用α-氰基-β-（1-苯基吲哚-3-基）丙烯酸酯测定大鼠肝脏和心脏线粒体中丙酮酸载体的浓度。
The concentration of the mitochondrial pyruvate carrier in rat liver and heart mitochondria determined with alpha-cyano-beta-(1-phenylindol-3-yl)acrylate.
作者信息
Shearman M S, Halestrap A P
出版信息
Biochem J. 1984 Nov 1;223(3):673-6. doi: 10.1042/bj2230673.
Abstract
alpha-Cyano-beta-(1-phenylindol-3-yl)acrylate inhibited pyruvate transport into both liver and heart mitochondria approximately linearly with respect to its concentration until 65% inhibition was achieved. The extent of inhibition was dependent on the mitochondrial protein concentration. By extrapolation of plots of inhibition versus inhibitor concentration to total inhibition, or by mathematical analysis of the plots, the concentration of pyruvate transporter molecules per mg of protein was calculated to be approximately 100 pmol/mg for both heart and liver mitochondria, and the Ki about 7 nM. The data also suggest that pyruvate transport is rate-limiting for pyruvate oxidation by heart mitochondria in State 3, but not by liver mitochondria.
摘要
α-氰基-β-(1-苯基吲哚-3-基)丙烯酸酯抑制丙酮酸转运至肝脏和心脏线粒体，在达到65%抑制率之前，其抑制作用随浓度增加大致呈线性关系。抑制程度取决于线粒体蛋白浓度。通过将抑制率与抑制剂浓度的关系图外推至完全抑制，或对这些图进行数学分析，计算得出心脏和肝脏线粒体每毫克蛋白中丙酮酸转运体分子的浓度约为100 pmol/mg，Ki约为7 nM。数据还表明，在状态3下，丙酮酸转运是心脏线粒体丙酮酸氧化的限速步骤，但不是肝脏线粒体的限速步骤。
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