lysine demethylase 5B | 1.14.11.- Histone demethylases | IUPHAR/BPS Guide to PHARMACOLOGY

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lysine demethylase 5B

Target not currently curated in GtoImmuPdb

Target id: 2681

Nomenclature: lysine demethylase 5B

Family: 1.14.11.- Histone demethylases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1544 1q32.1 KDM5B lysine demethylase 5B
Mouse - 1544 1 E4 Kdm5b lysine (K)-specific demethylase 5B
Rat - 1544 13q13 Kdm5b lysine demethylase 5B
Previous and Unofficial Names
JARID1B | jumonji/ARID domain-containing protein 1B | Jumonji AT-rich interactive domain 1B | lysine (K)-specific demethylase 5B | PLU1
Database Links
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human PLU-1 (JARID1B) in complex with KDOAM25a (note that JARID1B=KDM5B).
PDB Id:  5A3N
Ligand:  KDOAM25
Resolution:  2.0Å
Species:  Human
References: 

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
GSK-J1 Hs Inhibition 6.8 pIC50 2
pIC50 6.8 (IC50 1.7x10-7 M) [2]
KDM5 inhibitor N71 Hs Irreversible inhibition 6.7 pIC50 3
pIC50 6.7 (IC50 2.2x10-7 M) [3]
Description: AlphaLISA derived IC50 values of the inhibition of KDM5B-mediated histone demethylation.
Compound 9 [doi:10.26434/chemrxiv.7072592.v1] Hs Inhibition 6.5 pIC50 5
pIC50 6.5 (IC50 3x10-7 M) [5]
PBIT Hs Inhibition 5.5 pIC50 4
pIC50 5.5 (IC50 3x10-6 M) [4]
GSK-J4 Hs Inhibition 5.0 pIC50 2
pIC50 5.0 (IC50 9.7x10-6 M) [2]
Inhibitor Comments
PBIT also inhibits KDM5A and KDM5C, with IC50 values of 6000 and 4900 nm respectively [4].
Gene Expression and Pathophysiology
Overexpression
Tissue or cell type: 
Pathophysiology:  Various cancers
Species:  Human
Technique: 
References:  1
General Comments
KDM5B is an H3K4 histone demethylase [6], belonging to a subfamily of demethylases responsible for the demethylation of H3K4me3 [4].

References

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1. Blair LP, Cao J, Zou MR, Sayegh J, Yan Q. (2011) Epigenetic Regulation by Lysine Demethylase 5 (KDM5) Enzymes in Cancer. Cancers (Basel), 3 (1): 1383-404. [PMID:21544224]

2. Heinemann B, Nielsen JM, Hudlebusch HR, Lees MJ, Larsen DV, Boesen T, Labelle M, Gerlach LO, Birk P, Helin K. (2014) Inhibition of demethylases by GSK-J1/J4. Nature, 514 (7520): E1-2. [PMID:25279926]

3. Horton JR, Woodcock CB, Chen Q, Liu X, Zhang X, Shanks J, Rai G, Mott BT, Jansen DJ, Kales SC et al.. (2018) Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A. J. Med. Chem., [Epub ahead of print]. [PMID:30392349]

4. Sayegh J, Cao J, Zou MR, Morales A, Blair LP, Norcia M, Hoyer D, Tackett AJ, Merkel JS, Yan Q. (2013) Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen. J. Biol. Chem., 288 (13): 9408-17. [PMID:23408432]

5. Vazquez-Rodriguez et al.. (2018) Design, Synthesis and Characterization of Covalent KDM5 Inhibitors. ChemRxiv, Preprint. DOI: 10.26434/chemrxiv.7072592.v1

6. Yamane K, Tateishi K, Klose RJ, Fang J, Fabrizio LA, Erdjument-Bromage H, Taylor-Papadimitriou J, Tempst P, Zhang Y. (2007) PLU-1 is an H3K4 demethylase involved in transcriptional repression and breast cancer cell proliferation. Mol. Cell, 25 (6): 801-12. [PMID:17363312]

How to cite this page

1.14.11.- Histone demethylases: lysine demethylase 5B. Last modified on 20/11/2018. Accessed on 19/04/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2681.