DGIdb - EZH2 Gene Record

EZH2 2146 Clinically Actionable

Alternate Names:

2146
ENHANCER OF ZESTE 2 POLYCOMB REPRESSIVE COMPLEX 2 SUBUNIT
EZH2
ENX-1
ENX1
EZH2b
KMT6
KMT6A
WVS
WVS2
601573
3527
ENSG00000106462
OTTHUMG00000158973
2654
Q15910
NP_004447
NM_004456
63
EZH1
Enhancer of zeste homolog 2
T25265
Histone-lysine N-methyltransferase EZH2
BE0009562

Gene Info:

Initial Gene Query	EZH2
Counted Citations from 1950-2000	276
GuideToPharmacology Gene Category Name	2.1.1.43 Histone methyltransferases (HMTs)
GuideToPharmacology Gene Category ID	871
Gene Biotype	PROTEIN_CODING

(12 More Sources)

Gene Categories: Category Details

TUMOR SUPPRESSOR
KINASE
SERINE THREONINE KINASE
HISTONE MODIFICATION
NUCLEAR HORMONE RECEPTOR
CLINICALLY ACTIONABLE
METHYL TRANSFERASE
ENZYME
TRANSCRIPTION FACTOR

Publications:

Knutson et al., 2014, Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma., Mol. Cancer Ther.
Qi et al., 2017, An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED., Nat. Chem. Biol.
Baker et al., 2015, Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors., Oncotarget
Ipsaro et al., 2017, Rapid generation of drug-resistance alleles at endogenous loci using CRISPR-Cas9 indel mutagenesis., PLoS ONE
Riquelme et al., 2016, Modulation of EZH2 Expression by MEK-ERK or PI3K-AKT Signaling in Lung Cancer Is Dictated by Different KRAS Oncogene Mutations., Cancer Res.
Vaswani RG et al., 2016, Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas., J Med Chem
Johnson et al., 2015, HDAC1,2 inhibition impairs EZH2- and BBAP-mediated DNA repair to overcome chemoresistance in EZH2 gain-of-function mutant diffuse large B-cell lymphoma., Oncotarget
Souroullas et al., 2016, An oncogenic Ezh2 mutation induces tumors through global redistribution of histone 3 lysine 27 trimethylation., Nat. Med.

TAZEMETOSTAT EZH2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

Knutson et al., 2014, Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma., Mol. Cancer Ther.

Qi et al., 2017, An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED., Nat. Chem. Biol.

Baker et al., 2015, Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors., Oncotarget

CPI-1205 EZH2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

Vaswani RG et al., 2016, Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas., J Med Chem

PF-06821497 EZH2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of enzyme function in a biochemical assay using the (activating) Y641N mutant form of EZH2.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:

MK-2206 EZH2

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Cell line xenograft

Indication/Tumor Type colon cancer

Indication/Tumor Type pancreatic cancer

Publications:

Riquelme et al., 2016, Modulation of EZH2 Expression by MEK-ERK or PI3K-AKT Signaling in Lung Cancer Is Dictated by Different KRAS Oncogene Mutations., Cancer Res.
SELUMETINIB EZH2

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy DZNep + Selumetinib

Indication/Tumor Type lung adenocarcinoma

Response Type sensitive

Publications:

Riquelme et al., 2016, Modulation of EZH2 Expression by MEK-ERK or PI3K-AKT Signaling in Lung Cancer Is Dictated by Different KRAS Oncogene Mutations., Cancer Res.
VORINOSTAT EZH2

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type diffuse large B-cell lymphoma

Response Type sensitive

Approval Status Preclinical

Publications:

Johnson et al., 2015, HDAC1,2 inhibition impairs EZH2- and BBAP-mediated DNA repair to overcome chemoresistance in EZH2 gain-of-function mutant diffuse large B-cell lymphoma., Oncotarget
DOXORUBICIN EZH2

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy ACY-957 + Doxorubicin

Indication/Tumor Type diffuse large B-cell lymphoma

Response Type sensitive

Publications:

Johnson et al., 2015, HDAC1,2 inhibition impairs EZH2- and BBAP-mediated DNA repair to overcome chemoresistance in EZH2 gain-of-function mutant diffuse large B-cell lymphoma., Oncotarget
DABRAFENIB EZH2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souroullas et al., 2016, An oncogenic Ezh2 mutation induces tumors through global redistribution of histone 3 lysine 27 trimethylation., Nat. Med.

Ensembl: ENSG00000106462
- Version: 101_38
Alternate Names:

EZH2 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
BaderLabGenes: EZH2
- Version: February-2014
Alternate Names:

2146 Entrez Gene ID

Gene Info:

Initial Gene Query EZH2

Counted Citations from 1950-2000 276

Gene Categories:

METHYL TRANSFERASE

Publications:
GuideToPharmacology: 2146
- Version: 29-September-2020
Alternate Names:

3527 HUGO Gene ID

3527 HUGO Gene Symbol

enhancer of zeste 2 polycomb repressive complex 2 subunit HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name 2.1.1.43 Histone methyltransferases (HMTs)

GuideToPharmacology Gene Category ID 871

Gene Categories:

ENZYME

Publications:

JAX-CKB: EZH2

Version: 27-September-2017

Alternate Names:

2146 CKB Entrez Id

EZH2 CKB Gene Synonym

ENX-1 CKB Gene Synonym

Gene Info:

Publications:

Riquelme et al., 2016, Modulation of EZH2 Expression by MEK-ERK or PI3K-AKT Signaling in Lung Cancer Is Dictated by Different KRAS Oncogene Mutations., Cancer Res.

Knutson et al., 2012, A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells., Nat. Chem. Biol.

Qi et al., 2017, An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED., Nat. Chem. Biol.

CIViC: EZH2
- Version: 14-September-2020
Alternate Names:

2146 Entrez Gene ID

63 CIViC Gene ID

Gene Info:

Publications:

Souroullas et al., 2016, An oncogenic Ezh2 mutation induces tumors through global redistribution of histone 3 lysine 27 trimethylation., Nat. Med.

DrugBank: BE0009562

Version: 5.1.7

Alternate Names:

EZH2 DrugBank Gene Name

Q15910 UniProt Accession

2146 Entrez Gene Id

Gene Info:

Publications:

Vaswani RG et al., 2016, Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas., J Med Chem

CGI: EZH2

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

Knutson et al., 2012, A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells., Nat. Chem. Biol.

Knutson et al., 2014, Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma., Mol. Cancer Ther.

OncoKB: EZH2
- Version: 23-July-2020
Alternate Names:

2146 OncoKB Entrez Id

ENX-1 OncoKB Gene Synonym

ENX1 OncoKB Gene Synonym

Gene Info:

Publications:
HumanProteinAtlas: EZH2
- Version: 19.3
Alternate Names:

ENSG00000106462 Ensembl Gene ID

ENX-1 Human Protein Atlas Gene Synonym

EZH1 Human Protein Atlas Gene Synonym

Gene Info:

Gene Categories:

ENZYME

Publications:
Pharos: EZH2
- Version: 03-September-2020
Alternate Names:

Histone-lysine N-methyltransferase EZH2 Gene Name

Q15910 UniProt ID

Gene Info:

Gene Categories:

TRANSCRIPTION FACTOR, NUCLEAR HORMONE RECEPTOR

Publications:
Tempus: EZH2
- Version: 11-November-2018
Alternate Names:

EZH2 Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
TTD: Enhancer of zeste homolog 2
- Version: 2020.06.01
Alternate Names:

EZH2 TTD Gene Abbreviation

T25265 TTD Target ID

Gene Info:

Publications:
MskImpact: EZH2
- Version: May-2015
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
FoundationOneGenes: EZH2
- Version: 03-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
CarisMolecularIntelligence: EZH2
- Version: 04-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
Oncomine: EZH2
- Version: v3
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Inhibition

Details of the Assay for Interaction	Inhibition of enzyme function in a biochemical assay using the (activating) Y641N mutant form of EZH2.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Approval Status	Preclinical - Cell line xenograft
Indication/Tumor Type	colon cancer
Indication/Tumor Type	pancreatic cancer

combination therapy	DZNep + Selumetinib
Indication/Tumor Type	lung adenocarcinoma
Response Type	sensitive

Indication/Tumor Type	diffuse large B-cell lymphoma
Response Type	sensitive
Approval Status	Preclinical

combination therapy	ACY-957 + Doxorubicin
Indication/Tumor Type	diffuse large B-cell lymphoma
Response Type	sensitive

3527	HUGO Gene ID
3527	HUGO Gene Symbol
enhancer of zeste 2 polycomb repressive complex 2 subunit	HUGO Gene Name

EZH2	DrugBank Gene Name
Q15910	UniProt Accession
2146	Entrez Gene Id

2146	OncoKB Entrez Id
ENX-1	OncoKB Gene Synonym
ENX1	OncoKB Gene Synonym

ENSG00000106462	Ensembl Gene ID
ENX-1	Human Protein Atlas Gene Synonym
EZH1	Human Protein Atlas Gene Synonym

Histone-lysine N-methyltransferase EZH2	Gene Name
Q15910	UniProt ID

EZH2 Gene Record

EZH2 2146 Clinically Actionable

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of enzyme function in a biochemical assay using the (activating) Y641N mutant form of EZH2. Specific Action of the Ligand Inhibition Endogenous Drug? False

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Approval Status Preclinical - Cell line xenograft Indication/Tumor Type colon cancer Indication/Tumor Type pancreatic cancer

Publications: Riquelme et al., 2016, Modulation of EZH2 Expression by MEK-ERK or PI3K-AKT Signaling in Lung Cancer Is Dictated by Different KRAS Oncogene Mutations., Cancer Res.

Interaction Types & Directionality: n/a

Interaction Info: combination therapy DZNep + Selumetinib Indication/Tumor Type lung adenocarcinoma Response Type sensitive

Publications: Riquelme et al., 2016, Modulation of EZH2 Expression by MEK-ERK or PI3K-AKT Signaling in Lung Cancer Is Dictated by Different KRAS Oncogene Mutations., Cancer Res.

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type diffuse large B-cell lymphoma Response Type sensitive Approval Status Preclinical

Publications: Johnson et al., 2015, HDAC1,2 inhibition impairs EZH2- and BBAP-mediated DNA repair to overcome chemoresistance in EZH2 gain-of-function mutant diffuse large B-cell lymphoma., Oncotarget

Interaction Types & Directionality: n/a

Interaction Info: combination therapy ACY-957 + Doxorubicin Indication/Tumor Type diffuse large B-cell lymphoma Response Type sensitive

Publications: Johnson et al., 2015, HDAC1,2 inhibition impairs EZH2- and BBAP-mediated DNA repair to overcome chemoresistance in EZH2 gain-of-function mutant diffuse large B-cell lymphoma., Oncotarget

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Souroullas et al., 2016, An oncogenic Ezh2 mutation induces tumors through global redistribution of histone 3 lysine 27 trimethylation., Nat. Med.

Ensembl: ENSG00000106462

Alternate Names: EZH2 Ensembl Gene Name

Gene Info: Gene Biotype PROTEIN_CODING

Publications:

BaderLabGenes: EZH2

Alternate Names: 2146 Entrez Gene ID

Gene Info: Initial Gene Query EZH2 Counted Citations from 1950-2000 276

Gene Categories: METHYL TRANSFERASE

Publications:

GuideToPharmacology: 2146

Alternate Names: 3527 HUGO Gene ID 3527 HUGO Gene Symbol enhancer of zeste 2 polycomb repressive complex 2 subunit HUGO Gene Name

Gene Info: GuideToPharmacology Gene Category Name 2.1.1.43 Histone methyltransferases (HMTs) GuideToPharmacology Gene Category ID 871

Gene Categories: ENZYME

Publications:

JAX-CKB: EZH2

Alternate Names: 2146 CKB Entrez Id EZH2 CKB Gene Synonym ENX-1 CKB Gene Synonym

Gene Info:

CIViC: EZH2

Alternate Names: 2146 Entrez Gene ID 63 CIViC Gene ID

Gene Info:

Publications: Souroullas et al., 2016, An oncogenic Ezh2 mutation induces tumors through global redistribution of histone 3 lysine 27 trimethylation., Nat. Med.

DrugBank: BE0009562

Alternate Names: EZH2 DrugBank Gene Name Q15910 UniProt Accession 2146 Entrez Gene Id

Gene Info:

CGI: EZH2

Alternate Names:

Gene Info:

Publications: Knutson et al., 2012, A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells., Nat. Chem. Biol. Knutson et al., 2014, Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma., Mol. Cancer Ther.

OncoKB: EZH2

Alternate Names: 2146 OncoKB Entrez Id ENX-1 OncoKB Gene Synonym ENX1 OncoKB Gene Synonym

Gene Info:

Publications:

HumanProteinAtlas: EZH2

Alternate Names: ENSG00000106462 Ensembl Gene ID ENX-1 Human Protein Atlas Gene Synonym EZH1 Human Protein Atlas Gene Synonym

Gene Info:

Gene Categories: ENZYME

Publications:

Pharos: EZH2

Alternate Names: Histone-lysine N-methyltransferase EZH2 Gene Name Q15910 UniProt ID

Gene Info:

Gene Categories: TRANSCRIPTION FACTOR, NUCLEAR HORMONE RECEPTOR

Publications:

Tempus: EZH2

Alternate Names: EZH2 Gene Symbol

Gene Info:

Gene Categories: CLINICALLY ACTIONABLE

Publications:

TTD: Enhancer of zeste homolog 2

Alternate Names: EZH2 TTD Gene Abbreviation T25265 TTD Target ID

Gene Info:

Publications:

MskImpact: EZH2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of enzyme function in a biochemical assay using the (activating) Y641N mutant form of EZH2.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Cell line xenograft

Indication/Tumor Type colon cancer

Indication/Tumor Type pancreatic cancer

Publications:

Riquelme et al., 2016, Modulation of EZH2 Expression by MEK-ERK or PI3K-AKT Signaling in Lung Cancer Is Dictated by Different KRAS Oncogene Mutations., Cancer Res.

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy DZNep + Selumetinib

Indication/Tumor Type lung adenocarcinoma

Response Type sensitive

Publications:

Riquelme et al., 2016, Modulation of EZH2 Expression by MEK-ERK or PI3K-AKT Signaling in Lung Cancer Is Dictated by Different KRAS Oncogene Mutations., Cancer Res.

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type diffuse large B-cell lymphoma

Response Type sensitive

Approval Status Preclinical

Publications:

Johnson et al., 2015, HDAC1,2 inhibition impairs EZH2- and BBAP-mediated DNA repair to overcome chemoresistance in EZH2 gain-of-function mutant diffuse large B-cell lymphoma., Oncotarget

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy ACY-957 + Doxorubicin

Indication/Tumor Type diffuse large B-cell lymphoma

Response Type sensitive

Publications:

Johnson et al., 2015, HDAC1,2 inhibition impairs EZH2- and BBAP-mediated DNA repair to overcome chemoresistance in EZH2 gain-of-function mutant diffuse large B-cell lymphoma., Oncotarget

Interaction Types & Directionality:

n/a

Publications:

Souroullas et al., 2016, An oncogenic Ezh2 mutation induces tumors through global redistribution of histone 3 lysine 27 trimethylation., Nat. Med.

Alternate Names:

EZH2 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Alternate Names:

2146 Entrez Gene ID

Gene Info:

Initial Gene Query EZH2

Counted Citations from 1950-2000 276

Gene Categories:

METHYL TRANSFERASE

Alternate Names:

3527 HUGO Gene ID

3527 HUGO Gene Symbol

enhancer of zeste 2 polycomb repressive complex 2 subunit HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name 2.1.1.43 Histone methyltransferases (HMTs)

GuideToPharmacology Gene Category ID 871

Gene Categories:

ENZYME

Alternate Names:

2146 CKB Entrez Id

EZH2 CKB Gene Synonym

ENX-1 CKB Gene Synonym

Alternate Names:

2146 Entrez Gene ID

63 CIViC Gene ID

Publications:

Souroullas et al., 2016, An oncogenic Ezh2 mutation induces tumors through global redistribution of histone 3 lysine 27 trimethylation., Nat. Med.

Alternate Names:

EZH2 DrugBank Gene Name

Q15910 UniProt Accession

2146 Entrez Gene Id

Publications:

Knutson et al., 2012, A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells., Nat. Chem. Biol.

Knutson et al., 2014, Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma., Mol. Cancer Ther.

Alternate Names:

2146 OncoKB Entrez Id

ENX-1 OncoKB Gene Synonym

ENX1 OncoKB Gene Synonym

Alternate Names:

ENSG00000106462 Ensembl Gene ID

ENX-1 Human Protein Atlas Gene Synonym

EZH1 Human Protein Atlas Gene Synonym

Gene Categories:

ENZYME

Alternate Names:

Histone-lysine N-methyltransferase EZH2 Gene Name

Q15910 UniProt ID

Gene Categories:

TRANSCRIPTION FACTOR, NUCLEAR HORMONE RECEPTOR

Alternate Names:

EZH2 Gene Symbol

Gene Categories:

CLINICALLY ACTIONABLE

Alternate Names:

EZH2 TTD Gene Abbreviation

T25265 TTD Target ID

Gene Categories:

CLINICALLY ACTIONABLE

Gene Categories:

CLINICALLY ACTIONABLE

Gene Categories:

CLINICALLY ACTIONABLE

Gene Categories:

CLINICALLY ACTIONABLE