| Residential College | false |
| Status | 已發表Published |
| LC/MS/MS method revealed that lung cancer cells exhibited distinct metabolite profiles upon the treatment with different anticancer pyruvate dehydrogenase kinases (PDKs) inhibitors | |
TAM KIN YIP 
| |
| 2019-09-09 | |
| Size of Audience | 150 |
| Type of Speaker | Invited Lecture |
| Abstract | Pyruvate dehydrogenase kinases (PDKs) dominate the critical switch between mitochondria-based respiration and cytoplasm based glycolysis by controlling pyruvate dehydrogenase (PDH) activity. Up-regulated PDKs play a great role in the Warburg effect in cancer cells and accordingly present a therapeutic target. Dichloroacetate (DCA) and AZD7545 are the two most-well-known PDK inhibitors exhibiting distinct pharmacological profiles. DCA showed anticancer effects in various preclinical models and clinical studies, while the primary preclinical indication of AZD7545 was on the improvement of glucose control in type II diabetes. Little, if any, study has been undertaken to elucidate the effects of PDK inhibition on the metabolites in the tricarboxylic acid (TCA) cycle. Herein, the metabolite alterations of non-small-cell lung cancer (NSCLC) cells upon the treatment with PDK inhibitors were studied using a liquid-chromatography-based tandem mass spectrometry method. The method was validated for quantification of some common glycolysis and TCA cycle catabolites with good sensitivity and reproducibility, including glucose, pyruvate, lactate, acetyl coenzyme A, citrate, α-ketoglutarate, fumarate, succinate, malate, and oxaloacetate. Our results suggested that NSCLC cells exhibited distinct metabolite profiles following the treatment with different PDK inhibitors, which may reflect the different pharmacological indications of these inhibitors. |
| Keyword | Aerobic Glycolysis Lc-ms/ms Pyruvate Dehydrogenase Kinases Cancer Metabolism |
| Conference Date | 9-11 September 2019 |
| Conference Place | Hotel Park, Split, Croatia |
| Document Type | Presentation |
| Collection | DEPARTMENT OF PHARMACEUTICAL SCIENCES |
| Corresponding Author | TAM KIN YIP |
| Affiliation | Faculty of Health Sciences |
| Recommended Citation GB/T 7714 | TAM KIN YIP. LC/MS/MS method revealed that lung cancer cells exhibited distinct metabolite profiles upon the treatment with different anticancer pyruvate dehydrogenase kinases (PDKs) inhibitors, 9-11 September 2019. |
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