Target Information
Target General Infomation | |||||
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Target ID |
T65889
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Former ID |
TTDI02110
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Target Name |
Pyruvate kinase M2
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Gene Name |
PKM
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Synonyms |
CTHBP; Cytosolic thyroid hormone-binding protein; OIP-3; Opa-interacting protein 3; Pyruvate kinase 2/3; Pyruvate kinase isozymes M1/M2; Pyruvate kinase muscle isozyme; THBP1; Thyroid hormone-binding protein 1; Tumor M2-PK; p58; PKM
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Target Type |
Clinical Trial
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Disease | Pain; Solid tumours [ICD9:338, 356.0, 356.8, 780, 140-199, 210-229; ICD10: G64, G90.0, R52, G89, C00-D48] | ||||
Refractory renal cell carcinoma [ICD9: 189; ICD10: C64] | |||||
Function |
Glycolytic enzyme that catalyzes the transfer of a phosphoryl group from phosphoenolpyruvate (PEP) to ADP, generating ATP. Stimulates POU5F1-mediated transcriptional activation. Plays a general role in caspase independent cell death of tumor cells. The ratio betwween the highly active tetrameric form and nearly inactive dimeric form determines whether glucose carbons are channeled to biosynthetic processes or used for glycolytic ATP production. The transition between the 2 forms contributes to the control of glycolysis and is important for tumor cell proliferation and survival. {ECO:0000269|PubMed:17308100, ECO:0000269|PubMed:18191611, ECO:0000269|PubMed:21620138}.
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BioChemical Class |
Kinase
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UniProt ID | |||||
EC Number |
EC 2.7.1.40
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Sequence |
MSKPHSEAGTAFIQTQQLHAAMADTFLEHMCRLDIDSPPITARNTGIICTIGPASRSVET
LKEMIKSGMNVARLNFSHGTHEYHAETIKNVRTATESFASDPILYRPVAVALDTKGPEIR TGLIKGSGTAEVELKKGATLKITLDNAYMEKCDENILWLDYKNICKVVEVGSKIYVDDGL ISLQVKQKGADFLVTEVENGGSLGSKKGVNLPGAAVDLPAVSEKDIQDLKFGVEQDVDMV FASFIRKASDVHEVRKVLGEKGKNIKIISKIENHEGVRRFDEILEASDGIMVARGDLGIE IPAEKVFLAQKMMIGRCNRAGKPVICATQMLESMIKKPRPTRAEGSDVANAVLDGADCIM LSGETAKGDYPLEAVRMQHLIAREAEAAIYHLQLFEELRRLAPITSDPTEATAVGAVEAS FKCCSGAIIVLTKSGRSAHQVARYRPRAPIIAVTRNPQTARQAHLYRGIFPVLCKDPVQE AWAEDVDLRVNFAMNVGKARGFFKKGDVVIVLTGWRPGSGFTNTMRVVPVP |
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Drugs and Mode of Action | |||||
References |
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