Target Information

Target General Infomation
Target ID
T65889
Former ID
TTDI02110
Target Name
Pyruvate kinase M2
Gene Name
PKM
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
Target Type
Clinical Trial
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}.
BioChemical Class
Kinase
UniProt ID
P14618
EC Number
EC 2.7.1.40
Sequence
MSKPHSEAGTAFIQTQQLHAAMADTFLEHMCRLDIDSPPITARNTGIICTIGPASRSVET
LKEMIKSGMNVARLNFSHGTHEYHAETIKNVRTATESFASDPILYRPVAVALDTKGPEIR
TGLIKGSGTAEVELKKGATLKITLDNAYMEKCDENILWLDYKNICKVVEVGSKIYVDDGL
ISLQVKQKGADFLVTEVENGGSLGSKKGVNLPGAAVDLPAVSEKDIQDLKFGVEQDVDMV
FASFIRKASDVHEVRKVLGEKGKNIKIISKIENHEGVRRFDEILEASDGIMVARGDLGIE
IPAEKVFLAQKMMIGRCNRAGKPVICATQMLESMIKKPRPTRAEGSDVANAVLDGADCIM
LSGETAKGDYPLEAVRMQHLIAREAEAAIYHLQLFEELRRLAPITSDPTEATAVGAVEAS
FKCCSGAIIVLTKSGRSAHQVARYRPRAPIIAVTRNPQTARQAHLYRGIFPVLCKDPVQE
AWAEDVDLRVNFAMNVGKARGFFKKGDVVIVLTGWRPGSGFTNTMRVVPVP
Drugs and Mode of Action
Drug(s) CAP-232 Drug Info Phase 2a Refractory renal cell carcinoma [522404]
CAP-232 Drug Info Phase 2 Pain; Solid tumours [522404]
Modulator CAP-232 Drug Info [1572591]
References
Ref 522404ClinicalTrials.gov (NCT00735332) Efficacy Study of TLN-232 in Patients With Recurring Metastatic Melanoma. U.S. National Institutes of Health.
Ref
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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