摘要
果糖-1,6-二磷酸酶(fructose1,6-bisphosptase,FBPase)是位于糖异生过程中第二步的限速酶,在机体血糖调控中发挥重要的生理作用。因此,针对该酶的抑制剂将具有抗糖尿病活性。目前,已有数个FBPase抑制剂分别进入不同临床研究阶段,提示针对该靶点的抗糖尿病药物研发前景十分可观。除此以外,近年研究发现,FBPase还可参与和调节其他疾病如肿瘤的发生、发展过程等。本文将围绕FBPase的结构特征、生理作用、其与2型糖尿病糖异生和胰岛素分泌的关系、FBPase抑制剂的研究进展以及该酶在其他疾病中调控作用等方面作一综述。
Fructose 1, 6-bisphosptase（FBPase）, a second rate-limiting enzyme in gluconeogenesis, has an important role in the control of gluconeogenesis, which involves in energy metabolism and glucose homeostasis. Inhibitors of FBPase exhibit an anti-diabetic activity. Some of FBPase inhibitors have entered the stage of clinical trials, which indicates that FBPase is a promising therapeutic target for the discovery and development of hypoglycemic drugs. In addition, recent studies have shown that FBPase can be used to treat other diseases such as the initiation and development of tumors in several cancer types. Here, we provide a review of the biological characteristics of FBPase and contributions of FBPase on gluconeogenesis and insulin secretion, the research and development of FBPase inhibitors and the regulatory role of FBPase in other diseases.
作者
李荣翠
刘率男
申竹芳
LI Rong-cui;LIU Shuai-nan;SHEN Zhu-fang(Diabetes Research Center of Chinese Academy of Medical Sciences,Key Laboratory of Polymorphic Drugs of Beijing,State Key Laboratory of Bioactive Substances and Functions of Natural Medicines,Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China)
出处
《药学学报》
CAS
CSCD
北大核心
2018年第9期1477-1483,共7页
Acta Pharmaceutica Sinica
基金
国家科技重大专项重大新药创制基金项目(2018ZX09711002-003-012)
中国医学科学院中央级公益性科研院所基本科研业务费(2016ZX350009)
中国医学科学院医学与健康创新工程(2017-I2M-1-010)
关键词
果糖-1
6-二磷酸酶
2型糖尿病
糖异生
胰岛素分泌
fructose-1
6-bisphosptase
type 2 diabetes mellitus
gluconeogenesis
insulin secretion
