Affinage

PDK2

[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial · UniProt Q15119

Length
407 aa
Mass
46.2 kDa
Annotated
2026-06-10
47 papers in source corpus 17 papers cited in narrative 17 extracted findings
Cross-family judge vs UniProt: Affinage preferred faithfulness: 6/6 claims corpus-supported (100%)

Mechanistic narrative

Synthesis pass · prose summary of the discoveries below

PDK2 is a mitochondrial kinase that phosphorylates and inactivates the E1α subunit of the pyruvate dehydrogenase complex (PDC), throttling conversion of pyruvate to acetyl-CoA and shifting cells toward aerobic glycolysis (PMID:38778217). Genetic knockout studies establish PDK2 as the dominant regulator of PDC activity in the fed state, with loss raising PDC activity and lowering blood glucose, while combined PDK2/PDK4 deletion produces fasting hypoglycaemia and ketoacidosis (PMID:22360721). Its kinase activity is allosterically governed by binding to the L2 lipoyl domain of the PDC E2 subunit, a site stimulated by K+ ions and dependent on inorganic phosphate, which also promotes PDK2 tetramerization and renders the enzyme sensitive to lipoyl-site occupancy; pharmacological and structural work defines two distinct druggable pockets—an ATP-binding active site (AZD7545, diarylisoxazoles) and a lipoyl-group binding site (Nov3r, compound 8c)—that are conformationally coupled across an asymmetric PDK2 dimer (PMID:14641018, PMID:18220415, PMID:32444142). PDK2 expression is transcriptionally elevated by loss of wild-type p53, by glucocorticoid receptor binding to the PDK2 promoter, and by O-GlcNAc-stabilized c-Myc, in each case suppressing PDH-driven oxidative metabolism in cancer cells and neurons (PMID:22123926, PMID:38778217, PMID:37188779). Beyond the PDC, PDK2 phosphorylates the mitochondrial rhomboid protease PARL to restrain PINK1/PARKIN-dependent mitophagy (PMID:28178523) and phosphorylates the transcription factor FOXK2 at Thr13/Ser30 via its FHA domain, establishing a FOXK2–PDK2 positive feedback loop that sustains glycolysis (PMID:38734828). Through these activities PDK2 couples mitochondrial pyruvate flux to redox balance and pathological phenotypes, including tumor growth, ischemia/reperfusion injury via a PDK2-PDH-Nrf2 antioxidant axis, and RANKL-driven osteoclast differentiation and bone loss (PMID:33125772, PMID:34712383).

Mechanistic history

Synthesis pass · year-by-year structured walk · 13 steps
  1. 2003 High

    Established PDK2 as a tractable pharmacological target whose inhibition reactivates PDH and improves systemic glucose handling, defining the enzyme's metabolic switch role in vivo.

    Evidence In vitro PDH activity assay with the inhibitor AZD7545 (EC50 ~5.2 nM) and in vivo dosing in Wistar and obese Zucker rats

    PMID:14641018

    Open questions at the time
    • Does not resolve isoform selectivity of AZD7545 across PDK1-4
    • No structural basis for inhibition provided at this stage
  2. 2008 High

    Defined the allosteric architecture of PDK2 regulation by showing lipoyl-domain (L2/E2) binding, K+ and phosphate dependence, and a distinct lipoyl-group inhibitory pocket separate from the ATP site.

    Evidence Biochemical binding assays of PDHK2 with GST-L2, kinase activity assays, gel filtration for oligomeric state, ligand competition with Nov3r (IC50 ~7.8 nM)

    PMID:18220415

    Open questions at the time
    • Atomic structure of the two binding sites not yet resolved here
    • Physiological trigger for tetramer formation in vivo unclear
  3. 2011 Medium

    Connected PDK2 to tumor metabolism by identifying wild-type p53 as a direct transcriptional repressor whose loss elevates PDK2 and drives the Warburg effect.

    Evidence p53 knockdown/overexpression in cancer cells, Western blot for PDK2 and phospho-PDC, lactate measurement

    PMID:22123926

    Open questions at the time
    • Direct p53 binding element on PDK2 promoter not mapped
    • Single-lab transcriptional mechanism
  4. 2011 Medium

    Placed PDK2 in a redox-responsive feed-forward loop with HIF1α, showing carcinogen-induced ROS upregulates PDK2 to sustain glycolysis and HIF1α accumulation.

    Evidence PDK2 qRT-PCR/Western blot, PDH activity and lactate/pyruvate assays, HIF1α blots, DCA and N-acetylcysteine treatment in oral keratinocytes

    PMID:21283817

    Open questions at the time
    • Whether ROS acts on PDK2 transcription directly or via an intermediate is unresolved
    • Single cell-type context
  5. 2012 High

    Genetic knockout established PDK2 as the dominant physiological regulator of PDC in the fed state, distinguishing its role from PDK4's fasting dominance.

    Evidence Single and double PDK2/PDK4 knockout mice; PDC activity assays; blood glucose, insulin, ketone, and stable-isotope flux measurements

    PMID:22360721

    Open questions at the time
    • Tissue-specific contributions not dissected
    • Does not address non-PDC substrate functions in vivo
  6. 2017 Medium

    Extended PDK2 substrate scope beyond the PDC by identifying PARL phosphorylation as a link between mitochondrial metabolism and mitophagy.

    Evidence Co-IP, phosphorylation assays, PARL cleavage Western blot, mitophagy reporters under mitochondrial stress

    PMID:28178523

    Open questions at the time
    • Phosphosite on PARL not pinpointed
    • Single-lab finding without reciprocal validation
  7. 2019 Medium

    Implicated PDK2 in coupling glycolytic phenotype to hypoxia/apoptosis resistance through Bnip3 alternative splicing.

    Evidence PDK2 inhibition (siRNA/DCA), RT-PCR isoform analysis, mitochondrial membrane potential and cell-death assays in Panc-1 cells

    PMID:26416963

    Open questions at the time
    • Mechanism linking a mitochondrial kinase to nuclear splicing not defined
    • No direct splicing-factor target identified
  8. 2020 High

    Provided structural proof of two coupled drug-binding pockets and an asymmetric PDK2 dimer, rationalizing allosteric inhibition.

    Evidence X-ray co-crystal structures with compound 8c (lipoyl site) and diarylisoxazoles GM10030/GM67520 (ATP site); ITC binding validation

    PMID:32444142

    Open questions at the time
    • Conformational coupling shown structurally but not kinetically dissected
    • Dimer asymmetry functional consequence in vivo unknown
  9. 2020 Medium

    Linked PDK2 activity to RANKL-driven osteoclastogenesis and bone homeostasis, broadening its physiological role beyond glucose metabolism.

    Evidence PDK2 knockout mice and AZD7545 inhibition, ovariectomy model, CREB/c-FOS/NFATc1 blots, osteoclast differentiation assays

    PMID:33125772

    Open questions at the time
    • How PDH/metabolic flux feeds into CREB/c-FOS signaling not mechanistically resolved
    • Single-lab study
  10. 2021 Medium

    Defined a PDK2-PDH-Nrf2 antioxidant axis governing oxidative stress and blood-brain barrier integrity in ischemia/reperfusion.

    Evidence MCAO and OGD models, DCA inhibition, Nrf2/HO-1 blots, ML385 Nrf2-inhibitor rescue

    PMID:34712383

    Open questions at the time
    • Reliance on pharmacological DCA rather than genetic PDK2 loss
    • Direct vs metabolic-flux-mediated Nrf2 induction not separated
  11. 2023 Medium

    Identified glucocorticoid receptor as a direct transcriptional driver of PDK2 in neurons, suppressing oxidative phosphorylation in response to glucocorticoids.

    Evidence ChIP of GR at PDK2 promoter, PDK2 knockdown, PDH phosphorylation blots, U-13C glucose tracing, in vivo silencing with behavioral readout

    PMID:37188779

    Open questions at the time
    • GR binding element sequence not defined
    • Single-lab neuronal context
  12. 2024 Medium

    Revealed a c-Myc–PDK2 transcriptional input controlled by O-GlcNAcylation, linking nutrient-sensing post-translational modification to PDH suppression and tumor growth.

    Evidence OGT depletion, c-Myc S415A glycosylation-site mutagenesis, ChIP, PDH phosphorylation assays, xenograft models

    PMID:38778217

    Open questions at the time
    • Direct c-Myc occupancy element on PDK2 promoter not mapped beyond ChIP
    • Single-lab pathway
  13. 2024 Medium

    Identified FOXK2 as a direct PDK2 phosphorylation substrate forming a glycolytic positive feedback loop, the first transcription-factor substrate establishing reciprocal PDK2 regulation.

    Evidence Co-IP, in vitro kinase assay, FOXK2 Thr13/Ser30 mutagenesis, PDK2 promoter luciferase reporter, xenograft assay in ovarian cancer

    PMID:38734828

    Open questions at the time
    • Structural basis of FHA-domain recognition not solved
    • Loop dynamics in non-cancer cells untested

Open questions

Synthesis pass · forward-looking unresolved questions
  • How PDK2's distinct activities—PDC inactivation versus non-canonical substrate phosphorylation (PARL, FOXK2) and reported transcriptional/proliferative effects—are coordinated, and which are druggable independently, remains unresolved.
  • No unified model reconciling mitochondrial kinase activity with apparent transcriptional/splicing influence
  • Substrate phosphosite specificity determinants undefined
  • Isoform-selective therapeutic exploitation not established

Mechanism profile

Synthesis pass · controlled-vocabulary classification · explore literature graph →
Molecular activity
GO:0016740 transferase activity 3 GO:0140096 catalytic activity, acting on a protein 3 GO:0140657 ATP-dependent activity 2
Localization
GO:0005739 mitochondrion 2
Pathway
R-HSA-1430728 Metabolism 3 R-HSA-9612973 Autophagy 1
Partners
FOXK2PARLPDHA1

Evidence

Reading pass · 17 per-paper findings extracted from the source corpus
Year Finding Method Journal Conf PMIDs
2011 Wild-type p53 directly represses transcription of PDK2, thereby reducing inactive phosphorylated pyruvate dehydrogenase complex (P-PDC) and limiting conversion of pyruvate to lactate (Warburg effect). Loss of p53 allows PDK2 elevation and promotes aerobic glycolysis. p53 knockdown/overexpression in cancer cells, Western blot for PDK2 and P-PDC, lactate measurement Cancer research Medium 22123926
2003 AZD7545, a small-molecule inhibitor of PDK2, activates PDH in vitro (EC50 ~5.2 nM in presence of PDK2) and in vivo, increasing the dephosphorylated (active) form of PDH in liver and skeletal muscle of rats and improving blood glucose control in obese Zucker rats. In vitro PDH activity assay with AZD7545 and PDK2; in vivo dosing in Wistar and obese Zucker rats; PDH activity measurement in tissue Biochemical Society transactions High 14641018
2012 PDHK2 (PDK2) knockout in mice increases PDH complex activity and lowers blood glucose in the fed state. Double knockout of PDHK2 and PDHK4 causes hypoglycaemia, ketoacidosis and hypothermia during fasting, establishing that PDK2 is the dominant regulator of PDH complex in the fed state while PDK4 dominates in the fasted state. Single and double PDK2/PDK4 knockout mice; PDH complex activity assays; blood glucose, insulin, and ketone measurements; stable isotope flux analysis The Biochemical journal High 22360721
2017 PDK2 phosphorylates the mitochondrial rhomboid protease PARL, regulating its N-terminal autocatalytic β-cleavage. PDK2-mediated phosphorylation of PARL negatively regulates PINK1/PARKIN-mediated mitophagy by controlling production of the less-active PARL cleavage product PACT, integrating mitochondrial metabolism with mitochondrial quality control. Co-IP; phosphorylation assays; mitochondrial stress assays; PARL cleavage Western blot; mitophagy reporters Cell reports Medium 28178523
2008 PDK2 binds the L2 lipoyl domain (E2 subunit of PDC) via a site stimulated by K+ ions at a site distinct from the ATP active site. Phosphate (Pi) is required for ADP, ATP, or pyruvate to interfere with PDK2 binding to L2 and promotes PDK2 tetramer formation. The acetyl-lipoate analog Nov3r inhibits E2-activated PDK2 (IC50 ~7.8 nM) by occupying the lipoyl-group binding site and preventing PDK2 binding to E2. Biochemical binding assays (PDHK2 and GST-L2 interaction), kinase activity assays, gel filtration for oligomeric state Biochemistry High 18220415
2020 Crystal structures of PDK2 in complex with inhibitor compound 8c (at the lipoyl-binding site) and novel 4,5-diarylisoxazole derivatives GM10030/GM67520 (at the ATP-binding site) reveal remote conformational coupling between the lipoyl-binding pocket and the ATP-binding pocket, and demonstrate an unprecedented asymmetric dimer conformation of PDK2. X-ray crystallography of PDK2 co-crystal structures; isothermal titration calorimetry for binding affinity Biochemical and biophysical research communications High 32444142
2024 PDK2 directly phosphorylates the transcription factor FOXK2 at Thr13 and Ser30 via interaction with the FOXK2 forkhead-associated (FHA) domain, enhancing FOXK2 transcriptional activity. FOXK2 in turn transcriptionally upregulates PDK2, creating a positive feedback loop that sustains glycolysis in ovarian cancer cells. Co-IP, in vitro kinase assay, site-directed mutagenesis of FOXK2 phosphorylation sites, luciferase reporter for PDK2 promoter, xenograft assay Oncogene Medium 38734828
2024 OGT-catalyzed O-GlcNAc modification of c-Myc at Ser415 stabilizes c-Myc protein, which transcriptionally upregulates PDK2 expression. Elevated PDK2 then phosphorylates the E1α subunit of the pyruvate dehydrogenase complex (PDH), inhibiting PDH activity, reducing mitochondrial pyruvate metabolism, suppressing ROS, and promoting xenograft tumor growth. OGT depletion, c-Myc glycosylation site mutagenesis (S415A), ChIP, PDH phosphorylation assays, xenograft models Cell death and differentiation Medium 38778217
2023 Glucocorticoid receptor (GR) directly binds the PDK2 promoter and stimulates PDK2 transcription in neurons in response to elevated glucocorticoids (GCs). Elevated PDK2 phosphorylates and inhibits PDH, reducing mitochondrial oxidative phosphorylation and TCA cycle flux. Silencing PDK2 abrogated glucocorticoid-induced PDH inhibition and restored neuronal oxidative phosphorylation. ChIP of GR at PDK2 promoter, PDK2 shRNA/siRNA knockdown, PDH phosphorylation Western blot, U-13C glucose isotope tracing, in vivo GR/PDK2 silencing with behavioral readout Molecular psychiatry Medium 37188779
2019 PDK2 mediates alternative pre-mRNA splicing of Bnip3 in cancer cells: inhibition of PDK2 in Panc-1 cells rapidly shifts Bnip3 isoform balance from the survival truncated Bnip3Δex3 toward the pro-death full-length Bnip3FL, inducing mitochondrial perturbations and cell death, coupling the glycolytic phenotype to hypoxia resistance. PDK2 inhibition (siRNA/DCA), RT-PCR isoform analysis, mitochondrial membrane potential assay, cell death assays The Journal of cell biology Medium 26416963
2020 PDK2 deficiency (genetic knockout and pharmacological inhibition with AZD7545) suppresses osteoclast differentiation by reducing phosphorylation of CREB and c-FOS, and consequent NFATc1 transcription downstream of RANKL signaling, thereby preventing ovariectomy-induced bone loss in mice. PDK2 knockout mice, PDK2 inhibitor AZD7545, ovariectomy model, CREB/c-FOS/NFATc1 Western blot, osteoclast differentiation assays from bone marrow cells Journal of bone and mineral research Medium 33125772
2021 PDK2 inhibition in ischemia/reperfusion injury increases PDH activity through the PDK2-PDH-Nrf2 axis: DCA-mediated PDK2 inhibition activates PDH, promotes glycolytic flux into the TCA cycle, and elevates Nrf2 and HO-1 antioxidant proteins, reducing oxidative stress and blood-brain barrier damage. MCAO mouse model, OGD in vitro model, DCA treatment, Western blot for PDK2/PDH/Nrf2/HO-1, Nrf2-specific inhibitor ML385 rescue experiment Oxidative medicine and cellular longevity Medium 34712383
2023 Oroxylin A (OA) disrupts the SIRT1/PDK2/PARL axis, inhibiting mitochondrial fusion; this synergizes with GLUT1 inhibition to break mitochondrial metabolic plasticity and sensitize hepatocellular carcinoma cells to glucose restriction. Pharmacological treatment with OA, mitochondrial fusion assays, spare respiratory capacity measurement, Western blot for SIRT1/PDK2/PARL Biomedicine & pharmacotherapy Low 37633053
2012 In C. elegans, PDHK-2 (PDK2 ortholog) expression is regulated by DAF-16 and NHR-49 transcription factors and is induced during long-term starvation and dauer state. PDHK-2 deficiency preserves fat stores by reducing lipase (ATGL, HSL) expression, extending dauer survival under nutrient restriction. C. elegans genetic mutants (pdhk-2 loss-of-function alleles), fat staining, lipase gene expression, survival assays, genetic epistasis with daf-2 PloS one Low 22848591
2011 Chronic cigarette smoke extract (CSE) treatment upregulates PDK2 expression in oral keratinocytes, decreasing PDH activity and increasing pyruvate and lactate production. This promotes HIF1α accumulation; ROS scavengers abolish PDK2 and HIF1α induction, and PDK2 inhibition with DCA reduces HIF1α and cell proliferation. PDK2 expression by qRT-PCR/Western blot, PDH activity assay, lactate/pyruvate measurement, HIF1α Western blot, DCA and N-acetylcysteine treatment, HIF1α inhibitor PloS one Medium 21283817
2019 PDK2 promotes cisplatin resistance in lung adenocarcinoma via transcriptional upregulation of CNNM3. PDK2 knockdown reduces CNNM3 expression and restores cisplatin sensitivity in vitro and in vivo. PDK2 overexpression/knockdown, CNNM3 luciferase reporter, cisplatin resistance assays, xenograft models Journal of drug targeting Low 30457021
2020 PDK2 overexpression in thyroid-associated ophthalmopathy (TAO) orbital fibroblasts enhances glycolysis (increased lactate, decreased oxygen consumption) and promotes fibroblast proliferation. PDK2 knockdown reduces cytoplasmic Akt levels and proliferation in TAO cells, placing PDK2 upstream of Akt signaling in this context. PDK2 siRNA knockdown, lactate production assay, oxygen consumption assay, Akt/pAkt308 quantification by capillary Western, EdU/BrdU proliferation assays Journal of molecular endocrinology Low 33086191

Source papers

Stage 0 corpus · 47 papers · ranked by NIH iCite citations
Year Title Journal Citations PMID
1999 Activation of serum- and glucocorticoid-regulated protein kinase by agonists that activate phosphatidylinositide 3-kinase is mediated by 3-phosphoinositide-dependent protein kinase-1 (PDK1) and PDK2. The Biochemical journal 496 10191262
2000 Akt/protein kinase B is regulated by autophosphorylation at the hypothetical PDK-2 site. The Journal of biological chemistry 420 10722653
1999 PDK1 acquires PDK2 activity in the presence of a synthetic peptide derived from the carboxyl terminus of PRK2. Current biology : CB 384 10226025
2011 p53 negatively regulates transcription of the pyruvate dehydrogenase kinase Pdk2. Cancer research 207 22123926
2005 PDK2: the missing piece in the receptor tyrosine kinase signaling pathway puzzle. American journal of physiology. Endocrinology and metabolism 115 16014356
2004 Differential roles of PDK1- and PDK2-phosphorylation sites in the yeast AGC kinases Ypk1, Pkc1 and Sch9. Microbiology (Reading, England) 98 15470109
2001 PDK2: a complex tail in one Akt. Science's STKE : signal transduction knowledge environment 97 11752635
2019 Dichloroacetate restores colorectal cancer chemosensitivity through the p53/miR-149-3p/PDK2-mediated glucose metabolic pathway. Oncogene 86 31597953
2021 DCA Protects against Oxidation Injury Attributed to Cerebral Ischemia-Reperfusion by Regulating Glycolysis through PDK2-PDH-Nrf2 Axis. Oxidative medicine and cellular longevity 77 34712383
2015 Activation of mitochondrial oxidation by PDK2 inhibition reverses cisplatin resistance in head and neck cancer. Cancer letters 75 26607904
2017 The Mitochondrial Rhomboid Protease PARL Is Regulated by PDK2 to Integrate Mitochondrial Quality Control and Metabolism. Cell reports 62 28178523
2003 AZD7545, a novel inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2), activates pyruvate dehydrogenase in vivo and improves blood glucose control in obese (fa/fa) Zucker rats. Biochemical Society transactions 62 14641018
2024 Cordycepin Modulates Microglial M2 Polarization Coupled with Mitochondrial Metabolic Reprogramming by Targeting HKII and PDK2. Advanced science (Weinheim, Baden-Wurttemberg, Germany) 55 38889331
2023 Targeting PDK2 rescues stress-induced impaired brain energy metabolism. Molecular psychiatry 40 37188779
2006 Oxysterol-binding protein-related protein (ORP) 9 is a PDK-2 substrate and regulates Akt phosphorylation. Cellular signalling 39 16962287
2024 The OGT-c-Myc-PDK2 axis rewires the TCA cycle and promotes colorectal tumor growth. Cell death and differentiation 38 38778217
2012 Fasting induces ketoacidosis and hypothermia in PDHK2/PDHK4-double-knockout mice. The Biochemical journal 38 22360721
2002 Characterization of PDK2 activity against protein kinase B gamma. Biochemistry 35 12162751
2022 Extracellular vesicles derived from Lactobacillus plantarum restore chemosensitivity through the PDK2-mediated glucose metabolic pathway in 5-FU-resistant colorectal cancer cells. Journal of microbiology (Seoul, Korea) 31 35781627
2015 PDK2-mediated alternative splicing switches Bnip3 from cell death to cell survival. The Journal of cell biology 31 26416963
2021 PDK2 leads to cisplatin resistance through suppression of mitochondrial function in ovarian clear cell carcinoma. Cancer science 27 34464482
1997 A translation frameshift mutation induced by a cytosine insertion in the polycystic kidney disease 2 gene (PDK2). Human molecular genetics 27 9175744
2020 Long noncoding RNA DUXAP8 contributes to the progression of hepatocellular carcinoma via regulating miR-422a/PDK2 axis. Cancer medicine 26 32022476
2021 The Use of Vitamin K2 in Patients With Parkinson's Disease and Mitochondrial Dysfunction (PD-K2): A Theranostic Pilot Study in a Placebo-Controlled Parallel Group Design. Frontiers in neurology 25 33505346
2024 Baicalin attenuates neuronal damage associated with SDH activation and PDK2-PDH axis dysfunction in early reperfusion. Phytomedicine : international journal of phytotherapy and phytopharmacology 22 38579645
2020 PDK2 Deficiency Prevents Ovariectomy-Induced Bone Loss in Mice by Regulating the RANKL-NFATc1 Pathway During Osteoclastogenesis. Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research 22 33125772
2017 PDK2 promotes chondrogenic differentiation of mesenchymal stem cells by upregulation of Sox6 and activation of JNK/MAPK/ERK pathway. Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas 21 28225870
2022 PDK1- and PDK2-mediated metabolic reprogramming contributes to the TGFβ1-promoted stem-like properties in head and neck cancer. Cancer & metabolism 20 36474273
2018 PDK2 induces cisplatin-resistance in lung adenocarcinoma via transcriptional regulation of CNNM3. Journal of drug targeting 19 30457021
2021 Circular RNA hsa_circ_0005397 promotes hepatocellular carcinoma progression by regulating the miR-326/PDK2 axis. The journal of gene medicine 17 33783904
2019 MicroRNA-214 suppresses cell proliferation and migration and cell metabolism by targeting PDK2 and PHF6 in hepatocellular carcinoma. Cell biology international 16 31329335
2022 circPTP4A2-miR-330-5p-PDK2 Signaling Facilitates In Vivo Survival of HuMSCs on SF-SIS Scaffolds and Improves the Repair of Damaged Endometrium. Oxidative medicine and cellular longevity 15 35571241
2019 Membrane-initiated cortisol action modulates early pyruvate dehydrogenase kinase 2 (pdk2) expression in fish skeletal muscle. Comparative biochemistry and physiology. Part A, Molecular & integrative physiology 15 30930204
2011 Chronic CSE treatment induces the growth of normal oral keratinocytes via PDK2 upregulation, increased glycolysis and HIF1α stabilization. PloS one 13 21283817
2008 Specific ion influences on self-association of pyruvate dehydrogenase kinase isoform 2 (PDHK2), binding of PDHK2 to the L2 lipoyl domain, and effects of the lipoyl group-binding site inhibitor, Nov3r. Biochemistry 12 18220415
2022 Inhibition of pyruvate dehydrogenase kinase improves carbohydrate utilization in Nile tilapia by regulating PDK2/4-PDHE1α axis and insulin sensitivity. Animal nutrition (Zhongguo xu mu shou yi xue hui) 11 36016966
2021 Circ_0091579 enhances the malignancy of hepatocellular carcinoma via miR-1287/PDK2 axis. Open life sciences 9 33817300
2020 PDK2-enhanced glycolysis promotes fibroblast proliferation in thyroid-associated ophthalmopathy. Journal of molecular endocrinology 9 33086191
2016 The Novel Small Molecule Inhibitor, OSU-T315, Suppresses Vestibular Schwannoma and Meningioma Growth by Inhibiting PDK2 Function in the AKT Pathway Activation. Austin journal of medical oncology 8 27642646
2024 Mitochondrial-related genes PDK2, CHDH, and ALDH5A1 served as a diagnostic signature and correlated with immune cell infiltration in ulcerative colitis. Aging 6 38376420
2024 Phosphorylation of FOXK2 at Thr13 and Ser30 by PDK2 sustains glycolysis through a positive feedback manner in ovarian cancer. Oncogene 6 38734828
2022 Chemokine (C-X-C motif) ligand 1 maintains the immune surveillance function of natural killer cells via the PDK2/mTOR signaling pathway. Cell biology and toxicology 6 35304656
2016 PDK2 and ABCG2 genes polymorphisms are correlated with blood glucose levels and uric acid in Tibetan gout patients. Genetics and molecular research : GMR 6 26909964
2023 Inhibition of mitochondrial fusion via SIRT1/PDK2/PARL axis breaks mitochondrial metabolic plasticity and sensitizes cancer cells to glucose restriction therapy. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie 5 37633053
2020 Structural basis for the inhibition of PDK2 by novel ATP- and lipoyl-binding site targeting compounds. Biochemical and biophysical research communications 4 32444142
2012 PDHK-2 deficiency is associated with attenuation of lipase-mediated fat consumption for the increased survival of Caenorhabditis elegans dauers. PloS one 4 22848591
2025 PDK2-enhanced glycolysis aggravates fibrosis via IL11 signaling pathway in Graves' orbitopathy. Frontiers in immunology 1 40018034

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