Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T92308
|
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| Former ID |
TTDS00312
|
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| Target Name |
DNA (cytosine-5)-methyltransferase
|
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| Synonyms |
DNA MTase; DNA methyltransferase; M.EcoDcm
|
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| Target Type |
Successful
|
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| Disease | Cancer [ICD9: 140-229; ICD10: C00-C96] | ||||
| Myelodysplastic syndrome [ICD9: 238.7; ICD10: D46] | |||||
| Function |
This methylase recognizes the double-stranded sequence ccwgg, causes specific methylation on c-2 on both strands.
|
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| BioChemical Class |
Methyltransferase superfamily
|
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| Target Validation |
T92308
|
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| EC Number |
EC 2.1.1.73
|
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| Drugs and Mode of Action | |||||
| Drug(s) | Azacitidine | Drug Info | Approved | Myelodysplastic syndrome | [1], [2] |
| Curcumin | Drug Info | Phase 3 | Cancer | [3], [4] | |
| Inhibitor | (L-)-S-adenosyl-L-homocysteine | Drug Info | [5] | ||
| Azacitidine | Drug Info | [1] | |||
| Curcumin | Drug Info | [6] | |||
| NSC-106084 | Drug Info | [6] | |||
| NSC-137546 | Drug Info | [6] | |||
| NSC-138419 | Drug Info | [6] | |||
| NSC-154957 | Drug Info | [6] | |||
| NSC-158324 | Drug Info | [6] | |||
| NSC-319745 | Drug Info | [6] | |||
| NSC-345763 | Drug Info | [6] | |||
| NSC-348926 | Drug Info | [6] | |||
| NSC-401077 | Drug Info | [6] | |||
| NSC-54162 | Drug Info | [6] | |||
| NSC-56071 | Drug Info | [6] | |||
| NSC-57893 | Drug Info | [6] | |||
| NSC-622444 | Drug Info | [6] | |||
| NSC-622445 | Drug Info | [6] | |||
| NSC-623548 | Drug Info | [6] | |||
| S-Adenosylhomocysteine | Drug Info | [6] | |||
| S-tubercidinylhomocysteine | Drug Info | [7] | |||
| References | |||||
| REF 1 | The DNA methyltransferase inhibitors azacitidine, decitabine and zebularine exert differential effects on cancer gene expression in acute myeloid leukemia cells. Leukemia. 2009 Jun;23(6):1019-28. Epub 2009 Feb 5. | ||||
| REF 2 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6796). | ||||
| REF 3 | Nanocurcumin: a promising therapeutic advancement over native curcumin. Crit Rev Ther Drug Carrier Syst. 2013;30(4):331-68. | ||||
| REF 4 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7000). | ||||
| REF 5 | Bioorg Med Chem Lett. 2009 May 15;19(10):2742-6. Epub 2009 Mar 28.Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors. | ||||
| REF 6 | Bioorg Med Chem. 2010 Jan 15;18(2):822-9. Epub 2009 Nov 27.Novel and selective DNA methyltransferase inhibitors: Docking-based virtual screening and experimental evaluation. | ||||
| REF 7 | Bioorg Med Chem Lett. 2009 May 15;19(10):2747-51. Epub 2009 Mar 28.SAR around (l)-S-adenosyl-l-homocysteine, an inhibitor of human DNA methyltransferase (DNMT) enzymes. | ||||
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