Eythropoietin receptor

Target id: 1718

Nomenclature: Eythropoietin receptor

Family: Prolactin receptor family

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

   GtoImmuPdb view: OFF :     Eythropoietin receptor has curated GtoImmuPdb data

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 508 19p13.3-p13.2 EPOR erythropoietin receptor
Mouse 1 507 9 7.93 cM Epor erythropoietin receptor
Rat 1 507 8q13 Epor erythropoietin receptor
Previous and Unofficial Names
EPO-R | erythropoietin receptor
Database Links
CATH/Gene3D
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
Orphanet
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human erythropoietin complexed to its receptor at 1.9 angstroms
PDB Id:  1EER
Ligand:  erythropoietin
Resolution:  1.9Å
Species:  Human
References:  5

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
erythropoietin {Sp: Human} Hs Agonist 11.1 pIC50 3
pIC50 11.1 (IC50 7x10-12 M) [3]
Description: Assay performed using recombinant human EPO
peginesatide Hs Agonist 10.4 pIC50 3
pIC50 10.4 (IC50 3.7x10-11 M) [3]
cibinetide Hs Agonist - - 2
[2]
Immunopharmacology Comments
A non-hematopoietic EPOR-containing receptor, called the innate repair receptor (IRR) or tissue-protective receptor, down-modulates the damaging effects of the immune response to tissue injury [1]. This EPO-mediated tissue-protective system acts via a heterodimeric receptor composed of the EPOR and the cytokine receptor β common receptor subunit (CD131) [1]. IRR is not normally expressed by normal tissues. Its expression is rapidly upregulated by tissue injury, inflammation and hypoxia. This system acts as a compensatory protective response in tissues exposed to tumor necrosis factor (TNF)-α and other proinflammatory cytokines that are released at sites of tissue insult, and promotes tissue recovery. Synthetic peptides that selectively activate the IRR (i.e. that do not activate the hematopoietic receptor responsible for erythropoiesis and are devoid of hematopoietic and thrombotic effects) are being developed for their potential tissue-protective and damage-mitigating effects in a number of pathological settings [4]- see cibinetide as an example.
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
Immuno Process ID:  9
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  erythropoietin receptor activity (GO:0004900) IDA
References: 
Clinically-Relevant Mutations and Pathophysiology
Disease:  Erythrocytosis, familial, 1; ECYT1
Synonyms: Primary familial polycythemia [Orphanet: ORPHA90042]
OMIM: 133100
Orphanet: ORPHA90042
General Comments
The EPO/EPOR sytem is responsible for erythropoiesis and has an endogenous tissue protective role. The classical hematopoietic EPO receptor is a homodimer of two EPOR subunits. A non-hematopoietic EPOR-containing receptor, called the innate repair receptor (IRR) or tissue-protective receptor exists, and structurally this is a heterodimer composed of the EPOR and the cytokine receptor β common receptor subunit (CD131) [1].

References

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1. Brines M, Cerami A. (2012) The receptor that tames the innate immune response. Mol. Med.18: 486-96. [PMID:22183892]

2. Cerami A, Brines M. (2009) Tissue protective peptides and peptide analogs for preventing and treating diseases and disorders associated with tissue damage. Patent number: WO2009094172. Assignee: Araim Pharmaceuticals, Inc.. Priority date: 18/10/2017. Publication date: 22/01/2009.

3. Fan Q, Leuther KK, Holmes CP, Fong KL, Zhang J, Velkovska S, Chen MJ, Mortensen RB, Leu K, Green JM et al.. (2006) Preclinical evaluation of Hematide, a novel erythropoiesis stimulating agent, for the treatment of anemia. Exp. Hematol.34 (10): 1303-11. [PMID:16982323]

4. Leist M, Ghezzi P, Grasso G, Bianchi R, Villa P, Fratelli M, Savino C, Bianchi M, Nielsen J, Gerwien J et al.. (2004) Derivatives of erythropoietin that are tissue protective but not erythropoietic. Science305 (5681): 239-42. [PMID:15247477]

5. Syed RS, Reid SW, Li C, Cheetham JC, Aoki KH, Liu B, Zhan H, Osslund TD, Chirino AJ, Zhang J et al.. (1998) Efficiency of signalling through cytokine receptors depends critically on receptor orientation. Nature395 (6701): 511-6. [PMID:9774108]

How to cite this page

Prolactin receptor family: Eythropoietin receptor. Last modified on 18/10/2017. Accessed on 13/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1718.