| Residential College | false |
| Status | 已發表Published |
| Dichloroacetophenone derivatives as pyruvate dehydrogenase kinase inhibitor in non-small cell lung cancer models | |
TAM KIN YIP 
| |
| 2023-09-05 | |
| Size of Audience | 200 |
| Type of Speaker | Invited Lecture |
| Abstract | Pyruvate dehydrogenase kinase 1 (PDK1) is a key enzyme involved in glucose metabolism and is often overexpressed in cancers exhibiting glycolytic phenotypes, such as non-small-cell lung cancers (NSCLC). Targeting PDK1 appears to be an attractive anticancer strategy. Based on a previously reported moderate potent anticancer PDK1 inhibitor, 64, we developed some dichloroacetophenone biphenylsulfone ethers, which exhibited good inhibitory effects on PDK1. The anticancer effects of these novel dichloroacetophenone derivatives were evaluated in NSCLC cell lines, namely NCI–H1299 and NCI–H1975. It was found that one of the derivatives, 31, exhibited sub-micromolar cancer cell IC50s and significantly suppressed the tumor growth in NCI–H1975 mouse xenograft model, outperforming the anticancer effects of 64. Our results suggested that 31 strongly inhibited PDK1 leading to effective modulations of the aberrant glucose metabolism in cancer cells, which could be an alternative anticancer strategy. |
| Keyword | Cancer Metabolism Aerobic Glycolysis Pyruvate Dehydrogenase Kinase |
| Conference Date | 4-6 September, 2023 |
| Conference Place | University Rectorate, Belgrade, Serbia |
| 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. Dichloroacetophenone derivatives as pyruvate dehydrogenase kinase inhibitor in non-small cell lung cancer models, 4-6 September, 2023. |
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