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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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View/Download:10/0
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Submit date:2018/10/30
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.
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View/Download:6/0
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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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Submit date:2018/10/30
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
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View/Download:9/0
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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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View/Download:6/0
  |  
Submit date:2018/10/30
aerobic glycolysis
AZD7545
dichloroacetate
LC-MS/MS
pyruvate dehydrogenase kinases
cancer metabolism
Identification and efficacy of glycine, serine and threonine metabolism in potentiating kanamycin-mediated killing of Edwardsiella piscicida
Journal article
JOURNAL OF PROTEOMICS, 2018,Volume: 183,Page: 34-44
Authors:
Ye, Jin-zhou
;
Lin, Xiang-min
;
Cheng, Zhi-xue
;
Su, Yu-bin
;
Li, Wan-xin
;
Ali, Far-man
;
Zheng, Jun
;
Peng, Bo
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View/Download:35/0
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Submit date:2018/10/30
Antibiotic Resistance
Metabolic Modulation
Glycine, Serine And Threonine Metabolism
Amino Acid
Glucose
Kanamycin
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 S.-L.
;
Zhang W.
;
Yang Z.
;
Hu X.
;
Tam K.Y.
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View/Download:3/0
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Submit date:2018/12/18
Anti-proliferation
Binding affinity
Pyruvate dehydrogenase complex
Pyruvate dehydrogenase kinase
Synthesis and biological evaluation of (R)-3,3,3-trifluoro-2-hydroxy-2methylpropionamides as pyruvate dehydrogenase kinase 1 (PDK1) inhibitors to reduce the growth of cancer cells
Conference paper
Authors:
Zhang, Shao-Lin
;
Zhang, Wen
;
Yang, Zheng
;
Hu, Xiaohui
;
Tam, Kin Yip
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View/Download:3/0
  |  
Submit date:2018/10/30
Pyruvate dehydrogenase kinase
Pyruvate dehydrogenase complex
Anti-proliferation
Binding affinity
Phenyl butyrate inhibits pyruvate dehydrogenase kinase 1 and contributes to its anti-cancer effect
Conference paper
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, Zhuhai, PEOPLES R CHINA, 2016-8-23-26
Authors:
Zhang, Wen
;
Zhang, Shao-Lin
;
Hu, Xiaohui
;
Tam, Kin Yip
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Submit date:2018/10/30
Phenyl Butyrate
Cancer
Pyruvate Dehydrogenase
Pyruvate Dehydrogenase Kinase 1
Tumor Metabolism
Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase to Inhibit Cancer Proliferation
Journal article
Journal of Medicinal Chemistry, 2016,Volume: 59,Issue: 7,Page: 3562-3568
Authors:
Zhang S.-L.
;
Hu X.
;
Zhang W.
;
Tam K.Y.
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View/Download:1/0
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Submit date:2018/12/18