Sanguinarine is an allosteric activator of AMP-activated protein kinase
28
Citation
41
Reference
10
Related Paper
Citation Trend
Keywords:
Sanguinarine
AMP-Activated Protein Kinase
AMP-activated kinase (AMPK) is central to sensing energy status in eukaryotic cells via binding of AMP and ATP to CBS (cystathionine beta-synthase) domains in the regulatory gamma subunit. The structure of a CBS-domain pair from human AMPK gamma1 in complex with the physiological activator AMP and the pharmacological activator ZMP (AICAR) is presented.
Gamma subunit
Cite
Citations (86)
AMP-activated protein kinase (AMPK) is a key sensor and regulator of glucose, lipid, and whole body energy metabolism. Activation of AMPK alleviates the symptoms of metabolic abnormalities associated with metabolic diseases including obesity and type 2 diabetes. The oriental traditional medicinal he...
AMP-Activated Protein Kinase
Cite
Citations (0)
AMP-Activated Protein Kinase
Cite
Citations (0)
Sanguinarine
AMP-Activated Protein Kinase
Cite
Citations (28)
A sensor of cellular energy status,the AMP-activated protein kinase( AMPK) exerts some effects on the modulation of glucose and lipid metabolism,which is highly related with cell viability and survival. AMPK is also activated by drugs such as metformin and salicylate. In addition,studies have shown that AMPK also exerts a wide range of effects on the signaling pathways including inflammation,cancer and metabolic disorders. The article focuses on the new findings of AMPK.
AMP-Activated Protein Kinase
Cite
Citations (0)
AMP activated protein kinase (AMPK) is a key regulator of cellular metabolism. AMPK activity is modulated in part by binding of AMP to the γ-subunit of the kinase, which increases the activity of the catalytic α-subunit. Because increased AMPK activity in the liver and in skeletal muscle leads to increased fatty acid oxidation and decreased cholesterol and fatty acid biosynthesis, activators of AMPK are being sought for treatment of type-2 diabetes and other metabolic disorders. The unique mechanism of AMPK activation offers an opportunity to develop small molecules that directly upregulate AMPK activity, and there exists a need for simplified methods to identify and characterize small-molecules that show isoform-specific effects on AMPK. We have developed a suite of fluorescence-based assays to identify and characterize such compounds, and have used these to characterize and compare activity of recombinant AMPK α1β1γ1 and α2β1γ1 isoforms in response to small molecule activators and inhibitors.
AMP-Activated Protein Kinase
Cite
Citations (2)
目的 Coptidis 根茎(CR ) ，亚洲植物(包括的黄连属 chinensis Franch ) 的弄干的根茎，被用来对待糖尿病 mellitus 几千年。我们探索了 CR 在骨胳的肌肉上直接扮演的可能性，为葡萄糖动态平衡负责的主要机关，并且激活 5-AMP-activated 蛋白质 kinase (AMPK ) ，导致骨胳的肌肉的新陈代谢的改进的一个发信号的中间人。孤立的老鼠 epitrochlearis 和 soleus 肌肉在包含一篇 CR 水摘录(CE ) 的一个缓冲区被孵化的方法，和 AMPK 和相关事件的激活被检验。响应 CE 治疗的结果，在 AMPK 的催化子单元的 Thr172 的 phosphorylation，为完整的 kinase 激活的必要的步，在两肌肉增加了。乙酰 CoA carboxylase (ACC ) 的 Ser79 的 Phosphorylation， AMPK 的内长的底层，附随地增加了。isoform 特定的 AMPK 活动的分析表明 CE 两个都激活催化子单元的 1 和 2 isoforms。重要地， AMPK phosphorylation 上的 CE 的最大的效果比 berberine (BBR ) 的显著地大，显示 CE 的行动完全没被归功于到 BBR。我们建议那 CE 的结论是在快抽动、慢抽动的骨胳的肌肉的 AMPK 的尖锐使活跃之物。
AMP-Activated Protein Kinase
Acetyl-CoA Carboxylase
Cite
Citations (0)
AMP-Activated Protein Kinase
Cite
Citations (242)
AMP-Activated Protein Kinase
Cite
Citations (11)
AMP-Activated Protein Kinase
Cite
Citations (0)