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signal transducer and activator of transcription 6

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 2993

Nomenclature: signal transducer and activator of transcription 6

Abbreviated Name: STAT6

Family: STAT transcription factors

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 847 12q13.3 STAT6 signal transducer and activator of transcription 6 1-2
Mouse - 837 10 74.59 cM Stat6 signal transducer and activator of transcription 6
Rat - 841 7q22 Stat6 signal transducer and activator of transcription 6
Previous and Unofficial Names Click here for help
IL-4 STAT | interleukin-4-induced transcription factor
Database Links Click here for help
Alphafold P42226 (Hs), P52633 (Mm)
ChEMBL Target CHEMBL5401 (Hs), CHEMBL2189147 (Mm)
Ensembl Gene ENSG00000166888 (Hs), ENSMUSG00000002147 (Mm), ENSRNOG00000025023 (Rn)
Entrez Gene 6778 (Hs), 20852 (Mm), 362896 (Rn)
Human Protein Atlas ENSG00000166888 (Hs)
KEGG Gene hsa:6778 (Hs), mmu:20852 (Mm), rno:362896 (Rn)
OMIM 601512 (Hs)
Pharos P42226 (Hs)
RefSeq Nucleotide NM_001178078 (Hs), NM_009284 (Mm), NM_001044250 (Rn)
RefSeq Protein NP_001171549 (Hs), NP_033310 (Mm), NP_001037715 (Rn)
UniProtKB P42226 (Hs), P52633 (Mm)
Wikipedia STAT6 (Hs)

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 19a [PMID: 26506089] Small molecule or natural product Immunopharmacology Ligand Hs Inhibition 7.6 pIC50 3
⤷ pIC50 7.6 (IC50 2.8x10-8 M) [3]
Description: Inhibition of STAT6 expressed in Escherichia coli using FAM-Ala-pTyr-Lys-ProPhe-Gln-Asp-Leu-Ile-NH2 as substrate by fluorescence polarization assay.
Immunopharmacology Comments
STAT6 plays a central role in exerting IL-4 mediated biological responses. The prosurvival activity of the Th2 cytokine IL-4 is mediated by STAT6-dependent transcription of the anti-apoptotic protein B-cell lymphoma-extra large (Bcl-XL). This mechanism explains the resistance to apoptosis that is observed epithelial tumours which produce IL-4 [4]. IL-13 also signals via STAT6-mediated transcriptional regulation. Since both IL-4 and IL-13 play significant roles in Th2 inflammatory reponses (e.g. allergy and atopy), blockade of STAT6 activity is an attractive mechanism for asthma and other allergic diseases. Phosphopeptides that interfere with the STAT6-cytokine receptor interaction have been developed to validate this pathway as as novel therapeutic opportunity for the design of drugs to treat allergic inflammation [3].
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  T cell (activation)
Immuno Process:  B cell (activation)
Immuno Process:  Immune regulation
Immuno Process:  Immune system development
Immuno Process:  Cytokine production & signalling
Immuno Process:  Cellular signalling

References

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1. Hou J, Schindler U, Henzel WJ, Ho TC, Brasseur M, McKnight SL. (1994) An interleukin-4-induced transcription factor: IL-4 Stat. Science, 265 (5179): 1701-6. [PMID:8085155]

2. Leek JP, Hamlin PJ, Bell SM, Lench NJ. (1997) Assignment of the STAT6 gene (STAT6) to human chromosome band 12q13 by in situ hybridization. Cytogenet Cell Genet, 79 (3-4): 208-9. [PMID:9605853]

3. Mandal PK, Morlacchi P, Knight JM, Link TM, Lee 4th GR, Nurieva R, Singh D, Dhanik A, Kavraki L, Corry DB et al.. (2015) Targeting the Src Homology 2 (SH2) Domain of Signal Transducer and Activator of Transcription 6 (STAT6) with Cell-Permeable, Phosphatase-Stable Phosphopeptide Mimics Potently Inhibits Tyr641 Phosphorylation and Transcriptional Activity. J Med Chem, 58 (22): 8970-84. [PMID:26506089]

4. Todaro M, Lombardo Y, Francipane MG, Alea MP, Cammareri P, Iovino F, Di Stefano AB, Di Bernardo C, Agrusa A, Condorelli G et al.. (2008) Apoptosis resistance in epithelial tumors is mediated by tumor-cell-derived interleukin-4. Cell Death Differ, 15 (4): 762-72. [PMID:18202702]

How to cite this page

STAT transcription factors: signal transducer and activator of transcription 6. Last modified on 13/03/2018. Accessed on 14/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2993.