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Open AccessJournal ArticleDOI

Activation of pyruvate dehydrogenase in perfused rat heart by dichloroacetate (Short Communication).

Sue Whitehouse, +1 more
- 01 Jun 1973 - 
- Vol. 134, Iss: 2, pp 651-653
TLDR
Evidence is given that dichloroacetate may facilitate the conversion of pyruvate dehydrogenase from an inactive (phosphorylated) form into an active (dephosphorylation) form.
Abstract
The activity of pyruvate dehydrogenase was assayed in extracts of rat hearts perfused in vitro with media containing glucose and insulin±acetate±dichloroacetate. Dichloroacetate (100μm, 1mm or 10mm) increased the activity of pyruvate dehydrogenase in perfusions with glucose or glucose+acetate. Evidence is given that dichloroacetate may facilitate the conversion of pyruvate dehydrogenase from an inactive (phosphorylated) form into an active (dephosphorylated) form.

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Journal ArticleDOI

The pharmacology of dichloroacetate.

TL;DR: Despite its potential toxicity and limited clinical experience, DCA and its derivatives may prove to be useful in probing regulatory aspects of intermediary metabolism and in the acute or chronic treatment of several metabolic disorders.
Journal ArticleDOI

Mechanism of activation of pyruvate dehydrogenase by dichloroacetate and other halogenated carboxylic acids.

TL;DR: It is concluded that the inhibition of pyruvate dehydrogenase kinase by dichloroacetate may account for the activation of pyrivate dehydration and pyruVate oxidation which it induces in isolated rat heart and diaphragm muscles, subject to certain assumptions as to the distribution of dichlorOacetate across the plasma membrane and the mitochondrial membrane.
Journal ArticleDOI

Anticancer Targets in the Glycolytic Metabolism of Tumors: A Comprehensive Review

TL;DR: This review addresses in a comprehensive manner the main molecular events accounting for high-rate glycolysis in cancer, and highlights the key role exerted by the hypoxia-inducible transcription factor HIF-1 in long-term adaptation to Hypoxia.
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