TY - DATA T1 - Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation PY - 2016/03/23 AU - Shao-Lin Zhang AU - Xiaohui Hu AU - Wen Zhang AU - Kin Yip Tam UR - https://acs.figshare.com/articles/journal_contribution/Unexpected_Discovery_of_Dichloroacetate_Derived_Adenosine_Triphosphate_Competitors_Targeting_Pyruvate_Dehydrogenase_Kinase_To_Inhibit_Cancer_Proliferation/3141958 DO - 10.1021/acs.jmedchem.5b01828.s001 L4 - https://ndownloader.figshare.com/files/4885279 KW - Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase KW - cancer cells proliferation KW - ATP KW - DCA KW - adenosine triphosphate KW - Unexpected Discovery KW - Inhibit Cancer Proliferation Pyruvate dehydrogenase kinases KW - PDK isoform 1 KW - cancer therapy N2 - 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). ER -