Thrombopoietin receptor | Prolactin receptor family | IUPHAR/BPS Guide to PHARMACOLOGY

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Thrombopoietin receptor

Target not currently curated in GtoImmuPdb

Target id: 1722

Nomenclature: Thrombopoietin receptor

Family: Prolactin receptor family

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

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

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
eltrombopag Hs Agonist 7.4 pEC50 2
pEC50 7.4 (EC50 3.8x10-8 M) [2]
thrombopoietin {Sp: Human} Hs Agonist - -
romiplostim Hs Agonist - -
avatrombopag Hs Agonist - - 1
[1]
lusutrombopag Hs Agonist - - 3
[3]
Clinically-Relevant Mutations and Pathophysiology
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 01/08/2018. Accessed on 17/08/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1722.