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Gene and Protein Information  |
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| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | - | 1616 | 19p13.2 | DNMT1 | DNA methyltransferase 1 | |
| Mouse | - | 1620 | 9 7.66 cM | Dnmt1 | DNA methyltransferase 1 | |
| Rat | - | 1622 | 8q13 | Dnmt1 | DNA methyltransferase 1 | |
| Previous and Unofficial Names |
| CXXC9 | MCMT | DNA (cytosine-5-)-methyltransferase 1 | DNA methyltransferase (cytosine-5) 1 |
| Database Links |
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| Alphafold | P26358 (Hs), P13864 (Mm), Q9Z330 (Rn) |
| BRENDA | 2.1.1.37 |
| ChEMBL Target | CHEMBL1993 (Hs), CHEMBL3351195 (Mm) |
| DrugBank Target | P26358 (Hs) |
| Ensembl Gene | ENSG00000130816 (Hs), ENSMUSG00000004099 (Mm), ENSRNOG00000039859 (Rn) |
| Entrez Gene | 1786 (Hs), 13433 (Mm), 84350 (Rn) |
| Human Protein Atlas | ENSG00000130816 (Hs) |
| KEGG Enzyme | 2.1.1.37 |
| KEGG Gene | hsa:1786 (Hs), mmu:13433 (Mm), rno:84350 (Rn) |
| OMIM | 126375 (Hs) |
| Orphanet | ORPHA270026 (Hs) |
| Pharos | P26358 (Hs) |
| RefSeq Nucleotide | NM_001130823 (Hs), NM_001199431 (Mm), NM_053354 (Rn) |
| RefSeq Protein | NP_001124295 (Hs), NP_001186360 (Mm), NP_445806 (Rn) |
| UniProtKB | P26358 (Hs), P13864 (Mm), Q9Z330 (Rn) |
| Wikipedia | DNMT1 (Hs) |
| Enzyme Reaction |
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Download all structure-activity data for this target as a CSV file 
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| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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
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| General Comments |
| Based on in vitro analysis, DNMT1 is proposed to bind the ORF8 protein of the SARS-CoV-2 virus [1], although the relevance of this interaction is unclear. |
1. Gordon DE, Jang GM, Bouhaddou M, Xu J, Obernier K, White KM, O'Meara MJ, Rezelj VV, Guo JZ, Swaney DL et al.. (2020) A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. Nature, 583 (7816): 459-468. [PMID:32353859]
2. Pappalardi MB, Keenan K, Cockerill M, Kellner WA, Stowell A, Sherk C, Wong K, Pathuri S, Briand J,Steidel M et al.. (2021) Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia. Nature Cancer, [Epub ahead of print]. DOI: 10.1038/s43018-021-00249-x
3. San José-Enériz E, Agirre X, Rabal O, Vilas-Zornoza A, Sanchez-Arias JA, Miranda E, Ugarte A, Roa S, Paiva B, Estella-Hermoso de Mendoza A et al.. (2017) Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies. Nat Commun, 8: 15424. [PMID:28548080]
4. 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]
5. 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]
2.1.1.- Methyltransferases: DNA methyltransferase 1. Last modified on 26/03/2024. Accessed on 13/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2605.
