Recent advance in the discovery of allosteric inhibitors binding to the AMP site of fructose-1,6-bisphosphatase.
- Author:
Zhan-mei LI
1
;
Jian-bo BIE
;
Hong-rui SONG
;
Bai-ling XU
Author Information
1. Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
- Publication Type:Journal Article
- MeSH:
Adenosine Monophosphate;
chemistry;
Allosteric Site;
Animals;
Binding Sites;
Blood Glucose;
metabolism;
Diabetes Mellitus, Type 2;
blood;
Enzyme Inhibitors;
chemistry;
pharmacology;
Fructose-Bisphosphatase;
antagonists & inhibitors;
chemistry;
metabolism;
Fructosediphosphates;
metabolism;
Fructosephosphates;
metabolism;
Humans
- From:
Acta Pharmaceutica Sinica
2011;46(11):1291-1300
- CountryChina
- Language:Chinese
-
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.
