Tclin AR Androgen receptor

Protein Summary

Description

Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription factor activity is modulated by bound coactivator and corepressor proteins like ZBTB7A that recruits NCOR1 and NCOR2 to the androgen response elements/ARE on target genes, negatively regulating androgen receptor signaling and androgen-induced cell proliferation (PubMed:20812024). Transcription activation is also down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3. Isoform 3 and isoform 4 lack the C-terminal ligand-binding domain and may therefore constitutively activate the transcription of a specific set of genes independently of steroid hormones. The androgen receptor gene is more than 90 kb long and codes for a protein that has 3 major functional domains: the N-terminal domain, DNA-binding domain, and androgen-binding domain. The protein functions as a steroid-hormone activated transcription factor. Upon binding the hormone ligand, the receptor dissociates from accessory proteins, translocates into the nucleus, dimerizes, and then stimulates transcription of androgen responsive genes. This gene contains 2 polymorphic trinucleotide repeat segments that encode polyglutamine and polyglycine tracts in the N-terminal transactivation domain of its protein. Expansion of the polyglutamine tract from the normal 9-34 repeats to the pathogenic 38-62 repeats causes spinal bulbar muscular atrophy (SBMA, also known as Kennedy's disease). Mutations in this gene are also associated with complete androgen insensitivity (CAIS). Alternative splicing results in multiple transcript variants encoding different isoforms. [provided by RefSeq, Jan 2017]

Uniprot Accession IDs

• P10275
• A0A0B4J1T2
• A2RUN2
• B1AKD7
• C0JKD3
• C0JKD4
• E7EVX6
• Q9UD95

Gene Name

• AR

Ensembl ID

• ENST00000374690
• ENSP00000363822
• ENSG00000169083
• ENST00000396043
• ENSP00000379358
• ENST00000504326
• ENSP00000421155

Symbol

• DHTR
• NR3C4
• KD
• AIS
• AR8
• TFM
• DHTR
• SBMA
• HYSP1
• NR3C4
• SMAX1
• HUMARA

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
chemical	1
drug	1
hub protein	1
kinase	1
molecular function	1

Protein Classes

PANTHER Classes

Protein / Transcription Factor / Androgen Receptor

Protein / Receptor / Androgen Receptor

Protein / Nucleic Acid Binding / Androgen Receptor

Protein / ... / C4 Zinc Finger Nuclear Receptor / Androgen Receptor

DTO Classes

Protein / Nuclear Receptor / 3-ketosteroid Receptors / Androgen Receptor

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: 9304.77   (req: < 5)

Gene RIFs: 1965   (req: <= 3)

Antibodies: 2276   (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: 9304.77   (req: >= 5)

Gene RIFs: 1965   (req: > 3)

Antibodies: 2276   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 74

Tchem

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

Active Ligands: 1016

Tclin

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

Active Drugs: 33