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P1, P5-双(5'-腺苷基)五磷酸:这种腺苷酸激酶抑制剂是线粒体过程的底物吗?

P1, P5-Bis-(5'-adenosyl)pentaphosphate: is this adenylate kinase inhibitor substrate for mitochondrial processes?

作者信息

Köhrle J, Lüstorff J, Schlimme E

出版信息

Z Naturforsch C Biosci. 1977 Sep-Oct;32(9-10):786-91. doi: 10.1515/znc-1977-9-1021.

Abstract
  1. P1, P5-Bis-(5'-adenosyl) pentaphosphate (AP5-A) inhibits "soluble" adenylate kinase even when this enzyme is an integral part of the complete mitochondrion. The Ki is 10(-5) M, i.e. about two orders of magnitude higher than the inhibitor contants determined for the purified adenylate kinase of rabbit muscle and an enzyme preparation separated from the mitochondrial intermembrane space. The weaker inhibitory effect is due to a lower accessibility of the enzyme. 2. as to be expected Ap5A which is of the "multisubstrate analogue"-type does not affect mitochondrial nucleoside diphosphate kinase. 3. Though Ap5A owns the structural elements of both ATP and ADP it is not a substrate of the adenine nucleotide carrier, i.e. neither it is exchanged across the inner mitochondrial membrane nor speicifically bound. 4. Ap5A is not metabolized by rat liver mitochondria.
摘要
  1. P1, P5 - 双 -(5'-腺苷基)五磷酸(AP5 - A)即使在“可溶性”腺苷酸激酶是完整线粒体的组成部分时也能抑制它。其抑制常数(Ki)为10⁻⁵ M,即比针对兔肌肉纯化的腺苷酸激酶以及从线粒体外膜间隙分离的酶制剂所测定的抑制常数高约两个数量级。抑制作用较弱是由于该酶的可及性较低。2. 正如所预期的,属于“多底物类似物”类型的Ap5A不影响线粒体核苷二磷酸激酶。3. 尽管Ap5A具有ATP和ADP的结构元件,但它不是腺嘌呤核苷酸载体的底物,即它既不能在线粒体内膜上进行交换,也不会特异性结合。4. Ap5A不能被大鼠肝脏线粒体代谢。

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