Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

DNMT3B (Q9UBC3) - Overview - Molecular Target Synopsis

Protein


DNMT3B, DNA (cytosine-5)-methyltransferase 3B
Enzyme Classification 2.1.1.37
UniProt Q9UBC3

Also Known as DNM3B_HUMAN, DNMT3B

Required for genome-wide de novo methylation and is essential for the establishment of DNA methylation patterns during development. 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 (By similarity). 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 (PubMed:27153398). Interacts with BAZ2A/TIP5, SUV39H1 and CBX4. Interacts with UHRF1 (By similarity). Interacts with DNMT1 and DNMT3A, SETDB1, UBL1, UBE2I9 and ZHX1. Interacts with the PRC2/EED-EZH2 complex.

5NRV
HUMAN DNMT3B PWWP DOMAIN IN COMPLEX WITH 6-DIPROPYLAMINO-1-HEXANOL
RCSB/PDB
Inspect Structure
See all 3D Structures for DNMT3B

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: DNMT3B is active in the following subcellular-locations: nucleus.
GO terms: DNMT3B is active in the following subcellular-locations: intracellular membrane-bounded organelle, nucleoplasm, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project DNMT3B has gain in 3 cell-lines, loss in 0 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: K_562, MCF7, CAKI_1

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NTERA-2, PA-1, HNT-34

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: K562, H1-hESC, SK-N-SH

(see details)

3D Structures


For DNMT3B there are:
11 structures (23 chains) solved
9 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

DNMT3B is solved in complex with the approved drug(s):

95E/ETHAMBUTOL (5NR3_A, 5NR3_B).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


DNMT3B has been screened with 68 compounds (80 bioactivities), 5 compounds have bioactivities that show binding affinity of <= 500nM (7 bioactivities). (see details)