DGIdb - DNMT1 Gene Record

DNMT1 1786 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

1786
DNA METHYLTRANSFERASE 1
DNMT1
ADCADN
AIM
CXXC9
DNMT
HSN1E
MCMT
m.HsaI
126375
2976
ENSG00000130816
OTTHUMG00000180397
2605
P26358
DNMT1_HUMAN
DNA (cytosine-5)-methyltransferase 1
CXXC-type zinc finger protein 9
DNA methyltransferase HsaI
DNA MTase HsaI
1510
DNA [cytosine-5]-methyltransferase
T92308
DNA [cytosine-5]-methyltransferase 1
T88304
NP_001124295
NM_001130823

Gene Info:

Target Main Class	Enzymes
Target Subclass	2.1.1.37
Target Class	Enzymes
Target Subclass	EC:2.1.1.37
Gene Biotype	PROTEIN_CODING
GuideToPharmacology Gene Category Name	2.1.1.- Methyltransferases
GuideToPharmacology Gene Category ID	843

(9 More Sources)

Gene Categories: Category Details

DRUG RESISTANCE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE
ENZYME

Publications:

Liu Z et al., 2009, Curcumin is a potent DNA hypomethylation agent., Bioorg Med Chem Lett
Ghoshal et al., 2005, 5-Aza-deoxycytidine induces selective degradation of DNA methyltransferase 1 by a proteasomal pathway that requires the KEN box, bromo-adjacent homology domain, and nuclear localization signal., Mol. Cell. Biol.
Fenaux, 2005, Inhibitors of DNA methylation: beyond myelodysplastic syndromes., Nat Clin Pract Oncol
Kaminskas et al., 2005, FDA drug approval summary: azacitidine (5-azacytidine, Vidaza) for injectable suspension., Oncologist
Ghoshal et al., 2007, DNA methyltransferases as targets for cancer therapy., Drugs Today
Leone et al., 2003, Inhibitors of DNA methylation in the treatment of hematological malignancies and MDS., Clin. Immunol.
Silverman et al., 2002, Randomized controlled trial of azacitidine in patients with the myelodysplastic syndrome: a study of the cancer and leukemia group B., J. Clin. Oncol.
Hollenbach et al., 2010, A comparison of azacitidine and decitabine activities in acute myeloid leukemia cell lines., PLoS ONE
Silverman, 2001, Targeting hypomethylation of DNA to achieve cellular differentiation in myelodysplastic syndromes (MDS)., Oncologist
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Glover et al., 1987, Biochemistry of azacitidine: a review., Cancer Treat Rep
O'Dwyer et al., 2008, Azacitidine and the beginnings of therapeutic epigenetic modulation., Expert Opin Pharmacother
Cataldo et al., 2009, Azacitidine for the treatment of myelodysplastic syndrome., Expert Rev Anticancer Ther
Creusot et al., 1982, Inhibition of DNA methyltransferase and induction of Friend erythroleukemia cell differentiation by 5-azacytidine and 5-aza-2'-deoxycytidine., J. Biol. Chem.
Segura-Pacheco et al., 2006, Global DNA hypermethylation-associated cancer chemotherapy resistance and its reversion with the demethylating agent hydralazine., J Transl Med
Sheikh KD et al., 2010, Fluorescent epigenetic small molecule induces expression of the tumor suppressor ras-association domain family 1A and inhibits human prostate xenograft., J Med Chem
Saba et al., 2005, Decitabine in myelodysplastic syndromes., Semin. Hematol.
Daskalakis et al., 2010, Decitabine., Recent Results Cancer Res.
Ando et al., 2000, Decitabine (5-Aza-2'-deoxycytidine) decreased DNA methylation and expression of MDR-1 gene in K562/ADM cells., Leukemia
Saunthararajah et al., 2003, Effects of 5-aza-2'-deoxycytidine on fetal hemoglobin levels, red cell adhesion, and hematopoietic differentiation in patients with sickle cell disease., Blood
Jabbour et al., 2008, Evolution of decitabine development: accomplishments, ongoing investigations, and future strategies., Cancer
Karpf et al., 2001, Activation of the p53 DNA damage response pathway after inhibition of DNA methyltransferase by 5-aza-2'-deoxycytidine., Mol. Pharmacol.
Stresemann et al., 2008, Modes of action of the DNA methyltransferase inhibitors azacytidine and decitabine., Int. J. Cancer
Csankovszki et al., 2001, Synergism of Xist RNA, DNA methylation, and histone hypoacetylation in maintaining X chromosome inactivation., J. Cell Biol.
Oki et al., 2007, Decitabine--bedside to bench., Crit. Rev. Oncol. Hematol.
Takebayashi et al., 2001, 5-Aza-2'-deoxycytidine induces histone hyperacetylation of mouse centromeric heterochromatin by a mechanism independent of DNA demethylation., Biochem. Biophys. Res. Commun.
Stewart et al., 2015, KRAS Genomic Status Predicts the Sensitivity of Ovarian Cancer Cells to Decitabine., Cancer Res.
Plitta B et al., 2012, New cytosine derivatives as inhibitors of DNA methylation., Eur J Med Chem
Wu et al., 2006, [Effect of environmental contaminants on DNA methyltransferase activity of mouse preimplantation embryos]., Wei Sheng Yan Jiu
Sasaki et al., 1986, Effect of 5-azacytidine on the differentiation of human leukemia K-562 cells., Int. J. Cell Cloning
Mutze et al., 2011, DNA methyltransferase 1 as a predictive biomarker and potential therapeutic target for chemotherapy in gastric cancer., Eur. J. Cancer
Parker et al., Mitoxantrone mediates demethylation and reexpression of cyclin d2, estrogen receptor and 14.3.3sigma in breast cancer cells., Cancer Biol. Ther.
Herranz et al., 2006, The novel DNA methylation inhibitor zebularine is effective against the development of murine T-cell lymphoma., Blood

ZEBULARINE DNMT1

Interaction Score: 4.73

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16239434

Sources:
NCI
HEXAHYDROCURCUMIN DNMT1

Interaction Score: 4.73

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19112019

Sources:
DTC
CHEMBL2063052 DNMT1

Interaction Score: 4.73

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22854677

Sources:
DTC
MAHANINE DNMT1

Interaction Score: 4.73

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20184324

Sources:
DTC
TETRAHYDROCURCUMIN DNMT1

Interaction Score: 4.73

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19112019

Sources:
DTC
DECITABINE DNMT1

Interaction Score: 3.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction DNA (cytosine-5)-methyltransferase 1 inhibitor

Direct Interaction yes

Trial Name Dacogen/decitabine

PMIDs:
16015501 20072836 11069027 12907443 18398832 11259619 18425818 11352938 17023173 11752352 11688997 25968887

Sources:
TdgClinicalTrial ChemblInteractions TEND CIViC
ANTROQUINONOL DNMT1

Interaction Score: 2.36

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
GUADECITABINE DNMT1

Interaction Score: 2.36

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PALIFOSFAMIDE DNMT1

Interaction Score: 2.36

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
FLUOROCYCLOPENTENYLCYTOSINE DNMT1

Interaction Score: 2.36

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
BISDEMETHOXYCURCUMIN DNMT1

Interaction Score: 1.58

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19112019

Sources:
DTC
BENZANTHRONE DNMT1

Interaction Score: 1.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
AZACITIDINE DNMT1

Interaction Score: 1.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name azacitidine,Vidaza

Novel drug target Established target

Mechanism of Interaction DNA (cytosine-5)-methyltransferase 1 inhibitor

PMIDs:
16341239 15793220 17612710 14585280 12011120 20126405 11700387 11752352 2443243 18627335 19589026 6173384

Sources:
TdgClinicalTrial ChemblInteractions NCI TEND TTD
DEMETHOXYCURCUMIN DNMT1

Interaction Score: 0.79

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19112019

Sources:
DTC
IFOSFAMIDE DNMT1

Interaction Score: 0.53

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
CHEMBL580076 DNMT1

Interaction Score: 0.39

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DAPHNORIN DNMT1

Interaction Score: 0.34

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
HYDROXYUREA DNMT1

Interaction Score: 0.34

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2422298

Sources:
NCI
CHEMBL1490332 DNMT1

Interaction Score: 0.34

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
FLOXURIDINE DNMT1

Interaction Score: 0.34

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15899874

Sources:
NCI
ADRIAMYCIN DNMT1

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16893460

Sources:
NCI
CEPHALOTHIN DNMT1

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL599013 DNMT1

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DIETHYLSTILBESTROL DNMT1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16598927

Sources:
NCI
MITOXANTRONE DNMT1

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12878861

Sources:
NCI
CURCUMIN DNMT1

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19112019

Sources:
DTC TTD
CISPLATIN DNMT1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21458988

Sources:
CIViC

Ensembl: ENSG00000130816
- Version: 101_38
Alternate Names:

DNMT1 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: P26358
- Version: 01-August-2011
Alternate Names:

P26358 Uniprot Accession

DNMT1 Gene Symbol

1786 Entrez Gene Id

Gene Info:

Target Main Class Enzymes

Target Subclass 2.1.1.37

Publications:
TdgClinicalTrial: P26358
- Version: January-2014
Alternate Names:

DNMT1 Gene Symbol

Gene Info:

Target Class Enzymes

Target Subclass EC:2.1.1.37

Publications:
GuideToPharmacology: 1786
- Version: 29-September-2020
Alternate Names:

2976 HUGO Gene ID

2976 HUGO Gene Symbol

DNA methyltransferase 1 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name 2.1.1.- Methyltransferases

GuideToPharmacology Gene Category ID 843

Gene Categories:

ENZYME

Publications:

CIViC: DNMT1

Version: 14-September-2020

Alternate Names:

1786 Entrez Gene ID

1510 CIViC Gene ID

Gene Info:

Gene Categories:

DRUG RESISTANCE

Publications:

Stewart et al., 2015, KRAS Genomic Status Predicts the Sensitivity of Ovarian Cancer Cells to Decitabine., Cancer Res.

Mutze et al., 2011, DNA methyltransferase 1 as a predictive biomarker and potential therapeutic target for chemotherapy in gastric cancer., Eur. J. Cancer

NCI: DNMT1

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Ghoshal et al., 2005, 5-Aza-deoxycytidine induces selective degradation of DNA methyltransferase 1 by a proteasomal pathway that requires the KEN box, bromo-adjacent homology domain, and nuclear localization signal., Mol. Cell. Biol.

Segura-Pacheco et al., 2006, Global DNA hypermethylation-associated cancer chemotherapy resistance and its reversion with the demethylating agent hydralazine., J Transl Med

Alcock et al., 2002, Farnesyltransferase inhibitor (L-744,832) restores TGF-beta type II receptor expression and enhances radiation sensitivity in K-ras mutant pancreatic cancer cell line MIA PaCa-2., Oncogene

DTC: DNMT1

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Liu Z et al., 2009, Curcumin is a potent DNA hypomethylation agent., Bioorg Med Chem Lett

Sheikh KD et al., 2010, Fluorescent epigenetic small molecule induces expression of the tumor suppressor ras-association domain family 1A and inhibits human prostate xenograft., J Med Chem

Plitta B et al., 2012, New cytosine derivatives as inhibitors of DNA methylation., Eur J Med Chem

HingoraniCasas: ENSG00000130816
- Version: 31-May-2017
Alternate Names:

ENSG00000130816 Gene Symbol

DNMT1 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: AIM
- Version: chembl_23
Alternate Names:

CXXC9 GENE_SYMBOL

DNMT GENE_SYMBOL

DNMT1 GENE_SYMBOL

Gene Info:

Publications:
TTD: DNA [cytosine-5]-methyltransferase
- Version: 2020.06.01
Alternate Names:

DNMT TTD Gene Abbreviation

T92308 TTD Target ID

Gene Info:

Publications:
TTD: DNA [cytosine-5]-methyltransferase 1
- Version: 2020.06.01
Alternate Names:

DNMT1 TTD Gene Abbreviation

T88304 TTD Target ID

Gene Info:

Publications:
Pharos: DNMT1
- Version: 01-May-2021
Alternate Names:

DNA (cytosine-5)-methyltransferase 1 Gene Name

P26358 UniProt ID

Gene Info:

Gene Categories:

ENZYME

Publications:
MskImpact: DNMT1
- Version: May-2015
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:

Mechanism of Interaction	DNA (cytosine-5)-methyltransferase 1 inhibitor
Direct Interaction	yes
Trial Name	Dacogen/decitabine

Trial Name	azacitidine,Vidaza
Novel drug target	Established target
Mechanism of Interaction	DNA (cytosine-5)-methyltransferase 1 inhibitor

2976	HUGO Gene ID
2976	HUGO Gene Symbol
DNA methyltransferase 1	HUGO Gene Name

DNA (cytosine-5)-methyltransferase 1	Gene Name
P26358	UniProt ID

DNMT1 Gene Record

DNMT1 1786 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16239434

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19112019

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22854677

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20184324

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19112019

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction DNA (cytosine-5)-methyltransferase 1 inhibitor Direct Interaction yes Trial Name Dacogen/decitabine

PMIDs: 16015501 20072836 11069027 12907443 18398832 11259619 18425818 11352938 17023173 11752352 11688997 25968887

Sources: TdgClinicalTrial ChemblInteractions TEND CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19112019

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name azacitidine,Vidaza Novel drug target Established target Mechanism of Interaction DNA (cytosine-5)-methyltransferase 1 inhibitor

PMIDs: 16341239 15793220 17612710 14585280 12011120 20126405 11700387 11752352 2443243 18627335 19589026 6173384

Sources: TdgClinicalTrial ChemblInteractions NCI TEND TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19112019

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: None found

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 2422298

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

n/a

PMIDs:
16239434

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
19112019

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22854677

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20184324

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
19112019

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction DNA (cytosine-5)-methyltransferase 1 inhibitor

Direct Interaction yes

Trial Name Dacogen/decitabine

PMIDs:
16015501 20072836 11069027 12907443 18398832 11259619 18425818 11352938 17023173 11752352 11688997 25968887

Sources:
TdgClinicalTrial ChemblInteractions TEND CIViC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
19112019

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name azacitidine,Vidaza

Novel drug target Established target

Mechanism of Interaction DNA (cytosine-5)-methyltransferase 1 inhibitor

PMIDs:
16341239 15793220 17612710 14585280 12011120 20126405 11700387 11752352 2443243 18627335 19589026 6173384

Sources:
TdgClinicalTrial ChemblInteractions NCI TEND TTD

Interaction Types & Directionality:

n/a

PMIDs:
19112019

Sources:
DTC

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
2422298

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
15899874

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
16893460

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
16598927

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
12878861

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
19112019