AMPK activators: mechanisms of action and physiological activities.

Exp Mol Med

Department of Biochemistry and Molecular Biology, Graduate School, Kyung Hee University, Seoul, Korea.

Published: April 2016


Category Ranking

98%

Total Visits

921

Avg Visit Duration

2 minutes

Citations

20

Article Abstract

AMP-activated protein kinase (AMPK) is a central regulator of energy homeostasis, which coordinates metabolic pathways and thus balances nutrient supply with energy demand. Because of the favorable physiological outcomes of AMPK activation on metabolism, AMPK has been considered to be an important therapeutic target for controlling human diseases including metabolic syndrome and cancer. Thus, activators of AMPK may have potential as novel therapeutics for these diseases. In this review, we provide a comprehensive summary of both indirect and direct AMPK activators and their modes of action in relation to the structure of AMPK. We discuss the functional differences among isoform-specific AMPK complexes and their significance regarding the development of novel AMPK activators and the potential for combining different AMPK activators in the treatment of human disease.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4855276PMC
http://dx.doi.org/10.1038/emm.2016.16DOI Listing

Publication Analysis

Top Keywords

ampk activators
16
ampk
10
activators mechanisms
4
mechanisms action
4
action physiological
4
physiological activities
4
activities amp-activated
4
amp-activated protein
4
protein kinase
4
kinase ampk
4

Similar Publications

The salt-inducible kinase (SIK) family encompasses three isoforms, SIK1, SIK2, and SIK3, which are members of the AMP-activated protein kinase (AMPK) family of serine/threonine protein kinases. SIK inhibition has emerged as a potential therapeutic approach across multiple indications, as SIKs regulate a diverse set of physiological processes such as metabolism, bone remodeling, immune response, malignancies, skin pigmentation, and circadian rhythm. Within isoform-specific SIK inhibitors there is a need to understand the distinct role of each protein, and here we describe the first SIK1 selective inhibitors.

View Article and Find Full Text PDF

Ethnopharmacological Relevance: Acute lung injury (ALI) is a severe health issue characterized by high morbidity and mortality, driven by excessive inflammatory responses. The traditional Chinese medicine Huashi Baidu Granules (HBG) demonstrated clinical efficacy in treating severe ALI, yet its mechanisms remain unclear.

Aim Of The Study: This research aimed to examine the efficacy and underlying mechanisms of HBG in a lipopolysaccharide (LPS)-induced ALI model, identify core herbal constituents, active compounds, and therapeutic targets, providing a foundation for optimizing HBG-based treatments.

View Article and Find Full Text PDF

Hepatic ischaemia-reperfusion (IR) injury is a serious clinical issue, especially in patients with type 2 diabetes mellitus (T2DM). As mitochondria play a critical role in the regulation of IR-induced liver damage, mitochondria-targeted treatment is of the utmost significance for improving outcomes. The present study explored the mitoprotective role of combined ginsenoside-MC1 (GMC1) and irisin administration in diabetic rats with hepatic IR injury.

View Article and Find Full Text PDF

Creating effective treatments for type 2 diabetes mellitus (T2DM) remains a critical global health challenge. This study investigates the antidiabetic mechanisms of subsp. B-53 ( B-53) in T2DM mice.

View Article and Find Full Text PDF

Kinases are activators of well‑known inflammatory cascades implicated in metabolic disorders, and abnormal activation of casein kinase II (CK2) is associated with several inflammatory disorders. However, thus far, its role in the low‑grade chronic inflammatory response known as 'metaflammation', which is a hallmark of obesity and type 2 diabetes, has not yet been elucidated. The present study aimed to evaluate the role of CK2 in diet‑induced metaflammation and the effects of the CK2 inhibitor 4,5,6,7‑tetrabromobenzotriazole (TBB) on a murine model fed a high‑fat‑high‑sugar (HFHS) diet.

View Article and Find Full Text PDF