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Thrombopoietin receptor

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Target id: 1722

Nomenclature: Thrombopoietin receptor

Family: Prolactin receptor family

Contents:

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
Alphafold P40238 (Hs), Q08351 (Mm)
CATH/Gene3D 2.60.40.10
ChEMBL Target CHEMBL1864 (Hs), CHEMBL1075309 (Mm)
DrugBank Target P40238 (Hs)
Ensembl Gene ENSG00000117400 (Hs), ENSMUSG00000006389 (Mm), ENSRNOG00000028377 (Rn)
Entrez Gene 4352 (Hs), 17480 (Mm), 366455 (Rn)
Human Protein Atlas ENSG00000117400 (Hs)
KEGG Gene hsa:4352 (Hs), mmu:17480 (Mm), rno:366455 (Rn)
OMIM 159530 (Hs)
Orphanet ORPHA123465 (Hs)
Pharos P40238 (Hs)
UniProtKB P40238 (Hs), Q08351 (Mm)
Wikipedia MPL (Hs)
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 Approved drug Hs Agonist - -
⤷
Immuno Process Associations
Immuno Process:  Immune regulation
Immuno Process:  Immune system development
Immuno Process:  Cytokine production & signalling
Immuno Process:  Chemotaxis & migration
Immuno Process:  Cellular signalling
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 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1722.