Target Information
| Target General Information | Top | |||||
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| Target ID |
T07958
(Former ID: TTDI01917)
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| Target Name |
Erythropoietin (EPO)
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| Synonyms |
Epoetin
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| Gene Name |
EPO
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Retinopathy [ICD-11: 9B71] | |||||
| 2 | Anemia [ICD-11: 3A00-3A9Z] | |||||
| Function |
Binds to EPOR leading to EPOR dimerization and JAK2 activation thereby activating specific downstream effectors, including STAT1 and STAT3. Hormone involved in the regulation of erythrocyte proliferation and differentiation and the maintenance of a physiological level of circulating erythrocyte mass.
Click to Show/Hide
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| UniProt ID | ||||||
| Sequence |
MGVHECPAWLWLLLSLLSLPLGLPVLGAPPRLICDSRVLERYLLEAKEAENITTGCAEHC
SLNENITVPDTKVNFYAWKRMEVGQQAVEVWQGLALLSEAVLRGQALLVNSSQPWEPLQL HVDKAVSGLRSLTTLLRALGAQKEAISPPDAASAAPLRTITADTFRKLFRVYSNFLRGKL KLYTGEACRTGDR Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| ADReCS ID | BADD_A06316 | |||||
| HIT2.0 ID | T10OIU | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 5 Clinical Trial Drugs | + | ||||
| 1 | LKA651 | Drug Info | Phase 2 | Diabetic macular edema | [2] | |
| 2 | MK-2578 | Drug Info | Phase 2 | Anemia | [3] | |
| 3 | Erythropoietin-transfected autologous cell therapy | Drug Info | Phase 1/2 | Anemia | [4] | |
| 4 | GC-1113 | Drug Info | Phase 1 | Anemia | [5] | |
| 5 | Long-acting erythropoietin conjugate | Drug Info | Phase 1 | Anemia | [6] | |
| Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
| 1 | FC EPO | Drug Info | Discontinued in Phase 1 | Anemia | [7] | |
| 2 | GLY-515n | Drug Info | Terminated | Cerebrovascular ischaemia | [8] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Agonist | [+] 2 Agonist drugs | + | ||||
| 1 | MK-2578 | Drug Info | [1] | |||
| 2 | FC EPO | Drug Info | [13] | |||
| Modulator | [+] 4 Modulator drugs | + | ||||
| 1 | Erythropoietin-transfected autologous cell therapy | Drug Info | [10] | |||
| 2 | GC-1113 | Drug Info | [11] | |||
| 3 | Long-acting erythropoietin conjugate | Drug Info | [12] | |||
| 4 | GLY-515n | Drug Info | [14] | |||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating Transcription Factors | ||||||
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 5 KEGG Pathways | + | ||||
| 1 | Cytokine-cytokine receptor interaction | |||||
| 2 | HIF-1 signaling pathway | |||||
| 3 | PI3K-Akt signaling pathway | |||||
| 4 | Jak-STAT signaling pathway | |||||
| 5 | Hematopoietic cell lineage | |||||
| PID Pathway | [+] 4 PID Pathways | + | ||||
| 1 | HIF-2-alpha transcription factor network | |||||
| 2 | Signaling events mediated by Stem cell factor receptor (c-Kit) | |||||
| 3 | EPO signaling pathway | |||||
| 4 | HIF-1-alpha transcription factor network | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Regulation of gene expression by Hypoxia-inducible Factor | |||||
| WikiPathways | [+] 4 WikiPathways | + | ||||
| 1 | EPO Receptor Signaling | |||||
| 2 | Hematopoietic Stem Cell Differentiation | |||||
| 3 | Differentiation Pathway | |||||
| 4 | Regulation of Hypoxia-inducible Factor (HIF) by Oxygen | |||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Merck ditches biogeneric. Nat Biotechnol. 2010 Jul;28(7):636. | |||||
| REF 2 | ClinicalTrials.gov (NCT03927690) Multiple Dose Safety and Efficacy of LKA651 in Patients With Diabetic Macular Edema. U.S. National Institutes of Health. | |||||
| REF 3 | ClinicalTrials.gov (NCT00968617) A Study of MK2578 in Patients With Chronic Kidney Disease Who Are Not on Dialysis (2578-002). U.S. National Institutes of Health. | |||||
| REF 4 | ClinicalTrials.gov (NCT00542568) Safety and Efficacy of Sustained Erythropoietin Therapy. U.S. National Institutes of Health. | |||||
| REF 5 | ClinicalTrials.gov (NCT01363934) To Evaluate the Safety, Tolerability, and Pharmacokinetics/Pharmacodynamics of Erythropoietin. U.S. National Institutes of Health. | |||||
| REF 6 | ClinicalTrials.gov (NCT01030315) A Study of HM10760A (Long-acting Erythropoietin) in Healthy Adult Caucasian and Japanese Subjects. U.S. National Institutes of Health. | |||||
| REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027346) | |||||
| 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 800027536) | |||||
| REF 9 | Clinical pipeline report, company report or official report of Novartis. | |||||
| REF 10 | Mesenchymal stromal cells engineered to express erythropoietin induce anti-erythropoietin antibodies and anemia in allorecipients. Mol Ther. 2009 Feb;17(2):369-72. | |||||
| REF 11 | A long-acting erythropoietin fused with noncytolytic human Fc for the treatment of anemia. Arch Pharm Res. 2012 May;35(5):757-9. | |||||
| REF 12 | Company report (Pharmexcil) | |||||
| REF 13 | Detection of EPO-Fc fusion protein in human blood: screening and confirmation protocols for sports drug testing. Drug Test Anal. 2012 Nov;4(11):818-29. | |||||
| REF 14 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027536) | |||||
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