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Development of pyruvate dehydrogenase kinase inhibitors in medicinal chemistry with particular emphasis as anticancer agents
Shao-Lin Zhang; Xiaohui Hu; Wen Zhang; Huankai Yao; Kin Yip Tam
2015-09
Source PublicationDrug Discovery Today
ISSN1359-6446
Volume20Issue:9Pages:1112-1119
Abstract

Many cancer cells demonstrate a high rate of glucose consumption via glycolysis to provide intermediates for macromolecule biosynthesis. To accomplish this metabolic change, the expression of pyruvate dehydrogenase kinases (PDKs) is rapidly increased in cancer cells. Inhibition of PDKs could promote the function of mitochondria by increasing the oxidative metabolism of pyruvate, resulting in the death of cancer cells. In this review, we provide an overview of the structural information available for PDKs and their connections to known therapeutic effects. We then describe the development of small molecule PDK inhibitors in medicinal chemistry with particular emphasis as anticancer agents. Finally, directions for further development of PDK inhibitors as potential anticancer agents are discussed.

DOIhttp://doi.org/10.1016/j.drudis.2015.03.012
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000361928000010
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Cited Times [WOS]:39   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Corresponding AuthorKin Yip Tam
AffiliationDrug Development Core, Faculty of Health Sciences, University of Macau, Macau, China
First Author AffilicationFaculty of Health Sciences
Corresponding Author AffilicationFaculty of Health Sciences
Recommended Citation
GB/T 7714
Shao-Lin Zhang,Xiaohui Hu,Wen Zhang,et al. Development of pyruvate dehydrogenase kinase inhibitors in medicinal chemistry with particular emphasis as anticancer agents[J]. Drug Discovery Today,2015,20(9):1112-1119.
APA Shao-Lin Zhang,Xiaohui Hu,Wen Zhang,Huankai Yao,&Kin Yip Tam.(2015).Development of pyruvate dehydrogenase kinase inhibitors in medicinal chemistry with particular emphasis as anticancer agents.Drug Discovery Today,20(9),1112-1119.
MLA Shao-Lin Zhang,et al."Development of pyruvate dehydrogenase kinase inhibitors in medicinal chemistry with particular emphasis as anticancer agents".Drug Discovery Today 20.9(2015):1112-1119.
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