Enzyme inhibition by fluoro compounds.
Enzyme inhibition by fluoro compounds.
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DOI：
10.1016/s0021-9258(17)44813-7
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发表时间：
1990-10
期刊：
影响因子：
--
通讯作者：
R. Abeles;T. Alston
中科院分区：
文献类型：
--
作者：
R. Abeles;T. Alston
鉴于其空间结构紧凑，强烈的电负性，和几乎异生物质的地位，氟是一个有吸引力的取代基的建设抑制类似物的酶底物。早期对这种可能性的兴趣是由乙酰胆碱酯酶的氟磷灭活剂的戏剧性效果、氟乙酸作为“致命合成”的一种情况的毒性以及尿嘧啶的5-氟抗代谢物的化疗效果所激发的。现在广泛的主题的方面的几个评论是可用的（例如，参考文献。1 -7），这Minireview主要集中在酶抑制剂，其中氟有助于抑制，而不作为离去基团。
In view of its steric compactness, intense electronegativity, and virtually xenobiotic status,’fluorine is an appealing substituent for the construction of inhibitory analogs of enzyme substrates. Early interest in this possibility was spurred by the dramatic effects of the fluorophosphorus inactivators of acetylcholinesterase, the toxicity of fluoroacetate as a case of “lethal synthesis,” and the chemotherapeutic efficacy of the 5-fluoro antimetabolite of uracil. Several reviews of aspects of the now extensive subject are available (for instance, Refs. l-7), and this Minireview focuses principally on enzyme inhibitors in which fluorine contributes to the inhibition without functioning as a leaving group.