jm5b01828_si_001.pdf (21.57 MB)
Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation
journal contribution
posted on 2016-03-23, 00:00 authored by Shao-Lin Zhang, Xiaohui Hu, Wen Zhang, Kin Yip TamPyruvate
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).