Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTIHYA4)

DTT Name Thrombopoietin receptor (MPL)
Synonyms TPOR; TPO-R; Proto-oncogene c-Mpl; Myeloproliferative leukemia protein; CD110 antigen; CD110; C-mpl
Gene Name MPL
DTT Type
Successful target
 [1]
Related Disease
Thrombocytopenia [ICD-11: 3B64]
BioChemical Class
Cytokine receptor
UniProt ID
TPOR_HUMAN
TTD ID
T16156
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPSWALFMVTSCLLLAPQNLAQVSSQDVSLLASDSEPLKCFSRTFEDLTCFWDEEEAAPS
GTYQLLYAYPREKPRACPLSSQSMPHFGTRYVCQFPDQEEVRLFFPLHLWVKNVFLNQTR
TQRVLFVDSVGLPAPPSIIKAMGGSQPGELQISWEEPAPEISDFLRYELRYGPRDPKNST
GPTVIQLIATETCCPALQRPHSASALDQSPCAQPTMPWQDGPKQTSPSREASALTAEGGS
CLISGLQPGNSYWLQLRSEPDGISLGGSWGSWSLPVTVDLPGDAVALGLQCFTLDLKNVT
CQWQQQDHASSQGFFYHSRARCCPRDRYPIWENCEEEEKTNPGLQTPQFSRCHFKSRNDS
IIHILVEVTTAPGTVHSYLGSPFWIHQAVRLPTPNLHWREISSGHLELEWQHPSSWAAQE
TCYQLRYTGEGHQDWKVLEPPLGARGGTLELRPRSRYRLQLRARLNGPTYQGPWSSWSDP
TRVETATETAWISLVTALHLVLGLSAVLGLLLLRWQFPAHYRRLRHALWPSLPDLHRVLG
QYLRDTAALSPPKATVSDTCEEVEPSLLEILPKSSERTPLPLCSSQAQMDYRRLQPSCLG
TMPLSVCPPMAESGSCCTTHIANHSYLPLSYWQQP
Function May represent a regulatory molecule specific for TPO-R-dependent immune responses. Receptor for thrombopoietin that acts as a primary regulator of megakaryopoiesis and platelet production.
KEGG Pathway
( )
( )
Reactome Pathway
Platelet Aggregation (Plug Formation) (R-HSA-76009 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
5 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
As-1670542 DMV05SW Thrombocytopenia 3B64 Approved [2]
Eltrombopag DMOGFIX Thrombocytopenia 3B64 Approved [1]
Lusutrombopag DMH6IKO Thrombocytopenia 3B64 Approved [3]
Revolade/Promacta DM8LRU2 Idiopathic thrombocytopenic purpura 3B64.10 Approved [4]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [5]
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3 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
LGD-4665 DM9T8A2 Immune thrombocytopenic purpura 3B64.13 Phase 2 [1]
BVI-007 DM43GPX Myocardial infarction BA41-BA43 Phase 1 [2]
NIP-004 DM0PYEQ Thrombocytopenia 3B64 Phase 1 [6]
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3 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
RhTPO DMCV0BZ Idiopathic thrombocytopenic purpura 3B64.10 Discontinued in Phase 3 [1]
Totrombopag DM6SUDC Thrombocytopenia 3B64 Discontinued in Phase 1 [4]
Promegapoietin DMS4FG0 Bone marrow transplantation QB63.6 Terminated [7]
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7 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
HL-034 DMMW0OF Discovery agent N.A. Investigative [2]
Non-peptide TPO mimics DMZ2DSK Thrombocytopenia 3B64 Investigative [2]
RI-TPO DMJD3WY Discovery agent N.A. Investigative [8]
SB-559457 DM0OLYF Acute myeloid leukaemia 2A60 Investigative [2]
SE-ET-TP020d DMCQNT9 Thrombocytopenia 3B64 Investigative [8]
STS-T4 DM5BATX Thrombocytopenia 3B64 Investigative [2]
ThromboMer DMRVXH7 Thrombocytopenia 3B64 Investigative [2]
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⏷ Show the Full List of 7 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Sarcoma 2C82 Muscle tissue 1.03E-38 -0.17 -0.79
Thrombocytopenia 3B64 Whole blood 8.96E-01 0.07 0.28
Acute myelocytic leukaemia 2C82 Bone marrow 2.61E-06 0.1 0.45
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References

1 Emerging drugs for idiopathic thrombocytopenic purpura in adults. Expert Opin Emerg Drugs. 2008 Jun;13(2):237-54.
2 URL: 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).
3 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
4 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
5 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
6 A novel nonpeptidyl human c-Mpl activator stimulates human megakaryopoiesis and thrombopoiesis. Blood. 2006 Jun 1;107(11):4300-7.
7 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
8 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.