Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT4LOT8)

DTT Name	Pyruvate kinase M2 (PKM)
Synonyms	p58; Tumor M2-PK; Thyroid hormone-binding protein 1; THBP1; Pyruvate kinase muscle isozyme; Pyruvate kinase isozymes M1/M2; Pyruvate kinase PKM; Pyruvate kinase 2/3; PKM2; PK3; PK2; Opa-interacting protein 3; OIP3; OIP-3; Cytosolic thyroid hormone-binding protein; CTHBP
Gene Name	PKM
DTT Type	Clinical trial target	[1]
BioChemical Class	Kinase
UniProt ID	KPYM_HUMAN
TTD ID	T65889
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
EC Number	EC 2.7.1.40
Sequence	MSKPHSEAGTAFIQTQQLHAAMADTFLEHMCRLDIDSPPITARNTGIICTIGPASRSVET LKEMIKSGMNVARLNFSHGTHEYHAETIKNVRTATESFASDPILYRPVAVALDTKGPEIR TGLIKGSGTAEVELKKGATLKITLDNAYMEKCDENILWLDYKNICKVVEVGSKIYVDDGL ISLQVKQKGADFLVTEVENGGSLGSKKGVNLPGAAVDLPAVSEKDIQDLKFGVEQDVDMV FASFIRKASDVHEVRKVLGEKGKNIKIISKIENHEGVRRFDEILEASDGIMVARGDLGIE IPAEKVFLAQKMMIGRCNRAGKPVICATQMLESMIKKPRPTRAEGSDVANAVLDGADCIM LSGETAKGDYPLEAVRMQHLIAREAEAAIYHLQLFEELRRLAPITSDPTEATAVGAVEAS FKCCSGAIIVLTKSGRSAHQVARYRPRAPIIAVTRNPQTARQAHLYRGIFPVLCKDPVQE AWAEDVDLRVNFAMNVGKARGFFKKGDVVIVLTGWRPGSGFTNTMRVVPVP
Function	Stimulates POU5F1-mediated transcriptional activation. Plays a general role in caspase independent cell death of tumor cells. The ratio between 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. Promotes in a STAT1-dependent manner, the expression of the immune checkpoint protein CD274 in ARNTL/BMAL1-deficient macrophages. Glycolytic enzyme that catalyzes the transfer of a phosphoryl group from phosphoenolpyruvate (PEP) to ADP, generating ATP.
KEGG Pathway	Glycolysis / Gluconeogenesis (hsa00010 ) Pyruvate metabolism (hsa00620 ) Metabolic pathways (hsa01100 ) Carbon metabolism (hsa01200 ) Biosynthesis of amino acids (hsa01230 ) Glucagon signaling pathway (hsa04922 ) Type II diabetes mellitus (hsa04930 ) Human papillomavirus infection (hsa05165 ) Viral carcinogenesis (hsa05203 ) Central carbon metabolism in cancer (hsa05230 )
Reactome Pathway	Glycolysis (R-HSA-70171 ) Neutrophil degranulation (R-HSA-6798695 )
BioCyc Pathway	MetaCyc:HS00906-MON

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This DTT

2 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CAP-232	DMR6LXM	Renal cell carcinoma	2C90	Phase 2a	[1]
TP-1454	DMBTL2M	Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]
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References

1	Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
2	Clinical pipeline report, company report or official report of Sumitomo Dainippon Pharma.