AMP activated protein kinase (AMPK) is a key regulator of cellular metabolism. AMPK activity is modulated in part by binding of AMP to the gamma-subunit of the kinase, which increases the activity of the catalytic alpha-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 alpha(1)beta(1)gamma(1) and alpha(2)beta(1)gamma(1) isoforms in response to small molecule activators and inhibitors.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2774621 | PMC |
| http://dx.doi.org/10.2174/1875397300801010034 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Hepatoprotective effects of polysaccharide from Morchella esculenta are associated with activation of the AMPK/Sirt1 signaling pathway in mice with NAFLD.
Int J Biol Macromol
January 2025
Department of Cardiovascular Surgery, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, Anhui 230001, China. Electronic address:
The functional food application of edible fungus polysaccharides has been widely studied based on their variety of potential pharmacological activities. However, the hepatoprotective effects and mechanisms of Morchella esculenta polysaccharide against nonalcoholic fatty liver disease (NAFLD) remain unknown. A high-fat diet (HFD) fed C57BL/6 J mice for 8 weeks was employed to establish NAFLD with simple steatosis, methionine choline deficiency (MCD) diet for 4 weeks induced hepatic steatohepatitis and fibrosis.
View Article and Find Full Text PDFBeneficial Effects of the Herbal Medicine Zuo Gui Wan in a Mice Model of Alzheimer's Disease via Drp1-Mediated Inhibition of Mitochondrial Fission and Activation of AMPK/PGC-1α-regulated Mitochondrial Bioenergetics.
J Ethnopharmacol
January 2025
School of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China. Electronic address:
Ethnopharmacological Relevance: Zuo Gui Wan (ZGW) is a well-known traditional Chinese medicine decoction used for approximately 400 years to treat age-related degenerative conditions, including cognitive impairment in older adults, osteoporosis, and general aging. However, the mechanism of action for ZGW remains unclear.
Aims Of The Study: This study aims to investigate the efficacy of ZGW in improving cognitive function in Alzheimer's disease (AD) animal models and to explore the underlying mechanisms, presenting a novel perspective in the field.
Maslinic acid improves mitochondrial function and inhibits oxidative stress and autophagy in human gastric smooth muscle cells.
Open Life Sci
January 2025
Department of Pediatrics, Fujian Provincial Hospital, Shengli Clinical Medical College of Fujian Medical University, No. 134 Dong Street, Fuzhou, Fujian, 350001, China.
Functional dyspepsia (FD) is a chronic disease that occurs in the gastroduodenal region and significantly impacts human health. Maslinic acid (MA), a pentacyclic triterpene acid, is the primary bioactive ingredient in Chinese medicinal herbs such as hawthorn, which exhibits beneficial impacts on the regulation of various disease progressions. However, the specific functions and associated pathways of MA in FD progression remain unclear and require further investigation.
View Article and Find Full Text PDFBone marrow mesenchymal stem cell-derived extracellular vesicles alleviate diabetes-exacerbated atherosclerosis via AMPK/mTOR pathway-mediated autophagy-related macrophage polarization.
Cardiovasc Diabetol
January 2025
Department of Cardiology, Beijing Anzhen Hospital, Capital Medical University, No.2 Anzhen Road, Chaoyang District, 100029, Beijing, China.
Introduction: Bone marrow-derived mesenchymal stem cell-derived extracellular vesicles (BMSC-EVs) are widely used for therapeutic purposes in preclinical studies. However, their utility in treating diabetes-associated atherosclerosis remains largely unexplored. Here, we aimed to characterize BMSC-EV-mediated regulation of autophagy and macrophage polarization.
View Article and Find Full Text PDFMitochondrial dysfunction-driven AMPK-p53 axis activation underpins the anti-hepatocellular carcinoma effects of sulfane sulfur.
Sci Rep
January 2025
Guangzhou Municipal and Guangdong Provincial Key Laboratory of Protein Modification and Disease, School of Basic Medical Sciences, Guangzhou Medical University, Guangzhou, 511436, China.
Hepatocellular carcinoma (HCC) is the most prevalent form of primary liver cancer, notoriously refractory to conventional chemotherapy. Historically, sulfane sulfur-based compounds have been explored for the treatment of HCC, but their efficacy has been underwhelming. We recently reported a novel sulfane sulfur donor, PSCP, which exhibited improved chemical stability and structural malleability.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!