DNA methyltransferase 1

Target id: 2605

Nomenclature: DNA methyltransferase 1

Family: 2.1.1.- Methyltransferases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for DNA methyltransferase 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1632 19p13.2 DNMT1 DNA methyltransferase 1
Mouse - 1620 9 A3 Dnmt1 DNA methyltransferase (cytosine-5) 1
Rat - 1622 8q13 Dnmt1 DNA methyltransferase 1
Previous and Unofficial Names
CXXC9 | MCMT | DNA (cytosine-5-)-methyltransferase 1
Database Links
BRENDA
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.1.1.37

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
bromo-deaza-SAH Hs Inhibition 6.0 pKi 2
pKi 6.0 (Ki 9.5x10-7 M) [2]
SGI-1027 Hs Inhibition 6.1 pIC50 1
pIC50 6.1 (IC50 8.5x10-7 M) [1]
Description: Value derived from a nanoscale HTS assay.
Inhibitor Comments
Azacitidine and decitabine are likely to be inhibitors of DNMT1 and DNMT3A. We infer primary target designation from reports of drug action in in vitro and in vivo studies despite the paucity of pharmacological affinity data.
Clinically-Relevant Mutations and Pathophysiology
Disease:  Cerebellar ataxia, deafness, and narcolepsy, autosomal dominant; ADCADN
OMIM: 604121
Orphanet: ORPHA314404
Disease:  Neuropathy, hereditary sensory, type IE; HSN1E
Disease Ontology: DOID:0050548
OMIM: 614116

References

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1. Valente S, Liu Y, Schnekenburger M, Zwergel C, Cosconati S, Gros C, Tardugno M, Labella D, Florean C, Minden S et al.. (2014) Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells. J. Med. Chem.57 (3): 701-13. [PMID:24387159]

2. Yu W, Smil D, Li F, Tempel W, Fedorov O, Nguyen KT, Bolshan Y, Al-Awar R, Knapp S, Arrowsmith CH et al.. (2013) Bromo-deaza-SAH: a potent and selective DOT1L inhibitor. Bioorg. Med. Chem.21 (7): 1787-94. [PMID:23433670]

How to cite this page

2.1.1.- Methyltransferases: DNA methyltransferase 1. Last modified on 22/10/2015. Accessed on 11/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2605.