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Thrombopoietin receptor

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Target not currently curated in GtoImmuPdb

Target id: 1722

Nomenclature: Thrombopoietin receptor

Family: Prolactin receptor family

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 635 1p34.2 MPL MPL proto-oncogene, thrombopoietin receptor
Mouse 1 625 4 54.61 cM Mpl myeloproliferative leukemia virus oncogene
Rat - - 5q36 Mpl MPL proto-oncogene, thrombopoietin receptor
Previous and Unofficial Names Click here for help
CD110 | MPL | Myeloproliferative leukemia protein | TPOR | MPL proto-oncogene, thrombopoietin receptor | MPL proto-oncogene
Database Links Click here for help
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Orphanet
Pharos
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
thrombopoietin {Sp: Human}

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
eltrombopag Small molecule or natural product Approved drug Primary target of this compound Hs Agonist 7.4 pEC50 2
pEC50 7.4 (EC50 3.8x10-8 M) [2]
thrombopoietin {Sp: Human} Peptide Ligand is endogenous in the given species Hs Agonist - -
romiplostim Peptide Approved drug Primary target of this compound Immunopharmacology Ligand Hs Agonist - -
avatrombopag Small molecule or natural product Approved drug Hs Agonist - - 1
[1]
lusutrombopag Small molecule or natural product Approved drug Primary target of this compound Hs Agonist - - 3
[3]
hetrombopag Small molecule or natural product Hs Agonist - -
Immuno Process Associations
Immuno Process:  Immune regulation
GO Annotations:  Associated to 6 GO processes, IEA only
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GO:0001780 neutrophil homeostasis IEA
GO:0035702 monocyte homeostasis IEA
GO:0050671 positive regulation of lymphocyte proliferation IEA
GO:1905221 positive regulation of platelet formation IEA
GO:1990959 eosinophil homeostasis IEA
GO:1990960 basophil homeostasis IEA
Immuno Process:  Immune system development
GO Annotations:  Associated to 3 GO processes, IEA only
GO:0030220 platelet formation IGI
GO:0060216 definitive hemopoiesis IMP
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GO:1905221 positive regulation of platelet formation IEA
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 3 GO processes
GO:0032642 regulation of chemokine production IMP
GO:0038163 thrombopoietin-mediated signaling pathway IDA
GO:0038164 thrombopoietin receptor activity IMP
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 3 GO processes
GO:0032642 regulation of chemokine production IMP
GO:0038163 thrombopoietin-mediated signaling pathway IDA
GO:0038164 thrombopoietin receptor activity IMP
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes, IEA only
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GO:0050671 positive regulation of lymphocyte proliferation IEA
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Congenital amegakaryocytic thrombocytopenia
OMIM: 604498
Orphanet: ORPHA3319
Disease:  Familial thrombocytosis
Description: A rare chronic myeloproliferative neoplasm (MPN) causing overproduction of platelets.
Synonyms: essential thrombocythaemia
hemorrhagic thrombocythemia
hereditary thrombocythemia
primary thrombocytosis
Disease Ontology: DOID:2224
Orphanet: ORPHA71493
Disease:  Myelofibrosis
Synonyms: Myelofibrosis with myeloid metaplasia [Orphanet: ORPHA824]
Disease Ontology: DOID:4971
OMIM: 254450
Orphanet: ORPHA824
Disease:  Polycythemia vera
Disease Ontology: DOID:8997
OMIM: 263300
Orphanet: ORPHA729
Disease:  Thrombocythemia 2; THCYT2
Synonyms: Essential thrombocythemia [Orphanet: ORPHA3318]
Essential thrombocytosis [Orphanet: ORPHA3318]
OMIM: 601977
Orphanet: ORPHA3318

References

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1. Fukushima-Shintani M, Suzuki K, Iwatsuki Y, Abe M, Sugasawa K, Hirayama F, Kawasaki T, Nakahata T. (2009) AKR-501 (YM477) a novel orally-active thrombopoietin receptor agonist. Eur. J. Haematol., 82 (4): 247-54. [PMID:19183407]

2. Marsilje TH, Alper PB, Lu W, Mutnick D, Michellys PY, He Y, Karanewsky DS, Chow D, Gerken A, Lao J et al.. (2008) Optimization of small molecule agonists of the thrombopoietin (Tpo) receptor derived from a benzo[a]carbazole hit scaffold. Bioorg. Med. Chem. Lett., 18 (19): 5259-62. [PMID:18783949]

3. Yoshida H, Yamada H, Nogami W, Dohi K, Kurino-Yamada T, Sugiyama K, Takahashi K, Gahara Y, Kitaura M, Hasegawa M et al.. (2018) Development of a new knock-in mouse model and evaluation of pharmacological activities of lusutrombopag, a novel, nonpeptidyl small-molecule agonist of the human thrombopoietin receptor c-Mpl. Exp. Hematol., 59: 30-39.e2. [PMID:29274361]

How to cite this page

Prolactin receptor family: Thrombopoietin receptor. Last modified on 07/02/2020. Accessed on 02/12/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1722.