Target General Infomation
Target ID
T65501
Former ID
TTDR01100
Target Name
DNA (cytosine-5)-methyltransferase 3B
Gene Name
DNMT3B
Synonyms
DNA MTase HsaIIIB; DNA methyltransferase 3B; DNA methyltransferase HsaIIIB; Dnmt3b; M.HsaIIIB; DNMT3B
Target Type
Clinical Trial
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.
BioChemical Class
Methyltransferase superfamily
Target Validation
T65501
UniProt ID
EC Number
EC 2.1.1.37
Sequence
MKGDTRHLNGEEDAGGREDSILVNGACSDQSSDSPPILEAIRTPEIRGRRSSSRLSKREV
SSLLSYTQDLTGDGDGEDGDGSDTPVMPKLFRETRTRSESPAVRTRNNNSVSSRERHRPS
PRSTRGRQGRNHVDESPVEFPATRSLRRRATASAGTPWPSPPSSYLTIDLTDDTEDTHGT
PQSSSTPYARLAQDSQQGGMESPQVEADSGDGDSSEYQDGKEFGIGDLVWGKIKGFSWWP
AMVVSWKATSKRQAMSGMRWVQWFGDGKFSEVSADKLVALGLFSQHFNLATFNKLVSYRK
AMYHALEKARVRAGKTFPSSPGDSLEDQLKPMLEWAHGGFKPTGIEGLKPNNTQPVVNKS
KVRRAGSRKLESRKYENKTRRRTADDSATSDYCPAPKRLKTNCYNNGKDRGDEDQSREQM
ASDVANNKSSLEDGCLSCGRKNPVSFHPLFEGGLCQTCRDRFLELFYMYDDDGYQSYCTV
CCEGRELLLCSNTSCCRCFCVECLEVLVGTGTAAEAKLQEPWSCYMCLPQRCHGVLRRRK
DWNVRLQAFFTSDTGLEYEAPKLYPAIPAARRRPIRVLSLFDGIATGYLVLKELGIKVGK
YVASEVCEESIAVGTVKHEGNIKYVNDVRNITKKNIEEWGPFDLVIGGSPCNDLSNVNPA
RKGLYEGTGRLFFEFYHLLNYSRPKEGDDRPFFWMFENVVAMKVGDKRDISRFLECNPVM
IDAIKVSAAHRARYFWGNLPGMNRPVIASKNDKLELQDCLEYNRIAKLKKVQTITTKSNS
IKQGKNQLFPVVMNGKEDVLWCTELERIFGFPVHYTDVSNMGRGARQKLLGRSWSVPVIR
HLFAPLKDYFACE
Drugs and Mode of Action
Drug(s) Curcumin Drug Info Phase 3 Cancer [532348], [542031]
Inhibitor (L-)-S-adenosyl-L-homocysteine Drug Info [530076]
Curcumin Drug Info [530577]
NSC-106084 Drug Info [530577]
NSC-137546 Drug Info [530577]
NSC-138419 Drug Info [530577]
NSC-154957 Drug Info [530577]
NSC-158324 Drug Info [530577]
NSC-319745 Drug Info [530577]
NSC-345763 Drug Info [530577]
NSC-348926 Drug Info [530577]
NSC-401077 Drug Info [530577]
NSC-54162 Drug Info [530577]
NSC-56071 Drug Info [530577]
NSC-57893 Drug Info [530577]
NSC-622444 Drug Info [530577]
NSC-622445 Drug Info [530577]
NSC-623548 Drug Info [530577]
S-Adenosylhomocysteine Drug Info [530577]
S-tubercidinylhomocysteine Drug Info [530075]
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 532348Nanocurcumin: a promising therapeutic advancement over native curcumin. Crit Rev Ther Drug Carrier Syst. 2013;30(4):331-68.
Ref 542031(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 530075Bioorg 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.
Ref 530076Bioorg 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 530577Bioorg 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.

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