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  1. General Info
  2. Effects Info
  3. Reference
Molecular Details
01. General Information
Name [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1
UniProt ID PDK1_HUMAN
Gene Name PDK1
Gene ID 5163
Synonyms
PDK1
Sequence
MRLARLLRGAALAGPGPGLRAAGFSRSFSSDSGSSPASERGVPGQVDFYARFSPSPLSMK
QFLDFGSVNACEKTSFMFLRQELPVRLANIMKEISLLPDNLLRTPSVQLVQSWYIQSLQE
LLDFKDKSAEDAKAIYDFTDTVIRIRNRHNDVIPTMAQGVIEYKESFGVDPVTSQNVQYF
LDRFYMSRISIRMLLNQHSLLFGGKGKGSPSHRKHIGSINPNCNVLEVIKDGYENARRLC
DLYYINSPELELEELNAKSPGQPIQVVYVPSHLYHMVFELFKNAMRATMEHHANRGVYPP
IQVHVTLGNEDLTVKMSDRGGGVPLRKIDRLFNYMYSTAPRPRVETSRAVPLAGFGYGLP
ISRLYAQYFQGDLKLYSLEGYGTDAVIYIKALSTDSIERLPVYNKAAWKHYNTNHEADDW
CVPSREPKDMTTFRSA
Pathway Map MAP LINK
T.C. Number 8.A.188.1.1
KEGG ID hsa5163
TTD ID T15776
Pfam PF02518; PF10436
02. Combinatorial Therapeutic Effect(s)
Synergistic Effect
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Enhancing Drug Efficacy
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Combination Pair ID: 236
Pair Name Beta-Elemene, Fluorouracil
Phytochemical Beta-Elemene
Drug Fluorouracil
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Regulate Info Down-regulation [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1 Phosphorylation
Result The conclusion obtained, considering that the results suggest that the combination may be important specifically in the treatment of TNBC.
Combination Pair ID: 582
Pair Name Eriocalyxin B, Gemcitabine
Phytochemical Eriocalyxin B
Drug Gemcitabine
Disease Info [ICD-11: 2C10] Pancreatic cancer Investigative
Regulate Info Down-regulation [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1 Phosphorylation
Result Gem and EriB (or Isodon extract) taken together in combination regulated PDK1/AKT1/caspase and JNK signaling and promoted apoptosis synergistically, which may contribute to the much increased anti-proliferative activity compared to either agent alone.
Combination Pair ID: 204
Pair Name Ginsenoside Rg3, Sorafenib
Phytochemical Ginsenoside Rg3
Drug Sorafenib
Disease Info [ICD-11: 2C12] Hepatocellular carcinoma Investigative
Regulate Info Down-regulation [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1 Phosphorylation
Result These findings suggest a promising strategy for HCC treatment, which could be performed in a sufficiently frequent manner.
Reversing Drug Resistance
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Combination Pair ID: 1035
Pair Name Shikonin, Gemcitabine
Phytochemical Shikonin
Drug Gemcitabine
Disease Info [ICD-11: 2C10] Pancreatic cancer Investigative
Regulate Info Down-regulation [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1 Expression
Result These results indicate that shikonin reduced MCT4 expression and activation, resulting in inhibition of aerobic glycolysis in CAFs and overcoming CAF-induced gemcitabine resistance in PC. Shikonin is a promising chemosensitizing phytochemical agent when used in combination with gemcitabine for PC treatment. The results suggest that disrupting the metabolic coupling between cancer cells and stromal cells might provide an attractive strategy for improving gemcitabine efficacy.
03. Reference
No. Title Href
1 β-Elemene Enhances the Chemotherapeutic Effect of 5-Fluorouracil in Triple-Negative Breast Cancer via PI3K/AKT, RAF-MEK-ErK, and NF-κB Signaling Pathways. Onco Targets Ther. 2020 Jun 9;13:5207-5222. doi: 10.2147/OTT.S242820. Click
2 Isodon eriocalyx and its bioactive component Eriocalyxin B enhance cytotoxic and apoptotic effects of gemcitabine in pancreatic cancer. Phytomedicine. 2018 May 15;44:56-64. doi: 10.1016/j.phymed.2018.03.055. Click
3 Synergistic anticancer activity of 20(S)-Ginsenoside Rg3 and Sorafenib in hepatocellular carcinoma by modulating PTEN/Akt signaling pathway. Biomed Pharmacother. 2018 Jan;97:1282-1288. doi: 10.1016/j.biopha.2017.11.006. Click
4 Shikonin reverses cancer-associated fibroblast-induced gemcitabine resistance in pancreatic cancer cells by suppressing monocarboxylate transporter 4-mediated reverse Warburg effect. Phytomedicine. 2024 Jan;123:155214. doi: 10.1016/j.phymed.2023.155214. Click
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