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

SETD7 (Q8WTS6) - Overview - Molecular Target Synopsis

Protein


SETD7, Histone-lysine N-methyltransferase SETD7
Enzyme Classification 2.1.1.43
UniProt Q8WTS6

Also Known as SETD7_HUMAN, SETD7, KIAA1717, KMT7, SET7, SET9

Histone methyltransferase that specifically monomethylates 'Lys-4' of histone H3. H3 'Lys-4' methylation represents a specific tag for epigenetic transcriptional activation. Plays a central role in the transcriptional activation of genes such as collagenase or insulin. Recruited by IPF1/PDX-1 to the insulin promoter, leading to activate transcription. Has also methyltransferase activity toward non-histone proteins such as p53/TP53, TAF10, and possibly TAF7 by recognizing and binding the [KR]-[STA]-K in substrate proteins. Monomethylates 'Lys-189' of TAF10, leading to increase the affinity of TAF10 for RNA polymerase II. Monomethylates 'Lys-372' of p53/TP53, stabilizing p53/TP53 and increasing p53/TP53-mediated transcriptional activation. Interacts with IPF1/PDX-1.

5YLT
CRYSTAL STRUCTURE OF SET7/9 IN COMPLEX WITH A CYPROHEPTADINE DERIVATIVE
RCSB/PDB
Inspect Structure
See all 3D Structures for SETD7

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: SETD7 is active in the following subcellular-locations: chromosome, nucleus.
GO terms: SETD7 is active in the following subcellular-locations: chromosome, nucleolus, nucleoplasm.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project SETD7 has gain in 0 cell-lines, loss in 3 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, SF_295, MDA_MB_231

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HCC2688, Hs 746T, NCI-H820

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: HSMM, NHLF, MCF-7

(see details)

3D Structures


For SETD7 there are:
32 structures (42 chains) solved
30 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

SETD7 is solved in complex with the approved drug(s):

C7H/CYPROHEPTADINE (5AYF_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


SETD7 has been screened with 188 compounds (224 bioactivities), 1 compounds have bioactivities that show binding affinity of <= 500nM (2 bioactivities). (see details)