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

KDM2A (Q9Y2K7) - Overview - Molecular Target Synopsis

Protein


KDM2A, Lysine-specific demethylase 2A
Enzyme Classification 1.14.11.27
UniProt Q9Y2K7

Also Known as KDM2A_HUMAN, KDM2A, CXXC8, FBL7, FBXL11, JHDM1A, KIAA1004

Histone demethylase that specifically demethylates 'Lys-36' of histone H3, thereby playing a central role in histone code. Preferentially demethylates dimethylated H3 'Lys-36' residue while it has weak or no activity for mono- and tri-methylated H3 'Lys-36'. May also recognize and bind to some phosphorylated proteins and promote their ubiquitination and degradation. Required to maintain the heterochromatic state. Associates with centromeres and represses transcription of small non-coding RNAs that are encoded by the clusters of satellite repeats at the centromere. Required to sustain centromeric integrity and genomic stability, particularly during mitosis. Part of a SCF (SKP1-cullin-F-box) protein ligase complex (By similarity). Interacts with CBX5/HP1A; the interaction promotes CBX5 localization to chromatin.

6C16
UBIQUITIN VARIANT (UBV.FBL10.1) BOUND TO A HUMAN SKP1-FBL11 FRAGMENT COMPLEX.
RCSB/PDB
Inspect Structure
See all 3D Structures for KDM2A

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: KDM2A is active in the following subcellular-locations: nucleoplasm, nucleus.
GO terms: KDM2A is active in the following subcellular-locations: nucleoplasm.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project KDM2A has gain in 11 cell-lines, loss in 0 cell-lines and no signal in 994 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are:

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HuH-7, SNU-387, HCC366

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: SK-N-SH, HSMM, NHLF

(see details)

3D Structures


For KDM2A there are:
5 structures (9 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


KDM2A has been screened with 97 compounds (131 bioactivities), 12 compounds have bioactivities that show binding affinity of <= 500nM (19 bioactivities). (see details)