Details of the Drug Therapeutic Target (DTT)

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

• DTT Name: DNA [cytosine-5]-methyltransferase 3A (DNMT3A)
• Synonyms: M.HsaIIIA; Dnmt3a; DNA methyltransferase HsaIIIA; DNA MTase HsaIIIA; DNA (cytosine-5)-methyltransferase 3A
• Gene Name: DNMT3A
• DTT Type: Patented-recorded target; [1]
• BioChemical Class: Methyltransferase
• UniProt ID: DNM3A_HUMAN
• TTD ID: T29355
• EC Number: EC 2.1.1.37
• Sequence:
  MPAMPSSGPGDTSSSAAEREEDRKDGEEQEEPRGKEERQEPSTTARKVGRPGRKRKHPPV
  ESGDTPKDPAVISKSPSMAQDSGASELLPNGDLEKRSEPQPEEGSPAGGQKGGAPAEGEG
  AAETLPEASRAVENGCCTPKEGRGAPAEAGKEQKETNIESMKMEGSRGRLRGGLGWESSL
  RQRPMPRLTFQAGDPYYISKRKRDEWLARWKREAEKKAKVIAGMNAVEENQGPGESQKVE
  EASPPAVQQPTDPASPTVATTPEPVGSDAGDKNATKAGDDEPEYEDGRGFGIGELVWGKL
  RGFSWWPGRIVSWWMTGRSRAAEGTRWVMWFGDGKFSVVCVEKLMPLSSFCSAFHQATYN
  KQPMYRKAIYEVLQVASSRAGKLFPVCHDSDESDTAKAVEVQNKPMIEWALGGFQPSGPK
  GLEPPEEEKNPYKEVYTDMWVEPEAAAYAPPPPAKKPRKSTAEKPKVKEIIDERTRERLV
  YEVRQKCRNIEDICISCGSLNVTLEHPLFVGGMCQNCKNCFLECAYQYDDDGYQSYCTIC
  CGGREVLMCGNNNCCRCFCVECVDLLVGPGAAQAAIKEDPWNCYMCGHKGTYGLLRRRED
  WPSRLQMFFANNHDQEFDPPKVYPPVPAEKRKPIRVLSLFDGIATGLLVLKDLGIQVDRY
  IASEVCEDSITVGMVRHQGKIMYVGDVRSVTQKHIQEWGPFDLVIGGSPCNDLSIVNPAR
  KGLYEGTGRLFFEFYRLLHDARPKEGDDRPFFWLFENVVAMGVSDKRDISRFLESNPVMI
  DAKEVSAAHRARYFWGNLPGMNRPLASTVNDKLELQECLEHGRIAKFSKVRTITTRSNSI
  KQGKDQHFPVFMNEKEDILWCTEMERVFGFPVHYTDVSNMSRLARQRLLGRSWSVPVIRH
  LFAPLKEYFACV
• Function: DNA methylation is coordinated with methylation of histones. It modifies DNA in a non-processive manner and also methylates non-CpG sites. May preferentially methylate DNA linker between 2 nucleosomal cores and is inhibited by histone H1. Plays a role in paternal and maternal imprinting. Required for methylation of most imprinted loci in germ cells. Acts as a transcriptional corepressor for ZBTB18. Recruited to trimethylated 'Lys-36' of histone H3 (H3K36me3) sites. Can actively repress transcription through the recruitment of HDAC activity. 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:
  RMTs methylate histone arginines (R-HSA-3214858)
  SUMOylation of DNA methylation proteins (R-HSA-4655427)
  DNA methylation (R-HSA-5334118)
  Defective pyroptosis (R-HSA-9710421)
  PRC2 methylates histones and DNA (R-HSA-212300)

Molecular Interaction Atlas (MIA) of This DTT

8 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID27376512-Compound-Figure2aExample1	DMP59OX	N. A.	N. A.	Patented	[1]
PMID27376512-Compound-Figure3CG	DMZIKN6	N. A.	N. A.	Patented	[1]
PMID27376512-Compound-Figure3CM	DMIS4H0	N. A.	N. A.	Patented	[1]
PMID27376512-Compound-Figure3CN	DMP7DL6	N. A.	N. A.	Patented	[1]
PMID27376512-Compound-MTC-422	DM1MVQD	N. A.	N. A.	Patented	[1]
PMID27376512-Compound-MTC-423	DM9RSDX	N. A.	N. A.	Patented	[1]
PMID27376512-Compound-MTC-424	DMGNRZU	N. A.	N. A.	Patented	[1]
PMID27376512-Compound-MTC-427	DMWXEZD	N. A.	N. A.	Patented	[1]

References

• [1] DNA methyltransferase inhibitors: an updated patent review (2012-2015).Expert Opin Ther Pat. 2016 Sep;26(9):1017-30.