Target Information
| Target General Information | Top | |||||
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| Target ID |
T65197
(Former ID: TTDS00144)
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| Target Name |
Erythropoietin Receptor (EPOR)
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| Synonyms |
Full-length form; EPO-R
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| Gene Name |
EPOR
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 3 Target-related Diseases | + | ||||
| 1 | Anemia [ICD-11: 3A00-3A9Z] | |||||
| 2 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| 3 | Transplant rejection [ICD-11: NE84] | |||||
| Function |
Mediates erythropoietin-induced erythroblast proliferation and differentiation. Upon EPO stimulation, EPOR dimerizes triggering the JAK2/STAT5 signaling cascade. In some cell types, can also activate STAT1 and STAT3. May also activate the LYN tyrosine kinase. Receptor for erythropoietin.
Click to Show/Hide
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| BioChemical Class |
Cytokine receptor
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| UniProt ID | ||||||
| Sequence |
MDHLGASLWPQVGSLCLLLAGAAWAPPPNLPDPKFESKAALLAARGPEELLCFTERLEDL
VCFWEEAASAGVGPGNYSFSYQLEDEPWKLCRLHQAPTARGAVRFWCSLPTADTSSFVPL ELRVTAASGAPRYHRVIHINEVVLLDAPVGLVARLADESGHVVLRWLPPPETPMTSHIRY EVDVSAGNGAGSVQRVEILEGRTECVLSNLRGRTRYTFAVRARMAEPSFGGFWSAWSEPV SLLTPSDLDPLILTLSLILVVILVLLTVLALLSHRRALKQKIWPGIPSPESEFEGLFTTH KGNFQLWLYQNDGCLWWSPCTPFTEDPPASLEVLSERCWGTMQAVEPGTDDEGPLLEPVG SEHAQDTYLVLDKWLLPRNPPSEDLPGPGGSVDIVAMDEGSEASSCSSALASKPSPEGAS AASFEYTILDPSSQLLRPWTLCPELPPTPPHLKYLYLVVSDSGISTDYSSGDSQGAQGGL SDGPYSNPYENSLIPAAEPLPPSYVACS Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T89LO8 | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 4 Approved Drugs | + | ||||
| 1 | Darbepoetin alfa | Drug Info | Approved | Anemia | [2] | |
| 2 | Epoetin alfa | Drug Info | Approved | Anemia | [3] | |
| 3 | Methoxy polyethylene glycol-epoetin beta | Drug Info | Approved | Kidney transplant rejection | [4], [5] | |
| 4 | RHuEPO | Drug Info | Approved | Solid tumour/cancer | [5], [6] | |
| Clinical Trial Drug(s) | [+] 4 Clinical Trial Drugs | + | ||||
| 1 | Epoetin zeta | Drug Info | Phase 3 | Anemia | [7] | |
| 2 | ErepoXen | Drug Info | Phase 3 | Anemia | [8] | |
| 3 | Hematide | Drug Info | Phase 3 | Anemia | [9] | |
| 4 | Cibinetide | Drug Info | Phase 2 | Depression | [10] | |
| Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
| 1 | GlycoPEGylated erythropoietin | Drug Info | Discontinued in Phase 2 | Solid tumour/cancer | [11] | |
| 2 | Albupoietin | Drug Info | Terminated | Anemia | [12] | |
| Mode of Action | [+] 5 Modes of Action | + | ||||
| Agonist | [+] 5 Agonist drugs | + | ||||
| 1 | Darbepoetin alfa | Drug Info | [13] | |||
| 2 | Epoetin alfa | Drug Info | [1], [14] | |||
| 3 | ErepoXen | Drug Info | [17] | |||
| 4 | Hematide | Drug Info | [18], [19], [20] | |||
| 5 | Cibinetide | Drug Info | [21] | |||
| Activator | [+] 1 Activator drugs | + | ||||
| 1 | Methoxy polyethylene glycol-epoetin beta | Drug Info | [4] | |||
| Stimulator | [+] 7 Stimulator drugs | + | ||||
| 1 | RHuEPO | Drug Info | [15] | |||
| 2 | BBT-009 | Drug Info | [15] | |||
| 3 | BBT-021 | Drug Info | [15] | |||
| 4 | Erythropoietin | Drug Info | [15] | |||
| 5 | P-1116 | Drug Info | [15] | |||
| 6 | PEG-EPO | Drug Info | [15] | |||
| 7 | PT-401 | Drug Info | [15] | |||
| Modulator | [+] 6 Modulator drugs | + | ||||
| 1 | Epoetin zeta | Drug Info | [16] | |||
| 2 | GlycoPEGylated erythropoietin | Drug Info | [22] | |||
| 3 | Albupoietin | Drug Info | [23] | |||
| 4 | EPO peptide mimetics | Drug Info | [15] | |||
| 5 | EPO-derived peptide | Drug Info | [15] | |||
| 6 | Nova-EPO | Drug Info | [15] | |||
| Inhibitor | [+] 1 Inhibitor drugs | + | ||||
| 1 | 3,5 DIBROMOTYROSINE | Drug Info | [24] | |||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating Transcription Factors | ||||||
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
| 1 | Cytokine-cytokine receptor interaction | |||||
| 2 | PI3K-Akt signaling pathway | |||||
| 3 | Jak-STAT signaling pathway | |||||
| 4 | Hematopoietic cell lineage | |||||
| NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
| 1 | TGF_beta_Receptor Signaling Pathway | |||||
| PID Pathway | [+] 2 PID Pathways | + | ||||
| 1 | Signaling events mediated by Stem cell factor receptor (c-Kit) | |||||
| 2 | EPO signaling pathway | |||||
| WikiPathways | [+] 1 WikiPathways | + | ||||
| 1 | EPO Receptor Signaling | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | 2007 Standards, Options, and Recommendations: use of erythropoiesis-stimulating agents (ESA: epoetin alfa, epoetin beta, and darbepoetin) for the management of anemia in children with cancer. PediatrBlood Cancer. 2009 Jul;53(1):7-12. | |||||
| REF 2 | Emerging treatments for traumatic brain injury. Expert Opin Emerg Drugs. 2009 Mar;14(1):67-84. | |||||
| REF 3 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (BLA) 103951. | |||||
| REF 4 | 2007 FDA drug approvals: a year of flux. Nat Rev Drug Discov. 2008 Feb;7(2):107-9. | |||||
| REF 5 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008056) | |||||
| REF 7 | Comparison of the therapeutic effects of epoetin zeta to epoetin alfa in the maintenance phase of renal anaemia treatment. Curr Med Res Opin. 2008 Mar;24(3):625-37. | |||||
| REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033828) | |||||
| REF 9 | Clinical pipeline report, company report or official report of Takeda. | |||||
| REF 10 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035038) | |||||
| REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018390) | |||||
| REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017518) | |||||
| REF 13 | A cytosolic domain of the erythropoietin receptor contributes to endoplasmic reticulum-associated degradation. Eur J Biochem. 1999 Jul;263(2):410-9. | |||||
| REF 14 | Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51. | |||||
| REF 15 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1718). | |||||
| REF 16 | Long-term safety and tolerability of epoetin zeta, administered intravenously, for maintenance treatment of renal anemia. Adv Ther. 2008 Nov;25(11):1215-28. | |||||
| REF 17 | Combination erythropoietin-hydroxyurea therapy in sickle cell disease: experience from the National Institutes of Health and a literature review. Haematologica. 2006 Aug;91(8):1076-83. | |||||
| REF 18 | Nat Rev Drug Discov. 2013 Feb;12(2):87-90. | |||||
| REF 19 | Peginesatide and erythropoietin stimulate similar erythropoietin receptor-mediated signal transduction and gene induction events. Exp Hematol. 2012 Jul;40(7):575-87. | |||||
| REF 20 | Anemia in chronic kidney disease: status of new therapies. Curr Opin Nephrol Hypertens. 2009 Mar;18(2):112-5. | |||||
| REF 21 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 22 | Design of Homogeneous, MonoPEGylated Erythropoietin Analogs With Preserved In Vitro Bioactivity. Exp Hematol. 2006 June; 34(6): 697-704. | |||||
| REF 23 | Clinical pipeline report, company report or official report of cogenesys. | |||||
| REF 24 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | |||||
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