O2
Homo sapiens
-
histone H3 L-lysine9 + succinate + formaldehyde + CO2
-
-
?
Organism
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
Homo sapiens
O60341
-
-
Source Tissue
Source Tissue
Commentary
Organism
Textmining
chondrocyte
osteoarthritic chondrocytes
Homo sapiens
-
Substrates and Products (Substrate)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
histone H3 N6,N6-dimethyl-L-lysine9 + 2-oxoglutarate + O2
-
744188
Homo sapiens
histone H3 N6-methyl-L-lysine9 + succinate + formaldehyde + CO2
-
-
-
?
histone H3 N6-methyl-L-lysine9 + 2-oxoglutarate + O2
-
744188
Homo sapiens
histone H3 L-lysine9 + succinate + formaldehyde + CO2
-
-
-
?
additional information
histone H3 N6,N6,N6-trimethyl-L-lysine9 is no substrate
744188
Homo sapiens
?
-
-
-
-
Cofactor
Cofactor
Commentary
Organism
Structure
FAD
required, LSD1 utilizes FAD as an essential cofactor in catalyzing demethylation of mono- and di-methylated H3K9. Interleukin-1-induced H3K9 demethylation and LSD1 recruitment in human chondrocytes are not associated with significant changes in FAD levels
Homo sapiens
Activating Compound (protein specific)
Activating Compound
Commentary
Organism
Structure
additional information
interleukin-1beta enhances recruitment of LSD1 to mPGES-1 promoter
Homo sapiens
Cloned(Commentary) (protein specific)
Commentary
Organism
gene KDM1A, real-time PCR enzyme expression analysis
Homo sapiens
Cofactor (protein specific)
Cofactor
Commentary
Organism
Structure
FAD
required, LSD1 utilizes FAD as an essential cofactor in catalyzing demethylation of mono- and di-methylated H3K9. Interleukin-1-induced H3K9 demethylation and LSD1 recruitment in human chondrocytes are not associated with significant changes in FAD levels
Homo sapiens
Engineering (protein specific)
Amino acid exchange
Commentary
Organism
additional information
the enzyme is knocked out by expression of specific siRNA for LSD1 in chondrocytes
Homo sapiens
Inhibitors (protein specific)
Inhibitors
Commentary
Organism
Structure
Pargyline
-
Homo sapiens
Tranylcypromine
-
Homo sapiens
Localization (protein specific)
Localization
Commentary
Organism
GeneOntology No.
Textmining
chromatin
-
Homo sapiens
785
-
mitochondrion
enzyme LSD1 is present at the proximal region of the microsomal PGES-1 promoter
Homo sapiens
5739
-
Metals/Ions (protein specific)
Metals/Ions
Commentary
Organism
Structure
Fe2+
required
Homo sapiens
Natural Substrates/ Products (Substrates) (protein specific)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
histone H3 N6,N6-dimethyl-L-lysine9 + 2-oxoglutarate + O2
Homo sapiens
-
histone H3 N6-methyl-L-lysine9 + succinate + formaldehyde + CO2
-
-
?
histone H3 N6-methyl-L-lysine9 + 2-oxoglutarate + O2
Homo sapiens
-
histone H3 L-lysine9 + succinate + formaldehyde + CO2
-
-
?
Source Tissue (protein specific)
Source Tissue
Commentary
Organism
Textmining
chondrocyte
osteoarthritic chondrocytes
Homo sapiens
-
Substrates and Products (Substrate) (protein specific)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
histone H3 N6,N6-dimethyl-L-lysine9 + 2-oxoglutarate + O2
-
744188
Homo sapiens
histone H3 N6-methyl-L-lysine9 + succinate + formaldehyde + CO2
-
-
-
?
histone H3 N6-methyl-L-lysine9 + 2-oxoglutarate + O2
-
744188
Homo sapiens
histone H3 L-lysine9 + succinate + formaldehyde + CO2
-
-
-
?
additional information
histone H3 N6,N6,N6-trimethyl-L-lysine9 is no substrate
744188
Homo sapiens
?
-
-
-
-
General Information
General Information
Commentary
Organism
evolution
the enzyme belongs to the superfamily of flavin adenine dinucleotide (FAD)–dependent amine oxidases
Homo sapiens
malfunction
both pharmacological inhibition of LSD1 and small interfering RNA (siRNA) knockdown prevents interleukin 1beta-induced H3K9 demethylation at the mPGES-1 promoter as well as concomitant mPGES-1 protein expression. The level of LSD1 expression is elevated in osteoarthritis cartilage
Homo sapiens
physiological function
lysine-specific demethylase 1-mediated demethylation of histone H3 lysine 9 contributes to interleukin 1beta-induced microsomal prostaglandin E synthase 1 (mPGES-1) expression in human osteoarthritic chondrocytes. mPGES-1 catalyzes the terminal step in the biosynthesis of PGE2, a critical mediator in the pathophysiology of osteoarthritis. Histone methylation plays an important role in epigenetic gene regulation. LSD1 modulates gene expression through demethylation of either H3K4 or H3K9. H3K9 methylation usually suppresses transcription, whereas H3K4 methylation generally activates transcription. The induction of mPGES-1 expression by interleukin-1beta is associated with decreased levels of mono- and dimethylated H3K9, but not trimethylated H3K9, at the mPGES-1 promoter correlating with the recruitment of the histone demethylase LSD1
Homo sapiens
General Information (protein specific)
General Information
Commentary
Organism
evolution
the enzyme belongs to the superfamily of flavin adenine dinucleotide (FAD)–dependent amine oxidases
Homo sapiens
malfunction
both pharmacological inhibition of LSD1 and small interfering RNA (siRNA) knockdown prevents interleukin 1beta-induced H3K9 demethylation at the mPGES-1 promoter as well as concomitant mPGES-1 protein expression. The level of LSD1 expression is elevated in osteoarthritis cartilage
Homo sapiens
physiological function
lysine-specific demethylase 1-mediated demethylation of histone H3 lysine 9 contributes to interleukin 1beta-induced microsomal prostaglandin E synthase 1 (mPGES-1) expression in human osteoarthritic chondrocytes. mPGES-1 catalyzes the terminal step in the biosynthesis of PGE2, a critical mediator in the pathophysiology of osteoarthritis. Histone methylation plays an important role in epigenetic gene regulation. LSD1 modulates gene expression through demethylation of either H3K4 or H3K9. H3K9 methylation usually suppresses transcription, whereas H3K4 methylation generally activates transcription. The induction of mPGES-1 expression by interleukin-1beta is associated with decreased levels of mono- and dimethylated H3K9, but not trimethylated H3K9, at the mPGES-1 promoter correlating with the recruitment of the histone demethylase LSD1
Homo sapiens
Other publictions for EC 1.14.11.B1
No.
1st author
Pub Med
title
organims
journal
volume
pages
year
Activating Compound
Application
Cloned(Commentary)
Crystallization (Commentary)
Engineering
General Stability
Inhibitors
KM Value [mM]
Localization
Metals/Ions
Molecular Weight [Da]
Natural Substrates/ Products (Substrates)
Organic Solvent Stability
Organism
Oxidation Stability
Posttranslational Modification
Purification (Commentary)
Reaction
Renatured (Commentary)
Source Tissue
Specific Activity [micromol/min/mg]
Storage Stability
Substrates and Products (Substrate)
Subunits
Temperature Optimum [°C]
Temperature Range [°C]
Temperature Stability [°C]
Turnover Number [1/s]
pH Optimum
pH Range
pH Stability
Cofactor
Ki Value [mM]
pI Value
IC50 Value
Activating Compound (protein specific)
Application (protein specific)
Cloned(Commentary) (protein specific)
Cofactor (protein specific)
Crystallization (Commentary) (protein specific)
Engineering (protein specific)
General Stability (protein specific)
IC50 Value (protein specific)
Inhibitors (protein specific)
Ki Value [mM] (protein specific)
KM Value [mM] (protein specific)
Localization (protein specific)
Metals/Ions (protein specific)
Molecular Weight [Da] (protein specific)
Natural Substrates/ Products (Substrates) (protein specific)
Organic Solvent Stability (protein specific)
Oxidation Stability (protein specific)
Posttranslational Modification (protein specific)
Purification (Commentary) (protein specific)
Renatured (Commentary) (protein specific)
Source Tissue (protein specific)
Specific Activity [micromol/min/mg] (protein specific)
Storage Stability (protein specific)
Substrates and Products (Substrate) (protein specific)
Subunits (protein specific)
Temperature Optimum [°C] (protein specific)
Temperature Range [°C] (protein specific)
Temperature Stability [°C] (protein specific)
Turnover Number [1/s] (protein specific)
pH Optimum (protein specific)
pH Range (protein specific)
pH Stability (protein specific)
pI Value (protein specific)
Expression
General Information
General Information (protein specific)
Expression (protein specific)
KCat/KM [mM/s]
KCat/KM [mM/s] (protein specific)
743916
Hancock
The activity of JmjC histone ...
Homo sapiens
ACS Chem. Biol.
12
1011-1019
2017
-
1
1
-
1
-
-
4
-
-
-
1
-
1
-
-
1
-
-
1
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
1
1
-
-
1
-
-
-
-
4
-
-
-
1
-
-
-
1
-
1
-
-
3
-
-
-
-
-
-
-
-
-
-
2
2
-
-
-
743984
Cai
Histone demethylase JMJD1C re ...
Homo sapiens
Am. J. Cancer Res.
7
115-124
2017
-
-
1
-
1
-
-
-
1
-
-
1
-
2
-
-
-
-
-
11
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
11
-
-
1
-
-
-
-
-
-
-
-
-
-
2
2
-
-
-
744413
Maina
Histone demethylase PHF8 regu ...
Homo sapiens
Biochim. Biophys. Acta
1860
1002-1012
2017
-
-
-
-
1
-
-
-
1
-
-
3
-
1
-
-
-
-
-
2
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
3
-
-
-
-
-
2
-
-
4
-
-
-
-
-
-
-
-
-
-
2
2
-
-
-
744494
Amano
Development and crystallograp ...
Homo sapiens
Bioorg. Med. Chem.
25
2617-2624
2017
-
-
-
1
-
-
15
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
1
-
-
-
1
-
-
-
13
-
-
-
-
-
-
1
-
-
-
15
13
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
745030
Audonnet
JMJ24 antagonizes histone H3K ...
Arabidopsis thaliana, Arabidopsis thaliana Col-0
Gene Expr. Patterns
25-26
1-7
2017
-
-
1
-
1
-
-
-
-
-
-
4
-
5
-
-
-
-
-
-
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
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-
2
-
-
2
-
-
-
-
-
-
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-
4
-
-
-
-
-
-
-
-
4
-
-
-
-
-
-
-
-
-
-
2
4
-
-
-
745752
Liu
LincRNAFEZF1-AS1 represses p2 ...
Homo sapiens
Mol. Cancer
16
39
2017
-
-
-
-
-
-
-
-
1
1
-
3
-
1
-
-
-
-
-
3
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
1
-
3
-
-
-
-
-
3
-
-
3
-
-
-
-
-
-
-
-
-
-
1
1
-
-
-
745771
Vyas
Lysine-specific demethylase-1 ...
Mus musculus
Mol. Cell. Neurosci.
82
1-11
2017
-
-
1
-
1
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
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-
1
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-
1
-
-
-
-
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-
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-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
2
2
-
-
-
745949
An
HistoneH3 demethylase JMJD2A ...
Homo sapiens
Oncotarget
8
49093-49109
2017
-
-
1
-
1
-
-
-
-
-
-
1
-
1
-
-
-
-
-
4
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
4
-
-
1
-
-
-
-
-
-
-
-
-
-
2
2
-
-
-
745951
Qin
The histone demethylase Kdm3a ...
Mus musculus
Oncotarget
8
84761-84775
2017
1
-
-
-
1
-
-
-
1
1
-
3
-
2
-
-
-
-
-
5
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
1
-
-
-
-
-
1
1
-
3
-
-
-
-
-
5
-
-
4
-
-
-
-
-
-
-
-
-
-
3
3
-
-
-
746085
Dutta
JMJ27, an Arabidopsis H3K9 hi ...
Arabidopsis thaliana
Plant J.
91
1015-1028
2017
-
-
1
-
1
-
-
-
1
1
-
2
-
3
-
-
-
-
-
4
-
-
5
-
1
-
1
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1
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1
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1
1
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2
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-
-
4
-
-
5
-
1
-
1
-
-
-
-
-
1
3
3
1
-
-
746217
Jang
Histone H3K9 demethylase JMJD ...
Homo sapiens
PLoS ONE
12
e0168185
2017
-
-
1
-
1
-
-
-
1
1
-
2
-
1
-
-
-
-
-
3
-
-
2
-
-
-
-
-
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-
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1
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1
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1
1
-
2
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3
-
-
2
-
-
-
-
-
-
-
-
-
-
4
4
-
-
-
744236
Choi
KDM7A histone demethylase med ...
Homo sapiens
Biochem. Biophys. Res. Commun.
478
1355-1362
2016
-
-
1
-
1
-
-
-
2
-
-
1
-
2
-
-
-
-
-
2
-
-
1
-
-
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1
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1
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2
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1
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-
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-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
2
2
-
-
-
744347
Burg
Lysine-specific demethylase 1 ...
Homo sapiens
Biochemistry
55
1652-1662
2016
-
-
-
-
-
-
3
-
1
-
-
3
-
1
-
-
-
-
-
-
-
-
4
1
1
-
-
-
1
-
-
1
3
-
1
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-
-
1
-
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-
1
3
3
-
1
-
-
3
-
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-
-
-
-
4
1
1
-
-
-
1
-
-
-
-
2
2
-
-
-
744722
Morera
4-biphenylalanine- and 3-phen ...
Homo sapiens
ChemMedChem
11
2063-2083
2016
1
-
1
-
-
-
33
1
1
1
-
3
-
2
-
-
1
1
-
2
-
-
5
-
1
-
-
-
1
-
-
-
-
-
30
1
-
1
-
-
-
-
30
33
-
1
1
1
-
3
-
-
-
1
-
2
-
-
5
-
1
-
-
-
1
-
-
-
-
2
2
-
-
-
744782
Pedanou
The histone H3K9 demethylase ...
Homo sapiens
eLife
5
e16844
2016
-
-
1
-
2
-
-
-
2
-
-
3
-
3
-
-
-
-
-
5
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
2
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-
2
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3
-
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-
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5
-
-
3
-
-
-
-
-
-
-
-
-
2
3
3
2
-
-
744785
Pedersen
Continual removal of H3K9 pro ...
Mus musculus, Mus musculus C57BL/6
EMBO J.
35
1550-1564
2016
-
-
1
-
1
-
-
-
2
-
-
10
-
5
-
-
-
-
-
1
-
-
10
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
3
-
-
-
-
-
4
-
-
10
-
-
-
-
-
3
-
-
10
-
-
-
-
-
-
-
-
-
2
3
9
3
-
-
745525
Bavetsias
8-Substituted pyrido[3,4-d]py ...
Homo sapiens
J. Med. Chem.
59
1388-1409
2016
-
-
1
1
1
-
64
-
1
1
-
2
-
2
-
-
1
-
-
2
-
-
3
-
1
-
-
-
1
-
-
-
-
-
-
-
-
1
-
1
1
-
-
123
-
-
2
2
-
2
-
-
-
1
-
4
-
-
3
-
2
-
-
-
2
-
-
-
-
-
-
-
-
-
745889
Yuan
KDM4C, a H3K9me3 histone deme ...
Homo sapiens
Neoplasia
18
594-609
2016
-
2
-
-
1
-
1
-
3
-
-
1
-
2
-
-
-
-
-
4
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
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2
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697546
Nottke
Developmental roles of the his ...
Arabidopsis thaliana, Caenorhabditis elegans, Drosophila melanogaster, Homo sapiens, Mus musculus, Saccharomyces cerevisiae, Schizosaccharomyces pombe
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10
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2
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2
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697557
Brasacchio
Hyperglycemia induces a dynami ...
Homo sapiens, Mus musculus
Diabetes
58
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2009
2
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Nicholson
LSD1 demethylates histone and ...
Mammalia
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698098
Lorbeck
The histone demethylase DmelKd ...
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H3K4 dimethylation in hepatoce ...
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The lysine demethylase LSD1 (K ...
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700397
Ciccone
KDM1B is a histone H3K4 demeth ...
Mus musculus
Nature
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LSD1-mediated epigenetic modif ...
Mus musculus
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701212
Lan
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Yang
Role of hypoxia-inducible fact ...
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Novel oligoamine analogues inh ...
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Mimasu
Crystal structure of histone d ...
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Hypoxia upregulates the histon ...
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Lloret-Llinares
Characterization of Drosophila ...
Drosophila melanogaster
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Zhu
Lysine-specific demethylase 1 ...
Homo sapiens
PLoS ONE
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Spedaletti
Characterization of a lysine-s ...
Arabidopsis thaliana
Biochemistry
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2008
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Role of the lysine-specific de ...
Mus musculus
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Lan
Mechanisms involved in the reg ...
Caenorhabditis elegans, Drosophila melanogaster, Mus musculus
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316-325
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3
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698105
Pasini
Coordinated regulation of tran ...
Mus musculus
Genes Dev.
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1345-1355
2008
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698354
Cui
Histone lysine methyltransfera ...
Plasmodium falciparum
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Chau
Cell cycle association of the ...
Homo sapiens
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Yokoyama
Transrepressive function of TL ...
Homo sapiens
Mol. Cell. Biol.
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Tsai
p53-targeted LSD1 functions in ...
Mus musculus
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Dey
The histone demethylase KDM5b/ ...
Mus musculus
Mol. Cell. Biol.
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Lopez-Bigas
Genome-wide analysis of the H3 ...
Homo sapiens
Mol. Cell
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Lee
Distinct binding modes specify ...
Homo sapiens
Nat. Struct. Mol. Biol.
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Opel
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Forneris
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