Property Summary

NCBI Gene PubMed Count 236
Grant Count 146
R01 Count 75
Funding $18,124,002.82
PubMed Score 1313.47
PubTator Score 447.47

Knowledge Summary

Patent (72,928)

Expression

  Differential Expression (26)

Synonym

Accession P14618 A6NFK3 B2R5N8 B3KRY0 B4DFX8 B4DUU6 P14786 Q53GK4 Q96E76 Q9BWB5 Q9UCV6 Q9UPF2
Symbols PK3
TCB
OIP3
PKM2
CTHBP
THBP1
HEL-S-30

Gene

PKM

PDB

1T5A   1ZJH   3BJF   3BJT   3G2G   3GQY   3GR4   3H6O   3ME3   3SRD   3SRF   3SRH   3U2Z   4B2D   4FXF   4FXJ   4G1N   4JPG   4QG6   4QG8   4QG9   4QGC   4RPP   4WJ8   4YJ5  

  TechDev Info (1)

Gary Johnson Kinome profile via MIB/MS Technology

MLP Assay (23)

AID Type Active / Inconclusive / Inactive Description
954 confirmatory 0 / 16 / 1263 qHTS Assay for Activators of Human Muscle Pyruvate Kinase
958 confirmatory 26 / 66 / 1187 qHTS Assay for Inhibitors of Human Muscle Pyruvate Kinase
1540 confirmatory 123 / 34 / 8 Secondary assay for Activators of Human Pyruvate Kinase M2 isoform
1542 confirmatory 0 / 86 / 45 Secondary assay for Activators of Human Pyruvate Kinase M1 isoform
1631 confirmatory 892 / 3758 / 259866 qHTS Assay for Activators of Human Muscle isoform 2 Pyruvate Kinase
1634 confirmatory 154 / 1528 / 262834 qHTS Assay for Inhibitors of Human Muscle isoform 2 Pyruvate Kinase
1751 confirmatory 94 / 8 / 23 Confirmation Concentration-Response Assay for Activators of Human Muscle isoform 2 Pyruvate Kinase
1780 confirmatory 0 / 0 / 113 Confirmation Concentration-Response Assay for Activators of Human Muscle isoform 1 Pyruvate Kinase
2095 summary 6 / 0 / 0 qHTS Assay for Activators of Human Muscle isoform 2 Pyruvate Kinase: Summary
2263 confirmatory 24 / 6 / 24 Confirmation Concentration-Response Assay for Inhibitors of Human Muscle isoform 2 Pyruvate Kinase
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Gene RIF (186)

PMID Text
27012213 PKM1 has a role in resistance to anti-cancer drugs
26989901 Multivariable analysis showed that combined expression of pyruvate kinase type M2 and lactate dehydrogenase A was an independent poor prognostic marker for survival.
26981025 Data indicate that combined use of immunochemical test for hemoglobin (FIT) and fecal M2-type pyruvate kinase (M2-PK) permitted the identification of 18 more neoplasm (25%).
26975375 Ubiquitylation of PKM2 by parkin does not affect its stability but decreases its enzymatic activity.
26926996 PKM2 serves a previously unidentified role as a molecular integrator of metabolic dysfunction, oxidative stress and tissue inflammation and represents a novel therapeutic target in cardiovascular disease.
26874904 These results define a novel mechanism by which PKM2 regulates glioma cell growth, and also define a novel set of potential therapeutic targets along the PKM2-HuR-p27 pathway
26787900 demonstrate that PKM2 deacetylation is integral to SIRT6-mediated tumor suppression and inhibition of metastasis. Additionally, reduced SIRT6 levels correlate with elevated nuclear acetylated PKM2 levels in increasing grades of hepatocellular carcinoma
26780311 Mammalian photoreceptors contain dimeric and tetrameric PKM2 and LDH-A. This is consistent with the ability to switch between energy production and biosynthesis like a proliferating tissue, possibly due to demands of opsin synthesis.
26739387 in hypoxic pancreatic tumors PKM2 interferes both with NF-kappaB/p65 and HIF-1alpha activation that ultimately triggers VEGF-A secretion and subsequent blood vessel formation.
26702927 PKM2/TG2 interplay plays an important role in the regulation of autophagy in particular under cellular stressful conditions such as those displayed by cancer cells.
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AA Sequence

MSKPHSEAGTAFIQTQQLHAAMADTFLEHMCRLDIDSPPITARNTGIICTIGPASRSVETLKEMIKSGMN      1 - 70
VARLNFSHGTHEYHAETIKNVRTATESFASDPILYRPVAVALDTKGPEIRTGLIKGSGTAEVELKKGATL     71 - 140
KITLDNAYMEKCDENILWLDYKNICKVVEVGSKIYVDDGLISLQVKQKGADFLVTEVENGGSLGSKKGVN    141 - 210
LPGAAVDLPAVSEKDIQDLKFGVEQDVDMVFASFIRKASDVHEVRKVLGEKGKNIKIISKIENHEGVRRF    211 - 280
DEILEASDGIMVARGDLGIEIPAEKVFLAQKMMIGRCNRAGKPVICATQMLESMIKKPRPTRAEGSDVAN    281 - 350
AVLDGADCIMLSGETAKGDYPLEAVRMQHLIAREAEAAIYHLQLFEELRRLAPITSDPTEATAVGAVEAS    351 - 420
FKCCSGAIIVLTKSGRSAHQVARYRPRAPIIAVTRNPQTARQAHLYRGIFPVLCKDPVQEAWAEDVDLRV    421 - 490
NFAMNVGKARGFFKKGDVVIVLTGWRPGSGFTNTMRVVPVP                                 491 - 531
//

Text Mined References (256)

PMID Year Title
27012213 2016 PKM1 is involved in resistance to anti-cancer drugs.
26989901 2016 Pyruvate Kinase M2 and Lactate Dehydrogenase A Are Overexpressed in Pancreatic Cancer and Correlate with Poor Outcome.
26981025 2016 Colorectal cancer detection in an asymptomatic population: fecal immunochemical test for hemoglobin vs. fecal M2-type pyruvate kinase.
26975375 2016 Parkin Regulates the Activity of Pyruvate Kinase M2.
26926996 2016 The glycolytic enzyme PKM2 bridges metabolic and inflammatory dysfunction in coronary artery disease.
26874904 2016 PKM2 uses control of HuR localization to regulate p27 and cell cycle progression in human glioblastoma cells.
26787900 2016 SIRT6 deacetylates PKM2 to suppress its nuclear localization and oncogenic functions.
26780311 2016 M-Type Pyruvate Kinase Isoforms and Lactate Dehydrogenase A in the Mammalian Retina: Metabolic Implications.
26739387 2016 PKM2 promotes tumor angiogenesis by regulating HIF-1? through NF-?B activation.
26702927 2015 The transglutaminase type 2 and pyruvate kinase isoenzyme M2 interplay in autophagy regulation.
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