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Literature summary for 2.7.11.31 extracted from
- Insulin resistance and fuel homeostasis: the role of AMP-activated protein kinase (2009), Acta Physiol. (Oxf.), 196, 129-145.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| 5-aminoimidazole-4-carboxamide riboside | AICAR | Mus musculus |  |
| 5-aminoimidazole-4-carboxamide riboside | AICAR, activates AMPK, whereby increasing the rate of fatty acid oxidation in isolated human muscle strips and cultured human skeletal muscle cells. In isolated human muscle strips, AICAR induces glucose uptake, that is associated with increased translocation of the glucose transporter, GLUT4, to the plasma membrane | Homo sapiens | |
| 5-aminoimidazole-4-carboxamide riboside | AICAR, in perfused hindlimb, AICAR induces glucose uptake, that is associated with increased translocation of the glucose transporter, GLUT4, to the plasma membrane. Reduces insulin-stimulated glycogen synthase activity in isolated skeletal muscle. Diminishes ectopic lipid deposition in liver and muscle of Zucker diabetic fatty rats and slows the progression to type 2 diabetes in these animals | Rattus norvegicus | |
| A-769662 | small molecule direct activator of AMPK, increases glucose uptake in both L6 myotubes and primary myotubes | Homo sapiens | |
| A-769662 | small molecule direct activator of AMPK, reduces fatty acid synthesis in primary hepatocytes | Rattus norvegicus | |
| A-769662 | small molecule direct activator of AMPK, treatment of ob/ob mice for 5 days decreases plasma glucose and triglyceride concentrations, lowers hepatic triglyceride content and reduces expression of gluconeogenesis genes in the liver | Mus musculus | |
| adiponectin | activation of AMPK, which is mediated via cell surface receptor AdipoR1 | Mus musculus | |
| additional information | in healthy humans, an acute bout of exercise activates AMPK in an isoform and intensity-dependent manner | Homo sapiens |
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | AMPK is a highly attractive target for the prevention and treatment of type 2 diabetes and other disorders of the metabolic syndrome, and to curb the prevalence and costs of type 2 diabetes | Homo sapiens |
| drug development | AMPK is a highly attractive target for the prevention and treatment of type 2 diabetes and other disorders of the metabolic syndrome, and to curb the prevalence and costs of type 2 diabetes | Rattus norvegicus |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
- |
- |
| Rattus norvegicus | - |
Sprague-Dawley rats | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| hepatocyte | - |
Mus musculus | - |
| hepatocyte | - |
Rattus norvegicus | - |
| hindlimb | - |
Rattus norvegicus | - |
| liver | - |
Mus musculus | - |
| liver | - |
Rattus norvegicus | - |
| muscle | strip | Homo sapiens | - |
| myocyte | - |
Homo sapiens | - |
| myotube | L6 myotubes and primary myotubes | Homo sapiens | - |
| skeletal muscle | - |
Mus musculus | - |
| skeletal muscle | - |
Homo sapiens | - |
| skeletal muscle | - |
Rattus norvegicus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | AMPK phosphorylates histone deacetylase 5 (HDAC5) at Ser259 and Ser498 in primary myocytes | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| AMP-activated protein kinase | - |
Mus musculus |
| AMP-activated protein kinase | - |
Homo sapiens |
| AMP-activated protein kinase | - |
Rattus norvegicus |
| AMPK | - |
Mus musculus |
| AMPK | - |
Homo sapiens |
| AMPK | - |
Rattus norvegicus |
General Information
| General Information | Comment | Organism |
|---|---|---|
| malfunction | mice lacking either the alpha1 or alpha2 AMPK catalytic subunits demonstrate that AMPK is required for the effect of AICAR on glucose uptake. Transgenic mice expressing an inactive form of AMPK alpha2 subunit specifically in skeletal muscle develop impaired whole-body glucose tolerance and iInsulin resistance in skeletal muscle, particularly when fed a high-fat diet | Mus musculus |
| metabolism | plays an important role in the regulation of both lipid and glucose metabolism. Direct link between AMPK activation and fatty acid metabolism. Has the potential of ameliorating insulin resistance and improving glucose homeostasis. A gain-of-function mutation in the gene encoding AMPK gamma3-subunit is reported to confer beneficial effects on muscle fuel metabolism | Homo sapiens |
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