Target General Infomation
Target ID
T65197 (Former ID: TTDS00144)
Target Name
Erythropoietin Receptor (EPOR)
Synonyms
Full-length form; EPO-R
Gene Name
EPOR
Target Type
Successful target
[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.
BioChemical Class
Cytokine receptor
UniProt ID
EPOR_HUMAN
Sequence
MDHLGASLWPQVGSLCLLLAGAAWAPPPNLPDPKFESKAALLAARGPEELLCFTERLEDL
VCFWEEAASAGVGPGNYSFSYQLEDEPWKLCRLHQAPTARGAVRFWCSLPTADTSSFVPL
ELRVTAASGAPRYHRVIHINEVVLLDAPVGLVARLADESGHVVLRWLPPPETPMTSHIRY
EVDVSAGNGAGSVQRVEILEGRTECVLSNLRGRTRYTFAVRARMAEPSFGGFWSAWSEPV
SLLTPSDLDPLILTLSLILVVILVLLTVLALLSHRRALKQKIWPGIPSPESEFEGLFTTH
KGNFQLWLYQNDGCLWWSPCTPFTEDPPASLEVLSERCWGTMQAVEPGTDDEGPLLEPVG
SEHAQDTYLVLDKWLLPRNPPSEDLPGPGGSVDIVAMDEGSEASSCSSALASKPSPEGAS
AASFEYTILDPSSQLLRPWTLCPELPPTPPHLKYLYLVVSDSGISTDYSSGDSQGAQGGL
SDGPYSNPYENSLIPAAEPLPPSYVACS
Drugs and Modes of Action
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) [+] 5 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 ARA 290 Drug Info Phase 2 Depression [10]
5 Cibinetide Drug Info Phase 2 Sarcoidosis [11]
Discontinued Drug(s) [+] 2 Discontinued Drugs +
1 GlycoPEGylated erythropoietin Drug Info Discontinued in Phase 2 Solid tumour/cancer [12]
2 Albupoietin Drug Info Terminated Anemia [13]
Mode of Action [+] 5 Modes of Action +
Agonist [+] 6 Agonist drugs +
1 Darbepoetin alfa Drug Info [14]
2 Epoetin alfa Drug Info [1], [15]
3 ErepoXen Drug Info [18]
4 Hematide Drug Info [19], [20], [21]
5 ARA 290 Drug Info [22], [23]
6 Cibinetide Drug Info [11]
Activator [+] 1 Activator drugs +
1 Methoxy polyethylene glycol-epoetin beta Drug Info [4]
Stimulator [+] 7 Stimulator drugs +
1 RHuEPO Drug Info [16]
2 BBT-009 Drug Info [16]
3 BBT-021 Drug Info [16]
4 Erythropoietin Drug Info [16]
5 P-1116 Drug Info [16]
6 PEG-EPO Drug Info [16]
7 PT-401 Drug Info [16]
Modulator [+] 7 Modulator drugs +
1 Epoetin zeta Drug Info [17]
2 GlycoPEGylated erythropoietin Drug Info [24]
3 Albupoietin Drug Info [25]
4 EPO peptide mimetics Drug Info [16]
5 EPO-derived peptide Drug Info [16]
6 Nova-EPO Drug Info [16]
7 PharmaPEG-EPO Drug Info [16]
Inhibitor [+] 1 Inhibitor drugs +
1 3,5 DIBROMOTYROSINE Drug Info [26]
Target Regulators
Target-regulating Transcription Factors
Target-interacting Proteins
Target Profiles in Patients
Target Expression
 Profile (TEP)
Target Affiliated Biological Pathways
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
Target Validation
References
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 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
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 800018390)
REF 13 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 14 A cytosolic domain of the erythropoietin receptor contributes to endoplasmic reticulum-associated degradation. Eur J Biochem. 1999 Jul;263(2):410-9.
REF 15 Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
REF 16 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 17 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 18 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 19 Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
REF 20 Peginesatide and erythropoietin stimulate similar erythropoietin receptor-mediated signal transduction and gene induction events. Exp Hematol. 2012 Jul;40(7):575-87.
REF 21 Anemia in chronic kidney disease: status of new therapies. Curr Opin Nephrol Hypertens. 2009 Mar;18(2):112-5.
REF 22 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
REF 23 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
REF 24 Design of Homogeneous, MonoPEGylated Erythropoietin Analogs With Preserved In Vitro Bioactivity. Exp Hematol. 2006 June; 34(6): 697-704.
REF 25 Clinical pipeline report, company report or official report of cogenesys.
REF 26 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.

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