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Title 

Antidiabetic and antiobesity effects of Ampkinone (6f), a novel small molecule activator of AMP-activated protein kinase

 

AMPK를 타겟으로 하는 Ampkinone의 항 비만 및 항 당뇨 효과

Authors 

S OhS J KimJung Hwan HwangH Y LeeM J RyuJ ParkY S JoY K KimChul Ho LeeK R KweonM ShongS B Park

Publisher 

American Chemical Society

Issue Date 

2010

Citation 

Journal of Medicinal Chemistry, vol. 53, no. 20, pp. 7405-7413

Abstract 

Adenosine 5'-monophosphate (AMP) activated protein kinase (AMPK) has emerged as an attractive target molecule for the treatment of metabolic disorders, including obesity and type 2 diabetes. In this study, we identified a novel small molecule, ampkinone (6f), as an indirect AMPK activator, which was derived from the small molecule library constructed by diversity-oriented synthesis. Ampkinone stimulated the phosphorylation of AMPK via the indirect activation of AMPK in various cell lines. Ampkinone-mediated activation of AMPK required the activity of LKB1 and resulted in increased glucose uptake in muscle cells. In addition, ampkinone-treated DIO mice significantly reduced total body weight and overall fat mass. Histological examination and measurement of lipid parameters showed that ampkinone effectively improved metabolic abnormalities in the DIO mice model. Our results demonstrate that ampkinone, a small molecule with a privileged benzopyran substructure, has a potential as a new class of therapeutic agent for antidiabetic and antiobesity treatment via the indirect stimulation of AMPK.

ISSN 

0022-2623

Link 

http://dx.doi.org/10.1021/jm100565d

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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