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[与果糖-1,6-二磷酸酶AMP位点结合的变构抑制剂发现的最新进展]

[Recent advance in the discovery of allosteric inhibitors binding to the AMP site of fructose-1,6-bisphosphatase].

作者信息

Li Zhan-mei, Bie Jian-bo, Song Hong-rui, Xu Bai-ling

机构信息

Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

出版信息

Yao Xue Xue Bao. 2011 Nov;46(11):1291-300.

Abstract

Fructose-1, 6-bisphosphatase (FBPase), a rate-limiting enzyme involved in the pathway of gluconeogenesis, can catalyze the hydrolysis of fructose-1, 6-bisphosphate to fructose-6-phosphate. Upon inhibiting the activity of FBPase, the production of endogenous glucose can be decreased and the level of blood glucose lowered. Therefore, inhibitors of FBPase are expected to be novel potential therapeutics for the treatment of type II diabetes. Recent research efforts were reviewed in the field of developing allosteric inhibitors interacting with the AMP binding site of FBPase.

摘要

果糖-1,6-二磷酸酶(FBPase)是糖异生途径中的一种限速酶,可催化果糖-1,6-二磷酸水解为果糖-6-磷酸。抑制FBPase的活性后,内源性葡萄糖的生成会减少,血糖水平会降低。因此,FBPase抑制剂有望成为治疗II型糖尿病的新型潜在疗法。本文综述了在开发与FBPase的AMP结合位点相互作用的变构抑制剂领域的最新研究成果。

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