Tchem KDM5A Lysine-specific demethylase 5A

Protein Summary

Description

Histone demethylase that specifically demethylates 'Lys-4' of histone H3, thereby playing a central role in histone code. Does not demethylate histone H3 'Lys-9', H3 'Lys-27', H3 'Lys-36', H3 'Lys-79' or H4 'Lys-20'. Demethylates trimethylated and dimethylated but not monomethylated H3 'Lys-4'. Regulates specific gene transcription through DNA-binding on 5'-CCGCCC-3' motif (PubMed:18270511). May stimulate transcription mediated by nuclear receptors. Involved in transcriptional regulation of Hox proteins during cell differentiation (PubMed:19430464). May participate in transcriptional repression of cytokines such as CXCL12. Plays a role in the regulation of the circadian rhythm and in maintaining the normal periodicity of the circadian clock. In a histone demethylase-independent manner, acts as a coactivator of the CLOCK-ARNTL/BMAL1-mediated transcriptional activation of PER1/2 and other clock-controlled genes and increases histone acetylation at PER1/2 promoters by inhibiting the activity of HDAC1 (By similarity). Seems to act as a transcriptional corepressor for some genes such as MT1F and to favor the proliferation of cancer cells (PubMed:27427228). This gene encodes a member of the Jumonji, AT-rich interactive domain 1 (JARID1) histone demethylase protein family. The encoded protein plays a role in gene regulation through the histone code by specifically demethylating lysine 4 of histone H3. The encoded protein interacts with many other proteins, including retinoblastoma protein, and is implicated in the transcriptional regulation of Hox genes and cytokines. This gene may play a role in tumor progression. [provided by RefSeq, Aug 2013]

Uniprot Accession IDs

• P29375
• A8MV76
• Q4LE72
• Q86XZ1

Gene Name

• KDM5A

Ensembl ID

• ENST00000399788
• ENSP00000382688
• ENSG00000073614

Symbol

• JARID1A
• RBBP2
• RBP2
• RBP2
• RBBP2
• RBBP-2

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
protein domain	1
drug perturbation	0.96
transcription factor perturbation	0.94
molecular function	0.84
transcription factor binding site profile	0.83

Protein Classes

PANTHER Classes

Protein / Transcription Factor / Zinc Finger Transcription Factor / Lysine-specific Demethylase 5a

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 139.31   (req: < 5)

Gene RIFs: 68   (req: <= 3)

Antibodies: 195   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 139.31   (req: >= 5)

Gene RIFs: 68   (req: > 3)

Antibodies: 195   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 24

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 223

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 0