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Synthesis, biological evaluation and structure-activity relationship of novel dichloroacetophenones targeting pyruvate dehydrogenase kinases with potent anticancer activity Journal article
European Journal of Medicinal Chemistry, 2021,Volume: 214
Authors:  Xu,Biao;  Wang,Zhi Peng;  Liu,Qingwang;  Yang,Xiaohong;  Li,Xuemin;  Huang,Ding;  Qiu,Yanfei;  Tam,Kin Yip;  Zhang,Shao Lin;  He,Yun
Favorite |  | TC[WOS]:0 TC[Scopus]:0 | Submit date:2021/03/04
Cancer metabolism  Proliferation  Pyruvate dehydrogenase kinase  Structure-activity relationship  
Function of DHX33 in promoting Warburg effect via regulation of glycolytic genes Journal article
Journal of Cellular Physiology, 2021,Volume: 236,Issue: 2,Page: 981-996
Authors:  Peng,Cheng;  Hou,Sheng Tao;  Deng,Chu Xia;  Zhang,Yandong
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demethylation  DHX33  Gadd45a  glycolysis  RNA helicase  Warburg effect  
Dichloroacetophenones targeting at pyruvate dehydrogenase kinase 1 with improved selectivity and antiproliferative activity: Synthesis and structure-activity relationships Journal article
Bioorganic and Medicinal Chemistry Letters, 2018,Volume: 28,Issue: 21,Page: 3441-3445
Authors:  Zhang,Shao Lin;  Yang,Zheng;  Hu,Xiaohui;  Tam,Kin Yip
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Antiproliferative activity  Dichloroacetophenone  Kinase inhibition  Pyruvate dehydrogenase complex  Pyruvate dehydrogenase kinase  
Dichloroacetophenones targeting at pyruvate dehydrogenase kinase 1 with improved selectivity and antiproliferative activity: Synthesis and structure-activity relationships Journal article
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2018,Volume: 28,Issue: 21,Page: 3441-3445
Authors:  Zhang, Shao-Lin;  Yang, Zheng;  Hu, Xiaohui;  Tam, Kin Yip
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Pyruvate dehydrogenase kinase  Pyruvate dehydrogenase complex  Antiproliferative activity  Dichloroacetophenone  Kinase inhibition  
Identification of Novel Pyruvate Dehydrogenase Kinase 1 (PDK1) Inhibitors by Kinase Activity-Based High-Throughput Screening for Anticancer Therapeutics Journal article
ACS Combinatorial Science, 2018,Volume: 20,Issue: 11,Page: 660-671
Authors:  Zhang W.;  Hu X.;  Chakravarty H.;  Yang Z.;  Tam K.Y.
Favorite |  | TC[WOS]:3 TC[Scopus]:3 | Submit date:2018/12/18
cancer  high-throughput screening  pyruvate dehydrogenase kinase 1  small molecule inhibitors  Warburg effect  
Inhibition of pyruvate dehydrogenase kinase 1 enhances the anti-cancer effect of EGFR tyrosine kinase inhibitors in non-small cell lung cancer Journal article
EUROPEAN JOURNAL OF PHARMACOLOGY, 2018,Volume: 838,Page: 41-52
Authors:  Yang, Zheng;  Zhang, Shao-Lin;  Hu, Xiaohui;  Tam, Kin Yip
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Dichloroacetophenone  Epidermal Growth Factor Receptor  Tyrosine Kinase Inhibitor  Synergism  Hypoxia  Oxidative Phosphorylation  
Anticancer effects of some novel dichloroacetophenones through the inhibition of pyruvate dehydrogenase kinase 1 Journal article
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2018,Volume: 123,Page: 43-55
Authors:  Zhang, Shao-Lin;  Yang, Zheng;  Hu, Xiaohui;  Chakravarty, Harapriya;  Tam, Kin Yip
Favorite |  | TC[WOS]:7 TC[Scopus]:7 | Submit date:2018/10/30
Dichloroacetophenone  Pyruvate Dehydrogenase Kinase  Pyruvate Dehydrogenase Complex  Anticancer Activity  Metabolic Reprogramming  
Liquid Chromatography-Tandem Mass Spectrometry Method Revealed that Lung Cancer Cells Exhibited Distinct Metabolite Profiles upon the Treatment with Different Pyruvate Dehydrogenase Kinase Inhibitors Journal article
JOURNAL OF PROTEOME RESEARCH, 2018,Volume: 17,Issue: 9,Page: 3012-3021
Authors:  Zhang, Wen;  Hu, Xiaohui;  Zhou, Wei;  Tam, Kin Yip
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Aerobic Glycolysis  Azd7545  Dichloroacetate  Lc-ms/ms  Pyruvate Dehydrogenase Kinases  Cancer Metabolism  
Synthesis and biological evaluation of (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides as pyruvate dehydrogenase kinase 1 (PDK1) inhibitors to reduce the growth of cancer cells Journal article
European Journal of Pharmaceutical Sciences, 2017,Volume: 110,Page: 87-92
Authors:  Zhang,Shao Lin;  Zhang,Wen;  Yang,Zheng;  Hu,Xiaohui;  Tam,Kin Yip
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Anti-proliferation  Binding affinity  Pyruvate dehydrogenase complex  Pyruvate dehydrogenase kinase  
Phenyl butyrate inhibits pyruvate dehydrogenase kinase 1 and contributes to its anti-cancer effect Journal article
European Journal of Pharmaceutical Sciences, 2017,Volume: 110,Page: 93-100
Authors:  Zhang,Wen;  Zhang,Shao Lin;  Hu,Xiaohui;  Tam,Kin Yip
Favorite |  | TC[WOS]:8 TC[Scopus]:10 | Submit date:2021/03/04
Cancer  Phenyl butyrate  Pyruvate dehydrogenase  Pyruvate dehydrogenase kinase 1  Tumor metabolism