Target Information

Target General Infomation
Target ID
T16156
Former ID
TTDS00524
Target Name
Thrombopoietin Receptor
Gene Name
MPL
Synonyms
C-mpl; CD110 antigen; Myeloproliferative leukemia protein; TPO-R; TPOR; MPL
Target Type
Successful
Disease Acute myeloid leukemia [ICD9: 205; ICD10: C92.0]
Bone marrow transplantation [ICD9: 279.5, 996; ICD10: D89.8, T86]
Chronic liver disease; HCV induced thrombocytopaenia [ICD9: 287.3, 287.4, 287.5; ICD10: D69.6, P61.0]
Chemotherapy-induced thrombocytopenia; Myelodysplastic syndromes [ICD9: 238.7, 287.3, 287.4, 287.5; ICD10: D46, D69.6, P61.0]
Idiopathic thrombocytopenic purpura [ICD9: 287.31; ICD10: D69.3]
Immune thrombocytopenic purpura; Idiopathic thrombocytopenic purpura [ICD9: 287.31; ICD10: D69.3]
Liver disease [ICD9: 570-574; ICD10: K70-K77]
Myocardial infarction; Thrombotic stroke [ICD9:410, 434.91; ICD10: I21, I22, I61-I63]
Oncology-related thrombocytopaenia [ICD9: 287.3, 287.4, 287.5; ICD10: D69.6, P61.0]
Sarcoma; Idiopathic thrombocytopenic purpura [ICD9: 287.31; ICD10: D69.3]
Thrombocytopenic purpura [ICD10: D69]
Thrombocytopenia [ICD9: 287.3, 287.4, 287.5; ICD10: D69.6, P61.0]
Unspecified [ICD code not available]
Function
Receptor for thrombopoietin. May represent a regulatory molecule specific for TPO-R-dependent immune responses.
BioChemical Class
Type I cytokine receptor
Target Validation
T16156
UniProt ID
P40238
Sequence
MPSWALFMVTSCLLLAPQNLAQVSSQDVSLLASDSEPLKCFSRTFEDLTCFWDEEEAAPS
GTYQLLYAYPREKPRACPLSSQSMPHFGTRYVCQFPDQEEVRLFFPLHLWVKNVFLNQTR
TQRVLFVDSVGLPAPPSIIKAMGGSQPGELQISWEEPAPEISDFLRYELRYGPRDPKNST
GPTVIQLIATETCCPALQRPHSASALDQSPCAQPTMPWQDGPKQTSPSREASALTAEGGS
CLISGLQPGNSYWLQLRSEPDGISLGGSWGSWSLPVTVDLPGDAVALGLQCFTLDLKNVT
CQWQQQDHASSQGFFYHSRARCCPRDRYPIWENCEEEEKTNPGLQTPQFSRCHFKSRNDS
IIHILVEVTTAPGTVHSYLGSPFWIHQAVRLPTPNLHWREISSGHLELEWQHPSSWAAQE
TCYQLRYTGEGHQDWKVLEPPLGARGGTLELRPRSRYRLQLRARLNGPTYQGPWSSWSDP
TRVETATETAWISLVTALHLVLGLSAVLGLLLLRWQFPAHYRRLRHALWPSLPDLHRVLG
QYLRDTAALSPPKATVSDTCEEVEPSLLEILPKSSERTPLPLCSSQAQMDYRRLQPSCLG
TMPLSVCPPMAESGSCCTTHIANHSYLPLSYWQQP
Drugs and Mode of Action
Drug(s) Eltrombopag Drug Info Approved Thrombocytopenia [529941], [541996]
PROMACTA Drug Info Approved Thrombocytopenia [543468]
Revolade/Promacta Drug Info Approved Idiopathic thrombocytopenic purpura [538590]
Romiplostim Drug Info Approved Thrombocytopenia [529941], [542005]
E5501 Drug Info Phase 3 Idiopathic thrombocytopenic purpura [523622]
Eltrombopag Drug Info Phase 3 Idiopathic thrombocytopenic purpura [536737], [541996]
Revolade/Promacta Drug Info Phase 3 Chronic liver disease; HCV induced thrombocytopaenia [538590]
LGD-4665 Drug Info Phase 2 Immune thrombocytopenic purpura; Idiopathic thrombocytopenic purpura [536737]
Revolade/Promacta Drug Info Phase 2 Oncology-related thrombocytopaenia [538590]
Romiplostim Drug Info Phase 2 Chemotherapy-induced thrombocytopenia; Myelodysplastic syndromes [536737], [542005]
S-888711 Drug Info Phase 2 Liver disease [522925]
BVI-007 Drug Info Phase 1 Myocardial infarction; Thrombotic stroke [548615]
NIP-004 Drug Info Phase 1 Thrombocytopenia [548679]
RhTPO Drug Info Discontinued in Phase 3 Sarcoma; Idiopathic thrombocytopenic purpura [536737]
Thrombopoietin Drug Info Discontinued in Phase 3 Thrombocytopenia [468146], [547808]
Totrombopag Drug Info Discontinued in Phase 1 Thrombocytopenia [536737]
Promegapoietin Drug Info Terminated Bone marrow transplantation [546819]
Agonist AS-1670542 Drug Info [543468]
E5501 Drug Info [543468]
Eltrombopag Drug Info [536737]
LGD-4665 Drug Info [536737]
NIP-004 Drug Info [528043]
PROMACTA Drug Info [543468]
Revolade/Promacta Drug Info [550963]
RhTPO Drug Info [536737]
S-888711 Drug Info [544267]
SB-559457 Drug Info [543468]
STS-T4 Drug Info [543468]
Thrombopoietin Drug Info [535128]
Totrombopag Drug Info [550963]
Antagonist BVI-007 Drug Info [543468]
HL-034 Drug Info [543468]
Modulator Non-peptide TPO mimics Drug Info [543468]
Promegapoietin Drug Info [556264]
RI-TPO Drug Info [1572605]
Romiplostim Drug Info [529941]
SE-ET-TP020d Drug Info [1572605]
ThromboMer Drug Info [543468]
thrombopoietin antagonist Drug Info [1572605]
thrombopoietin mimetic antibodies Drug Info [1572605]
TPO therapy program, thrombocytopenia Drug Info [543468]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Cytokine-cytokine receptor interaction
Jak-STAT signaling pathway
WikiPathways Platelet Aggregation (Plug Formation)
References
Ref 468146(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. (Ligand id: 5063).
Ref 522925ClinicalTrials.gov (NCT01054443) A Study to Investigate the Efficacy and Safety of S-888711 Tablets Administered to Adult Subjects With Immune Thrombocytopenia (ITP). U.S. National Institutes of Health.
Ref 523622ClinicalTrials.gov (NCT01433978) A Phase 3, Multicenter, Randomized, Double-blind, Active-controlled, Parallel-group Trial With an Open-label Extension Phase to Evaluate the Efficacy and Safety of Oral E5501 Versus Eltrombopag, in Adults With Chronic Immune Thrombocytopenia (Idiopathic Thrombocytopenic Purpura). U.S. National Institutes of Health.
Ref 5299412008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
Ref 536737Emerging drugs for idiopathic thrombocytopenic purpura in adults. Expert Opin Emerg Drugs. 2008 Jun;13(2):237-54.
Ref 538590FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022291.
Ref 541996(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. (Ligand id: 6961).
Ref 542005(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. (Ligand id: 6974).
Ref 543468(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: 1722).
Ref 546819Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010450)
Ref 547808Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019480)
Ref 548615Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027040)
Ref 548679Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027636)
Ref 528043A novel nonpeptidyl human c-Mpl activator stimulates human megakaryopoiesis and thrombopoiesis. Blood. 2006 Jun 1;107(11):4300-7. Epub 2006 Feb 16.
Ref 5299412008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
Ref 535128Technology evaluation: thrombopoietin, Genentech/Pharmacia & Upjohn. Curr Opin Mol Ther. 2000 Apr;2(2):211-5.
Ref 536737Emerging drugs for idiopathic thrombocytopenic purpura in adults. Expert Opin Emerg Drugs. 2008 Jun;13(2):237-54.
Ref 543468(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: 1722).
Ref 544267Defective regulatory B-cell compartment in patients with immune thrombocytopenia. Blood. 2012 October 18; 120(16): 3318-3325.
Ref 550963Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 1572605The ChEMBL database in 2017.

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