signal transducer and activator of transcription 6 | STAT transcription factors | IUPHAR Guide to IMMUNOPHARMACOLOGY

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signal transducer and activator of transcription 6

Target id: 2993

Nomenclature: signal transducer and activator of transcription 6

Abbreviated Name: STAT6

Family: STAT transcription factors

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

   GtoImmuPdb view: ON :     signal transducer and activator of transcription 6 has curated data in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 847 12q13 STAT6 signal transducer and activator of transcription 6 1-2
Mouse - 837 10 D3; 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
IL-4 STAT | interleukin-4-induced transcription factor
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

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Inhibitors
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Ligand Sp. Action Affinity Units Reference
compound 19a [PMID: 26506089] 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].

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 15/12/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2993.