Property Summary

NCBI Gene PubMed Count 46
Grant Count 64
R01 Count 54
Funding $4,628,168.97
PubMed Score 42.98
PubTator Score 59.36

Knowledge Summary

Patent (5,561)

Expression

  Differential Expression (12)

Synonym

Accession Q15119 A8K3A7 B3KNW0 Q6P515 Q9BS05
Symbols PDHK2
PDKII

Gene

PANTHER Protein Class (3)

PDB

2BTZ   2BU2   2BU5   2BU6   2BU7   2BU8   4MP2   4MP7   4MPC   4MPE   4MPN   4V25   4V26  

Gene RIF (26)

PMID Text
26909964 The data demonstrate potential roles of PDK2 and ABCG2 polymorphisms in the metabolic phenotypes of Tibetan gout patients.
26607904 High glycolysis and PDK2 overexpression are closely linked to cisplatin resistance in head and neck cancer cells, which can be reversed by PDK2 nhibition.
26416963 The findings of the present study reveal a novel survival pathway that functionally couples the unique glycolytic phenotype in cancer cells to hypoxia resistance via a PDK2-dependent mechanism that switches Bnip3 from cell death to survival.
25976231 both PDK 1 and 2 isoforms are overexpressed in cutaneous melanoma compared to nevi, this expression being associated with the expression of the mTOR pathway effectors and independent of the BRAF mutational status
24356970 The final compound of this series, 2-[(2,4-dihydroxyphenyl)sulfonyl]isoindoline-4,6-diol, designated PS10, inhibits all four PDK isoforms with IC50 = 0.8 muM for PDK2.
23376776 we for the first time demonstrated that a low-nutrient condition drives cancer cells to utilize glycolysis to produce ATP, and this increases the Warburg effect through a novel mechanism involving ROS/AMPK-dependent activation of PDK.
23300259 Germline mutations in PKD2 gene is associated with autosomal-dominant polycystic kidney disease.
22910903 Inactivation of pyruvate dehydrogenase kinase 2 by mitochondrial reactive oxygen species.
22614004 Mitochondrial activation by inhibition of PDKII suppresses HIF1a signaling and angiogenesis in cancer.
22123926 Results established that wild-type p53 prevents manifestation of the Warburg effect by controlling Pdk2. These findings elucidate a new mechanism by which p53 suppresses tumorigenesis acting at the level of cancer cell metabolism.
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AA Sequence

MRWVWALLKNASLAGAPKYIEHFSKFSPSPLSMKQFLDFGSSNACEKTSFTFLRQELPVRLANIMKEINL      1 - 70
LPDRVLSTPSVQLVQSWYVQSLLDIMEFLDKDPEDHRTLSQFTDALVTIRNRHNDVVPTMAQGVLEYKDT     71 - 140
YGDDPVSNQNIQYFLDRFYLSRISIRMLINQHTLIFDGSTNPAHPKHIGSIDPNCNVSEVVKDAYDMAKL    141 - 210
LCDKYYMASPDLEIQEINAANSKQPIHMVYVPSHLYHMLFELFKNAMRATVESHESSLILPPIKVMVALG    211 - 280
EEDLSIKMSDRGGGVPLRKIERLFSYMYSTAPTPQPGTGGTPLAGFGYGLPISRLYAKYFQGDLQLFSME    281 - 350
GFGTDAVIYLKALSTDSVERLPVYNKSAWRHYQTIQEAGDWCVPSTEPKNTSTYRVS                 351 - 407
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Text Mined References (51)

PMID Year Title
26909964 2016 PDK2 and ABCG2 genes polymorphisms are correlated with blood glucose levels and uric acid in Tibetan gout patients.
26607904 2016 Activation of mitochondrial oxidation by PDK2 inhibition reverses cisplatin resistance in head and neck cancer.
26416963 2015 PDK2-mediated alternative splicing switches Bnip3 from cell death to cell survival.
25976231 2015 Overexpression of pyruvate dehydrogenase kinase supports dichloroacetate as a candidate for cutaneous melanoma therapy.
24356970 2014 Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket.
24275569 2014 An enzyme assisted RP-RPLC approach for in-depth analysis of human liver phosphoproteome.
23376776 2013 Nutrient deprivation induces the Warburg effect through ROS/AMPK-dependent activation of pyruvate dehydrogenase kinase.
23300259 2013 Epidemiology of autosomal-dominant polycystic kidney disease: an in-depth clinical study for south-western Germany.
22910903 2012 Inactivation of pyruvate dehydrogenase kinase 2 by mitochondrial reactive oxygen species.
22614004 2013 Mitochondrial activation by inhibition of PDKII suppresses HIF1a signaling and angiogenesis in cancer.
More...