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

KDM1B (Q8NB78) - Overview - Molecular Target Synopsis

Protein


KDM1B, Lysine-specific histone demethylase 1B
Enzyme Classification 1.-.-.-
UniProt Q8NB78

Also Known as KDM1B_HUMAN, KDM1B, AOF1, C6orf193, LSD2

Histone demethylase that demethylates 'Lys-4' of histone H3, a specific tag for epigenetic transcriptional activation, thereby acting as a corepressor. Required for de novo DNA methylation of a subset of imprinted genes during oogenesis. Acts by oxidizing the substrate by FAD to generate the corresponding imine that is subsequently hydrolyzed. Demethylates both mono- and di-methylated 'Lys-4' of histone H3. Has no effect on tri-methylated 'Lys-4', mono-, di- or tri-methylated 'Lys-9', mono-, di- or tri-methylated 'Lys-27', mono-, di- or tri-methylated 'Lys-36' of histone H3, or on mono-, di- or tri-methylated 'Lys-20' of histone H4. Does not form a complex with RCOR1/CoREST (By similarity). Interacts with its cofactor GLYR1 at nucleosomes; this interaction stimulates H3K4me1 and H3K4me2 demethylation (PubMed:23260659).

4HSU
CRYSTAL STRUCTURE OF LSD2-NPAC WITH H3(1-26)IN SPACE GROUP P21
RCSB/PDB
Inspect Structure
See all 3D Structures for KDM1B

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: KDM1B is active in the following subcellular-locations: nucleus.
GO terms: KDM1B is active in the following subcellular-locations: nucleoplasm, nucleosome, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project KDM1B has gain in 4 cell-lines, loss in 1 cell-lines and no signal in 999 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: NCI-H209, MHH-PREB-1, NCI-H522

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, NHEK, NHLF

(see details)

3D Structures


For KDM1B there are:
10 structures (15 chains) solved
10 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


KDM1B has been screened with 32 compounds (40 bioactivities). (see details)