Unexpected Discovery
of Dichloroacetate Derived
Adenosine Triphosphate
Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer
Proliferation
Shao-Lin Zhang
Xiaohui Hu
Wen Zhang
Kin Yip Tam
10.1021/acs.jmedchem.5b01828.s002
https://acs.figshare.com/articles/dataset/Unexpected_Discovery_of_Dichloroacetate_Derived_Adenosine_Triphosphate_Competitors_Targeting_Pyruvate_Dehydrogenase_Kinase_To_Inhibit_Cancer_Proliferation/3141955
Pyruvate
dehydrogenase kinases (PDKs) have recently emerged as
an attractive target for cancer therapy. Herein, we prepared a series
of compounds derived from dichloroacetate (DCA) which inhibited cancer
cells proliferation. For the first time, we have successfully developed
DCA derived inhibitors that preferentially bind to the adenosine triphosphate
(ATP) pocket of PDK isoform 1 (PDK1).
2016-03-23 00:00:00
Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase
cancer cells proliferation
ATP
DCA
adenosine triphosphate
Unexpected Discovery
Inhibit Cancer Proliferation Pyruvate dehydrogenase kinases
PDK isoform 1
cancer therapy