PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 21283817-8 2011 Notably, treatment with dichloroacetate, a PDK2 inhibitor, also decreased the HIF1alpha expression as well as cell proliferation in chronic CSE treated OKF6 cells. Dichloroacetic Acid 24-39 pyruvate dehydrogenase kinase 2 Homo sapiens 43-47 17544412-4 2007 We also show that Y80 and D117 are required for the communication between the DCA-binding site and active site of PDHK2. Dichloroacetic Acid 78-81 pyruvate dehydrogenase kinase 2 Homo sapiens 114-119 19833728-3 2009 In the present study, we investigated the role of the invariant C-terminal DW-motif in inhibition of human PDK2 by dichloroacetate (DCA). Dichloroacetic Acid 115-130 pyruvate dehydrogenase kinase 2 Homo sapiens 107-111 19833728-3 2009 In the present study, we investigated the role of the invariant C-terminal DW-motif in inhibition of human PDK2 by dichloroacetate (DCA). Dichloroacetic Acid 132-135 pyruvate dehydrogenase kinase 2 Homo sapiens 107-111 19833728-11 2009 This signaling network locks PDK2 in the inactive closed conformation, which is in equilibrium with the active open conformation without DCA and ADP. Dichloroacetic Acid 137-140 pyruvate dehydrogenase kinase 2 Homo sapiens 29-33 19147752-8 2009 Inhibition of PDK2 with dichloroacetate decreased HIF1alpha accumulation and reduced cell growth. Dichloroacetic Acid 24-39 pyruvate dehydrogenase kinase 2 Homo sapiens 14-18 18627174-6 2008 Here we show that mutations of three amino acid residues located in the vicinity of the active site of PDHK2 (R250, T302, and Y320) make the kinase resistant to the inhibitory effect of DCA, thereby uncoupling the active site from the allosteric site. Dichloroacetic Acid 186-189 pyruvate dehydrogenase kinase 2 Homo sapiens 103-108 17544412-0 2007 Amino acid residues responsible for the recognition of dichloroacetate by pyruvate dehydrogenase kinase 2. Dichloroacetic Acid 55-70 pyruvate dehydrogenase kinase 2 Homo sapiens 74-105 17544412-2 2007 This study was undertaken in order to map the DCA-binding site of PDHK2. Dichloroacetic Acid 46-49 pyruvate dehydrogenase kinase 2 Homo sapiens 66-71 9405293-8 1998 Apparent Ki values of the isoenzymes for the synthetic analogue of pyruvate, dichloroacetate, varied 40-fold, from 0.2 mM for PDK2 to 8 mM for PDK3. Dichloroacetic Acid 77-92 pyruvate dehydrogenase kinase 2 Homo sapiens 126-130 17222789-5 2007 Molecular inhibition of PDK2 by siRNA mimics DCA. Dichloroacetic Acid 45-48 pyruvate dehydrogenase kinase 2 Homo sapiens 24-28 10748134-10 2000 E2-activated PDK2 activity was stimulated >/=3-fold by reductive acetylation of E2; stimulated PDK2 retained high sensitivity to inhibition by ADP and DCA. Dichloroacetic Acid 154-157 pyruvate dehydrogenase kinase 2 Homo sapiens 13-17 10748134-10 2000 E2-activated PDK2 activity was stimulated >/=3-fold by reductive acetylation of E2; stimulated PDK2 retained high sensitivity to inhibition by ADP and DCA. Dichloroacetic Acid 154-157 pyruvate dehydrogenase kinase 2 Homo sapiens 98-102 10748134-9 2000 E2 activation of PDK2 resulted in a greatly enhanced sensitivity to inhibition by pyruvate or DCA; pyruvate was effective at significantly lower levels than DCA. Dichloroacetic Acid 94-97 pyruvate dehydrogenase kinase 2 Homo sapiens 17-21 10748134-9 2000 E2 activation of PDK2 resulted in a greatly enhanced sensitivity to inhibition by pyruvate or DCA; pyruvate was effective at significantly lower levels than DCA. Dichloroacetic Acid 157-160 pyruvate dehydrogenase kinase 2 Homo sapiens 17-21 31597953-0 2020 Dichloroacetate restores colorectal cancer chemosensitivity through the p53/miR-149-3p/PDK2-mediated glucose metabolic pathway. Dichloroacetic Acid 0-15 pyruvate dehydrogenase kinase 2 Homo sapiens 87-91 34445316-6 2021 However, the DCA-induced alterations in the mRNA and the protein levels of PDK1 and/or PDK2 did not always occur in parallel, implicating a role for post-transcriptional mechanisms. Dichloroacetic Acid 13-16 pyruvate dehydrogenase kinase 2 Homo sapiens 87-91 31597953-9 2020 Taken together, we determined that the p53/miR-149-3p/PDK2 signaling pathway can potentially be targeted with DCA treatment to overcome chemoresistant CRC. Dichloroacetic Acid 110-113 pyruvate dehydrogenase kinase 2 Homo sapiens 54-58 26607904-11 2016 High glycolysis and PDK2 overexpression are closely linked to cisplatin resistance in HNC cells; the latter can be overcome by DCA. Dichloroacetic Acid 127-130 pyruvate dehydrogenase kinase 2 Homo sapiens 20-24 31624634-1 2019 Dichloroacetate (DCA) is an investigational drug targeting the glycolytic hallmark of cancer by inhibiting pyruvate dehydrogenase kinases (PDK). Dichloroacetic Acid 0-15 pyruvate dehydrogenase kinase 2 Homo sapiens 139-142 31624634-1 2019 Dichloroacetate (DCA) is an investigational drug targeting the glycolytic hallmark of cancer by inhibiting pyruvate dehydrogenase kinases (PDK). Dichloroacetic Acid 17-20 pyruvate dehydrogenase kinase 2 Homo sapiens 139-142 31624634-14 2019 Overall, serum concentrations of DCA were sufficient to inhibit the constitutive target PDK2, but unlikely to inhibit targets induced in cancer. Dichloroacetic Acid 33-36 pyruvate dehydrogenase kinase 2 Homo sapiens 88-92 27323896-2 2016 Through molecular docking studies mono- and dihaloacetates are identified as potent PDK2 binders and matched their efficiency with dichloroacetic acid. Dichloroacetic Acid 131-150 pyruvate dehydrogenase kinase 2 Homo sapiens 84-88 28881758-7 2017 Moreover, combining paclitaxel withthe specific PDK2 inhibitor dichloroacetate had a synergistic inhibitory effect on the viability of paclitaxel-resistant lung cancer cells. Dichloroacetic Acid 63-78 pyruvate dehydrogenase kinase 2 Homo sapiens 48-52 24747400-5 2014 Pharmacologic PDK2 blockade with dichloroacetate or lentiviral PDK2 knockdown prevented DeltaPsim hyperpolarization, facilitated apoptosis and reduced myointima formation in injured human mammary and coronary arteries, rat aortas, rabbit iliac arteries and swine (pig) coronary arteries. Dichloroacetic Acid 33-48 pyruvate dehydrogenase kinase 2 Homo sapiens 14-18 25601413-4 2015 Moreover, docking studies revealed putative binding sites of phenylbutyrate on PDK2 and 3 that are located on different sites compared to dichloroacetate (DCA), a previously known PDK inhibitor. Dichloroacetic Acid 138-153 pyruvate dehydrogenase kinase 2 Homo sapiens 79-89 25601413-4 2015 Moreover, docking studies revealed putative binding sites of phenylbutyrate on PDK2 and 3 that are located on different sites compared to dichloroacetate (DCA), a previously known PDK inhibitor. Dichloroacetic Acid 155-158 pyruvate dehydrogenase kinase 2 Homo sapiens 79-89 25482950-3 2014 Dichloroacetate (DCA) is a pyruvate dehydrogenase kinase (PDK) inhibitor that can reverse the Warburg effect. Dichloroacetic Acid 0-15 pyruvate dehydrogenase kinase 2 Homo sapiens 58-61 25482950-3 2014 Dichloroacetate (DCA) is a pyruvate dehydrogenase kinase (PDK) inhibitor that can reverse the Warburg effect. Dichloroacetic Acid 17-20 pyruvate dehydrogenase kinase 2 Homo sapiens 58-61