General Information of Drug Therapeutic Target (DTT) (ID: TT6VZ78)

DTT Name DNA [cytosine-5]-methyltransferase 3B (DNMT3B)
Synonyms M.HsaIIIB; Dnmt3b; DNA methyltransferase HsaIIIB; DNA methyltransferase 3B; DNA MTase HsaIIIB; DNA (cytosine-5)-methyltransferase 3B
Gene Name DNMT3B
DTT Type
Clinical trial target
[1]
BioChemical Class
Methyltransferase
UniProt ID
DNM3B_HUMAN
TTD ID
T65501
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 2.1.1.37
Sequence
MKGDTRHLNGEEDAGGREDSILVNGACSDQSSDSPPILEAIRTPEIRGRRSSSRLSKREV
SSLLSYTQDLTGDGDGEDGDGSDTPVMPKLFRETRTRSESPAVRTRNNNSVSSRERHRPS
PRSTRGRQGRNHVDESPVEFPATRSLRRRATASAGTPWPSPPSSYLTIDLTDDTEDTHGT
PQSSSTPYARLAQDSQQGGMESPQVEADSGDGDSSEYQDGKEFGIGDLVWGKIKGFSWWP
AMVVSWKATSKRQAMSGMRWVQWFGDGKFSEVSADKLVALGLFSQHFNLATFNKLVSYRK
AMYHALEKARVRAGKTFPSSPGDSLEDQLKPMLEWAHGGFKPTGIEGLKPNNTQPVVNKS
KVRRAGSRKLESRKYENKTRRRTADDSATSDYCPAPKRLKTNCYNNGKDRGDEDQSREQM
ASDVANNKSSLEDGCLSCGRKNPVSFHPLFEGGLCQTCRDRFLELFYMYDDDGYQSYCTV
CCEGRELLLCSNTSCCRCFCVECLEVLVGTGTAAEAKLQEPWSCYMCLPQRCHGVLRRRK
DWNVRLQAFFTSDTGLEYEAPKLYPAIPAARRRPIRVLSLFDGIATGYLVLKELGIKVGK
YVASEVCEESIAVGTVKHEGNIKYVNDVRNITKKNIEEWGPFDLVIGGSPCNDLSNVNPA
RKGLYEGTGRLFFEFYHLLNYSRPKEGDDRPFFWMFENVVAMKVGDKRDISRFLECNPVM
IDAIKVSAAHRARYFWGNLPGMNRPVIASKNDKLELQDCLEYNRIAKLKKVQTITTKSNS
IKQGKNQLFPVVMNGKEDVLWCTELERIFGFPVHYTDVSNMGRGARQKLLGRSWSVPVIR
HLFAPLKDYFACE
Function
DNA methylation is coordinated with methylation of histones. May preferentially methylates nucleosomal DNA within the nucleosome core region. May function as transcriptional co-repressor by associating with CBX4 and independently of DNA methylation. Seems to be involved in gene silencing. In association with DNMT1 and via the recruitment of CTCFL/BORIS, involved in activation of BAG1 gene expression by modulating dimethylation of promoter histone H3 at H3K4 and H3K9. Isoforms 4 and 5 are probably not functional due to the deletion of two conserved methyltransferase motifs. Function as transcriptional corepressor by associating with ZHX1. Required for DUX4 silencing in somatic cells. Required for genome-wide de novo methylation and is essential for the establishment of DNA methylation patterns during development.
KEGG Pathway
Cysteine and methionine metabolism (hsa00270 )
Metabolic pathways (hsa01100 )
MicroRNAs in cancer (hsa05206 )
Reactome Pathway
NoRC negatively regulates rRNA expression (R-HSA-427413 )
DNA methylation (R-HSA-5334118 )
PRC2 methylates histones and DNA (R-HSA-212300 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
1 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Curcumin DMQPH29 Solid tumour/cancer 2A00-2F9Z Phase 3 [1]
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4 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
PMID27376512-Compound-MTC-422 DM1MVQD N. A. N. A. Patented [2]
PMID27376512-Compound-MTC-423 DM9RSDX N. A. N. A. Patented [2]
PMID27376512-Compound-MTC-424 DMGNRZU N. A. N. A. Patented [2]
PMID27376512-Compound-MTC-427 DMWXEZD N. A. N. A. Patented [2]
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17 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(L-)-S-adenosyl-L-homocysteine DMDUN83 Discovery agent N.A. Investigative [3]
NSC-106084 DM6ID8P Discovery agent N.A. Investigative [1]
NSC-137546 DMKQYMX Discovery agent N.A. Investigative [1]
NSC-138419 DMH684Q Discovery agent N.A. Investigative [1]
NSC-154957 DMW82SA Discovery agent N.A. Investigative [1]
NSC-158324 DMDR460 Discovery agent N.A. Investigative [1]
NSC-319745 DMF3G06 Discovery agent N.A. Investigative [1]
NSC-345763 DM2UPSV Discovery agent N.A. Investigative [1]
NSC-348926 DM3TDEO Discovery agent N.A. Investigative [1]
NSC-401077 DM0214E Discovery agent N.A. Investigative [1]
NSC-54162 DMW2Q6N Discovery agent N.A. Investigative [1]
NSC-56071 DMLEN4X Discovery agent N.A. Investigative [1]
NSC-57893 DMIRK41 Discovery agent N.A. Investigative [1]
NSC-622444 DMM5UT9 Discovery agent N.A. Investigative [1]
NSC-622445 DME35CB Discovery agent N.A. Investigative [1]
NSC-623548 DMW437Z Discovery agent N.A. Investigative [1]
S-tubercidinylhomocysteine DM9UHCY Discovery agent N.A. Investigative [4]
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⏷ Show the Full List of 17 Investigative Drug(s)

References

1 Novel and selective DNA methyltransferase inhibitors: Docking-based virtual screening and experimental evaluation. Bioorg Med Chem. 2010 Jan 15;18(2):822-9.
2 DNA methyltransferase inhibitors: an updated patent review (2012-2015).Expert Opin Ther Pat. 2016 Sep;26(9):1017-30.
3 Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors. Bioorg Med Chem Lett. 2009 May 15;19(10):2742-6.
4 SAR around (l)-S-adenosyl-l-homocysteine, an inhibitor of human DNA methyltransferase (DNMT) enzymes. Bioorg Med Chem Lett. 2009 May 15;19(10):2747-51.