Database Query Results : , , PDKs

PDKs, pyruvate dehydrogenase kinase: Click to Expand ⟱
Source:
Type:
– PDK1 is often upregulated in cancers and is central to the metabolic reprogramming (Warburg effect) that allows tumor cells to favor glycolysis over oxidative phosphorylation.
– Elevated PDK1 expression has been correlated with aggressive tumor behavior and poor prognosis in several cancer types, including non‐small cell lung cancer, ovarian cancer, and gastric cancer.

– Although PDK2 has a similar catalytic role as PDK1, its expression levels and impact may vary.
– Some studies have observed that increased PDK2 expression is associated with more aggressive cancer features and resistance to therapy in certain tumor types.

– PDK3 is often upregulated in response to hypoxic conditions—a common feature of solid tumors—which can further drive metabolic divergence in cancer cells.

– The role of PDK4 appears to be more variable. In some settings, its activity might be lower in tumor cells to favor the use of glycolysis, while in others, it may be upregulated as part of broader metabolic adaptations.

-By upregulating PDKs, cancer cells limit the flux of pyruvate into the mitochondria, thereby promoting glycolysis.


Scientific Papers found: Click to Expand⟱
3271- ALA,    Decrypting the potential role of α-lipoic acid in Alzheimer's disease
- Review, AD, NA
*antiOx↑, *memory↑, *neuroP↑, *Inflam↓, *IronCh↑, *NRF2↑, *BBB↑, *GlucoseCon↑, *Ach↑, *ROS↓, *p‑tau↓, *Aβ↓, *cognitive↑, *Hif1a↑, *Ca+2↓, *GLUT3↑, *GLUT4↑, *HO-1↑, *VEGF↑, *PDKs↓, *PDH↑, *VCAM-1↓, *GSH↑, *NRF2↑, *hepatoP↑, *ChAT↑,
2389- BA,    Baicalin alleviates lipid accumulation in adipocytes via inducing metabolic reprogramming and targeting Adenosine A1 receptor
- in-vitro, Obesity, 3T3
*ECAR↑, *OCR↓, *p‑AMPK↑, *p‑ACC↑, *Glycolysis↑, *lipidDe↓, *SREBP1↓, *FAO↑, *HK2↑, *PKM2↑, *LDHA↑, *PDKs↓, *ACC↓,
1889- DCA,    A mitochondria-K+ channel axis is suppressed in cancer and its normalization promotes apoptosis and inhibits cancer growth
- Review, Var, NA
PDKs↓, Glycolysis↓, mt-H2O2↑, Apoptosis↑, TumCP↓, TumCG↓, toxicity∅,
1887- DCA,    GSTZ1 expression and chloride concentrations modulate sensitivity of cancer cells to dichloroacetate
- in-vitro, Var, NA
GSTZ1∅, eff↓, PDKs↓, Chl∅, eff↓,
1885- DCA,    Role of SLC5A8, a plasma membrane transporter and a tumor suppressor, in the antitumor activity of dichloroacetate
- in-vitro, CRC, HCT116 - in-vitro, CRC, SW-620 - in-vitro, CRC, HT-29
SMCT1∅, eff↓, eff↑, eff↑, PDKs↓, MMP↓, Glycolysis↓, mitResp↑, ROS↑, eff↑,
1882- DCA,    Dichloroacetate (DCA) as a potential metabolic-targeting therapy for cancer
- Analysis, NA, NA
PDKs↓, PDH↑, lactateProd↓, Half-Life∅,
1878- DCA,  5-FU,    Synergistic Antitumor Effect of Dichloroacetate in Combination with 5-Fluorouracil in Colorectal Cancer
- in-vitro, CRC, LS174T - in-vitro, CRC, LoVo - in-vitro, CRC, SW-620 - in-vitro, CRC, HT-29
tumCV↓, eff↑, PDKs↓, lactateProd↓, Glycolysis↓, mitResp↑, TumCCA↑, Bcl-2↓, BAX↑, Casp3↑,
1877- DCA,    Non-Hodgkin′s Lymphoma Reversal with Dichloroacetate
- Case Report, lymphoma, NA
Remission↑, p‑PDKs↓, Glycolysis↓, i-Ca+2↓, toxicity↓, Dose∅,
1884- DCA,  Sal,    Dichloroacetate and Salinomycin Exert a Synergistic Cytotoxic Effect in Colorectal Cancer Cell Lines
- in-vitro, CRC, DLD1 - in-vitro, CRC, HCT116
eff↑, pH↓, PDKs↓, Warburg↓,
1875- DCA,    Dichloroacetate inhibits neuroblastoma growth by specifically acting against malignant undifferentiated cells
- in-vitro, neuroblastoma, NA - in-vivo, NA, NA
selectivity↑, AntiCan↑, TumVol↓, PDKs↓, mt-OXPHOS↑, MMP↓, Glycolysis↓, toxicity↓, Warburg↓, ROS↑, eff↑,
1873- DCA,    Dual-targeting of aberrant glucose metabolism in glioblastoma
- in-vitro, GBM, U87MG - in-vitro, GBM, U251
PDKs↓, eff↑, selectivity↑, MMP↓, ROS↑, Apoptosis↑, Warburg↓, eff↑, Dose∅, toxicity∅,
1872- DCA,    Dichloroacetate, a selective mitochondria-targeting drug for oral squamous cell carcinoma: a metabolic perspective of treatment
- in-vitro, Oral, HSC2 - in-vitro, Oral, HSC3
PDKs↓, ROS↑, OCR↑, other↑,
1864- DCA,  MET,    Dichloroacetate Enhances Apoptotic Cell Death via Oxidative Damage and Attenuates Lactate Production in Metformin-Treated Breast Cancer Cells
- in-vitro, BC, MCF-7 - in-vitro, BC, T47D - in-vitro, Nor, MCF10
PDKs↓, eff↑, ROS↑, PDK1↓, lactateProd↓, p‑PDH↑, Dose∅, OCR↑, DNA-PK↑, γH2AX↑, cl‑PARP↑, selectivity↑, *toxicity∅,
1867- DCA,  Chemo,    Sensitization of breast cancer cells to paclitaxel by dichloroacetate through inhibiting autophagy
- in-vivo, BC, NA - in-vitro, BC, NA
TumCG↓, eff↑, OS↑, PDKs↓, PDH↑,
4901- DCA,  Sal,    Dichloroacetate and Salinomycin as Therapeutic Agents in Cancer
- Review, NSCLC, NA
Glycolysis↓, OXPHOS↑, PDKs↓, ROS↑, Apoptosis↑, GlucoseCon↓, lactateProd↓, RadioS↑, TumAuto↑, mTOR↓, LC3s↓, p62↑, TumCG↓, OS↑, toxicity↝, ChemoSen↑, eff↑, eff↑, Ferritin↓, CSCs↓, EMT↓, ROS↑, Cyt‑c↑, Casp3↑, ER Stress↑, selectivity↑, eff↑, TumCG↓,
1628- HCA,  ALA,    Addition of Hydroxy Citrate improves effect of ALA
- Review, Var, NA
ACLY↓, other↓, ROS↑, eff↑, PDKs↓,
2044- PB,  DCA,    Differential inhibition of PDKs by phenylbutyrate and enhancement of pyruvate dehydrogenase complex activity by combination with dichloroacetate
- in-vivo, NA, NA
PDK1↓, PDKs↓, eff↑, PDH↑,
1888- VitB1/Thiamine,  DCA,    High Dose Vitamin B1 Reduces Proliferation in Cancer Cell Lines Analogous to Dichloroacetate
- in-vitro, PC, SK-N-BE - NA, PC, PANC1
p‑PDH↓, GlucoseCon↓, lactateProd↓, MMP↓, Casp3↑, eff↑, PDKs↓, selectivity↑, TumCG↓, Dose∅, MMP↓, ROS∅, toxicity↑, antiOx↑,

* indicates research on normal cells as opposed to diseased cells
Total Research Paper Matches: 18

Pathway results for Effect on Cancer / Diseased Cells:


Redox & Oxidative Stress

antiOx↑, 1,   GSTZ1∅, 1,   mt-H2O2↑, 1,   OXPHOS↑, 1,   mt-OXPHOS↑, 1,   ROS↑, 8,   ROS∅, 1,  

Metal & Cofactor Biology

Ferritin↓, 1,  

Mitochondria & Bioenergetics

mitResp↑, 2,   MMP↓, 5,   OCR↑, 2,  

Core Metabolism/Glycolysis

ACLY↓, 1,   GlucoseCon↓, 2,   Glycolysis↓, 6,   lactateProd↓, 5,   PDH↑, 3,   p‑PDH↓, 1,   p‑PDH↑, 1,   PDK1↓, 2,   PDKs↓, 15,   p‑PDKs↓, 1,   Warburg↓, 3,  

Cell Death

Apoptosis↑, 3,   BAX↑, 1,   Bcl-2↓, 1,   Casp3↑, 3,   Cyt‑c↑, 1,  

Transcription & Epigenetics

other↓, 1,   other↑, 1,   tumCV↓, 1,  

Protein Folding & ER Stress

ER Stress↑, 1,  

Autophagy & Lysosomes

LC3s↓, 1,   p62↑, 1,   TumAuto↑, 1,  

DNA Damage & Repair

DNA-PK↑, 1,   cl‑PARP↑, 1,   γH2AX↑, 1,  

Cell Cycle & Senescence

TumCCA↑, 1,  

Proliferation, Differentiation & Cell State

CSCs↓, 1,   EMT↓, 1,   mTOR↓, 1,   TumCG↓, 5,  

Migration

i-Ca+2↓, 1,   Chl∅, 1,   TumCP↓, 1,  

Barriers & Transport

SMCT1∅, 1,  

Cellular Microenvironment

pH↓, 1,  

Drug Metabolism & Resistance

ChemoSen↑, 1,   Dose∅, 4,   eff↓, 3,   eff↑, 16,   Half-Life∅, 1,   RadioS↑, 1,   selectivity↑, 5,  

Clinical Biomarkers

Ferritin↓, 1,  

Functional Outcomes

AntiCan↑, 1,   OS↑, 2,   Remission↑, 1,   toxicity↓, 2,   toxicity↑, 1,   toxicity↝, 1,   toxicity∅, 2,   TumVol↓, 1,  
Total Targets: 63

Pathway results for Effect on Normal Cells:


Redox & Oxidative Stress

antiOx↑, 1,   GSH↑, 1,   HO-1↑, 1,   lipidDe↓, 1,   NRF2↑, 2,   ROS↓, 1,  

Metal & Cofactor Biology

IronCh↑, 1,  

Mitochondria & Bioenergetics

OCR↓, 1,  

Core Metabolism/Glycolysis

ACC↓, 1,   p‑ACC↑, 1,   p‑AMPK↑, 1,   ECAR↑, 1,   FAO↑, 1,   GlucoseCon↑, 1,   Glycolysis↑, 1,   HK2↑, 1,   LDHA↑, 1,   PDH↑, 1,   PDKs↓, 2,   PKM2↑, 1,   SREBP1↓, 1,  

Transcription & Epigenetics

Ach↑, 1,  

Migration

Ca+2↓, 1,   VCAM-1↓, 1,  

Angiogenesis & Vasculature

Hif1a↑, 1,   VEGF↑, 1,  

Barriers & Transport

BBB↑, 1,   GLUT3↑, 1,   GLUT4↑, 1,  

Immune & Inflammatory Signaling

Inflam↓, 1,  

Synaptic & Neurotransmission

ChAT↑, 1,   p‑tau↓, 1,  

Protein Aggregation

Aβ↓, 1,  

Functional Outcomes

cognitive↑, 1,   hepatoP↑, 1,   memory↑, 1,   neuroP↑, 1,   toxicity∅, 1,  
Total Targets: 38

Scientific Paper Hit Count for: PDKs, pyruvate dehydrogenase kinase
15 Dichloroacetate
2 Alpha-Lipoic-Acid
2 salinomycin
1 Baicalin
1 5-fluorouracil
1 Metformin
1 Chemotherapy
1 HydroxyCitric Acid
1 Phenylbutyrate
1 Vitamin B1/Thiamine
Query results interpretion may depend on "conditions" listed in the research papers.
Such Conditions may include : 
  -low or high Dose
  -format for product, such as nano of lipid formations
  -different cell line effects
  -synergies with other products 
  -if effect was for normal or cancerous cells
Filter Conditions: Pro/AntiFlg:%  IllCat:%  CanType:%  Cells:%  prod#:%  Target#:1201  State#:%  Dir#:%
wNotes=0 sortOrder:rid,rpid

 

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