Therapeutic Targets Database
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TTD Target ID: TTDS00312

Target Information
NameDNA (cytosine-5)-methyltransferase    
Type of targetSuccessful target    
SynonymsDNA MTase    
DNA methyltransferase    
M.EcoDcm    
DiseaseHepatocellular carcinoma
[ICD9: 155   ICD10: C22.0]
[1]
Leukemia, unspecified
[ICD9: 208.9   ICD10: C91-C95]
[2]
Solid tumor
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[2]
Drug(s)AzacitidineApprovedMyelodysplastic syndrome[3]
DecitabineApprovedMyelodysplastic syndrome[4][5][2]
EC NumberEC 2.1.1.37
EC 2.1.1.73
UniProt IDP11876
FunctionThis methylase recognizes the double-stranded sequence ccwgg, causes specific methylation on c-2 on both strands.    
SequenceMQENISVTDSYSTGNAAQAMLEKLLQIYDVKTLVAQLNGVGENHWSAAILKRALANDSAW HRLSEKEFAHLQTLLPKPPAHHPHYAFRFIDLFAGIGGIRRGFESIGGQCVFTSEWNKHA VRTYKANHYCDPATHHFNEDIRDITLSHKEGVSDEAAAEHIRQHIPEHDVLLAGFPCQPF SLAGVSKKNSLGRAHGFACDTQGTLFFDVVRIIDARRPAMFVLENVKNLKSHDQGKTFRI IMQTLDELGYDVADAEDNGPDDPKIIDGKHFLPQHRERIVLVGFRRDLNLKADFTLRDIS ECFPAQRVTLAQLLDPMVEAKYILTPVLWKYLYRYAKKHQARGNGFGYGMVYPNNPQSVT RTLSARYYKDGAEILIDRGWDMATGEKDFDDPLNQQHRPRRLTPRECARLMGFEAPGEAK FRIPVSDTQAYRQFGNSVVVPVFAAVAKLLEPKIKQAVALRQQEAQHGRRSR
Target ValidationClick to Find Target Validation Information.    
Inhibitor (L-)-S-adenosyl-L-homocysteine[6]
Azacitidine[3]
CURCUMIN[7]
Decitabine[4][5][2]
NSC-106084[7]
NSC-137546[7]
NSC-138419[7]
NSC-154957[7]
NSC-158324[7]
NSC-319745[7]
NSC-345763[7]
NSC-348926[7]
NSC-401077[7]
NSC-54162[7]
NSC-56071[7]
NSC-57893[7]
NSC-622444[7]
NSC-622445[7]
NSC-623548[7]
S-Adenosylhomocysteine[7]
S-tubercidinylhomocysteine[8]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Increased DNA methyltransferase expression is associated with an early stage of human hepatocarcinogenesis. Jpn J Cancer Res. 1997 Dec;88(12):1165-70. To Reference
Ref 2Activation of the p53 DNA damage response pathway after inhibition of DNA methyltransferase by 5-aza-2'-deoxycytidine. Mol Pharmacol. 2001 Apr;59(4):751-7. To Reference
Ref 3The 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. To Reference
Ref 4Decitabine improves patient outcomes in myelodysplastic syndromes: results of a phase III randomized study. Cancer. 2006 Apr 15;106(8):1794-803. To Reference
Ref 5Results of decitabine (5-aza-2'deoxycytidine) therapy in 130 patients with chronic myelogenous leukemia. Cancer. 2003 Aug 1;98(3):522-8. To Reference
Ref 6Bioorg 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. To Reference
Ref 7Bioorg 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. To Reference
Ref 8Bioorg 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. To Reference



 

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