Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T65501
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| Former ID |
TTDR01100
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| Target Name |
DNA (cytosine-5)-methyltransferase 3B
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| Gene Name |
DNMT3B
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| Synonyms |
DNA MTase HsaIIIB; DNA methyltransferase 3B; DNA methyltransferase HsaIIIB; Dnmt3b; M.HsaIIIB; DNMT3B
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| Target Type |
Clinical Trial
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| Disease | Cancer [ICD9: 140-229; ICD10: C00-C96] | ||||
| Function |
Required for genome wide de novo methylation and is essential for development. Isoforms 4 and 5 are probably not functional due to the deletion of two conserved methyltransferase motifs.
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| BioChemical Class |
Methyltransferase superfamily
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| Target Validation |
T65501
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| UniProt ID | |||||
| EC Number |
EC 2.1.1.37
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| Sequence |
MKGDTRHLNGEEDAGGREDSILVNGACSDQSSDSPPILEAIRTPEIRGRRSSSRLSKREV
SSLLSYTQDLTGDGDGEDGDGSDTPVMPKLFRETRTRSESPAVRTRNNNSVSSRERHRPS PRSTRGRQGRNHVDESPVEFPATRSLRRRATASAGTPWPSPPSSYLTIDLTDDTEDTHGT PQSSSTPYARLAQDSQQGGMESPQVEADSGDGDSSEYQDGKEFGIGDLVWGKIKGFSWWP AMVVSWKATSKRQAMSGMRWVQWFGDGKFSEVSADKLVALGLFSQHFNLATFNKLVSYRK AMYHALEKARVRAGKTFPSSPGDSLEDQLKPMLEWAHGGFKPTGIEGLKPNNTQPVVNKS KVRRAGSRKLESRKYENKTRRRTADDSATSDYCPAPKRLKTNCYNNGKDRGDEDQSREQM ASDVANNKSSLEDGCLSCGRKNPVSFHPLFEGGLCQTCRDRFLELFYMYDDDGYQSYCTV CCEGRELLLCSNTSCCRCFCVECLEVLVGTGTAAEAKLQEPWSCYMCLPQRCHGVLRRRK DWNVRLQAFFTSDTGLEYEAPKLYPAIPAARRRPIRVLSLFDGIATGYLVLKELGIKVGK YVASEVCEESIAVGTVKHEGNIKYVNDVRNITKKNIEEWGPFDLVIGGSPCNDLSNVNPA RKGLYEGTGRLFFEFYHLLNYSRPKEGDDRPFFWMFENVVAMKVGDKRDISRFLECNPVM IDAIKVSAAHRARYFWGNLPGMNRPVIASKNDKLELQDCLEYNRIAKLKKVQTITTKSNS IKQGKNQLFPVVMNGKEDVLWCTELERIFGFPVHYTDVSNMGRGARQKLLGRSWSVPVIR HLFAPLKDYFACE |
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| Drugs and Mode of Action | |||||
| Drug(s) | Curcumin | Drug Info | Phase 3 | Cancer | [1], [2] |
| Inhibitor | (L-)-S-adenosyl-L-homocysteine | Drug Info | [3] | ||
| Curcumin | Drug Info | [4] | |||
| NSC-106084 | Drug Info | [4] | |||
| NSC-137546 | Drug Info | [4] | |||
| NSC-138419 | Drug Info | [4] | |||
| NSC-154957 | Drug Info | [4] | |||
| NSC-158324 | Drug Info | [4] | |||
| NSC-319745 | Drug Info | [4] | |||
| NSC-345763 | Drug Info | [4] | |||
| NSC-348926 | Drug Info | [4] | |||
| NSC-401077 | Drug Info | [4] | |||
| NSC-54162 | Drug Info | [4] | |||
| NSC-56071 | Drug Info | [4] | |||
| NSC-57893 | Drug Info | [4] | |||
| NSC-622444 | Drug Info | [4] | |||
| NSC-622445 | Drug Info | [4] | |||
| NSC-623548 | Drug Info | [4] | |||
| S-Adenosylhomocysteine | Drug Info | [4] | |||
| S-tubercidinylhomocysteine | Drug Info | [5] | |||
| Pathways | |||||
| KEGG Pathway | Cysteine and methionine metabolism | ||||
| Metabolic pathways | |||||
| MicroRNAs in cancer | |||||
| Reactome | PRC2 methylates histones and DNA | ||||
| NoRC negatively regulates rRNA expression | |||||
| DNA methylation | |||||
| WikiPathways | Mesodermal Commitment Pathway | ||||
| Endoderm Differentiation | |||||
| Trans-sulfuration and one carbon metabolism | |||||
| One Carbon Metabolism | |||||
| miR-targeted genes in lymphocytes - TarBase | |||||
| References | |||||
| REF 1 | Nanocurcumin: a promising therapeutic advancement over native curcumin. Crit Rev Ther Drug Carrier Syst. 2013;30(4):331-68. | ||||
| 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: 7000). | ||||
| REF 3 | 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 4 | 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 5 | 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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