Inhibition of Enzymes which Interact with Citrate by (—)Hydroxycitrate and 1,2,3,‐Tricarboxybenzene

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<jats:p>The effects of two citrate analogues, (—)hydroxycitrate and 1,2,3‐tricarboxybenzene, were studied using rat liver enzymes which interact with citrate.</jats:p><jats:p>The most pronounced effect of 1,2,3‐tricarboxybenzene was inhibition of acetyl‐CoA carboxylase (<jats:italic>K</jats:italic><jats:sub>i</jats:sub> 20 μM). It also inhibited the mitochondrial citrate transporter (50% inhibition at 3 mM), but was not a substrate for this transporter.</jats:p><jats:p>ATP‐citrate lyase was markedly inhibited by both free (—)hydroxycitrate (<jats:italic>K</jats:italic><jats:sub>i</jats:sub> 8 μM) and (—)hydroxycitrate lactone (<jats:italic>K</jats:italic><jats:sub>i</jats:sub> 50 to 100 μM). Acetyl‐CoA carboxylase was activated by both the forms of (—)hydroxycitrate (<jats:italic>K</jats:italic><jats:sub>a</jats:sub> 0.7 mM and 1.6 mM, respectively). (—)Hydroxycitrate is a substrate for the mitochondrial citrate transporter, but its rate of transport is less than 10% of that of citrate.</jats:p><jats:p>Other citrate metabolizing enzymes also were inhibited by 1,2,3‐tricarboxybenzene and (—)hydroxycitrate but much higher concentrations were required.</jats:p>

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