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Literature summary for 2.7.11.31 extracted from
- Role of AMP-activated protein kinase in the control of appetite (2008), J. Neuroendocrinol., 20, 942-951.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| 5-aminoimidazole-4-carboxamide riboside | AICAR | Rattus norvegicus |  |
| 5-aminoimidazole-4-carboxamide riboside | AICAR is able to reverse both the inhibitory effect on pAMPK and the C75-induced anorexia | Mus musculus | |
| corticosterone | counteracts inhibiting effect of sucrose and increases hypothalamic AMPK activity to levels comparable with saline-drinking animals | Rattus norvegicus | |
| D-glucose | - |
Rattus norvegicus | |
| dexamethasone | induces increase in AMPK in primary rat hypothalamic cell cultures, suggesting a direct effect of glucocorticoids on AMPK activity | Rattus norvegicus | |
| Insulin | insulin-induced hypoglycaemia in rats increases AMPK phosphorylation and alpha2AMPK activity in the arcuate nucleus/dorso-mediobasal hypothalamus and paraventricular nucleus | Rattus norvegicus | |
| leptin | has a tissue-specific effect on AMPK. In the skeletal muscle, it stimulates AMPK activity | Rattus norvegicus | |
| metformin | anti-diabetic agent, stimulates AMPK in the liver and in the muscle | Homo sapiens | |
| additional information | fasting results in activation of AMPK | Mus musculus | |
| additional information | inhibition of intracellular glucose utilisation through the administration of 2-deoxyglucose increases hypothalamic AMPK activity and food intake. Diabetic rats have enhanced AMPK activity, despite their high glucose levels, which should suppress hypothalamic AMPK. Thyroid hormones stimulate AMPK and acetyl-CoA carboxylase expression in skeletal muscle. 1 h of strenuous exercise in rats does not elicit significant changes in hypothalamic AMPK activity despite an increase in plasma ghrelin | Rattus norvegicus | |
| MT-II | melanocortin 4 receptor agonist, significantly augments AMPK and acetyl-CoA carboxylase phosphorylation, MT-II is a potent AMPK activator in muscle, even in mice on a high fat diet | Mus musculus | |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 6-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-3-pyridin-4-yl-pyrrazolo[1,5-a]-pyrimidine | compound C | Rattus norvegicus | |
| C75 | rapidly reduces the level of the phosphorylated AMPKalpha subunit in the hypothalamus. Also reduces pAMPK levels in fasted mice that have elevated hypothalamic pAMPK | Mus musculus | |
| leptin | has a tissue-specific effect on AMPK, in the hypothalamus, it decreases hypothalamic AMPK activity | Rattus norvegicus | |
| metformin | can inhibit the stimulatory effect of dexamethasone in primary hypothalamic culture, blocks the AMPK phosphorylation induced by low glucose in primary cultures of hypothalamic neurones | Rattus norvegicus | |
| additional information | SOCS3, an inhibitor of leptin-STAT3 signalling, inhibits leptin activation of AMPK in primary myotubes | Homo sapiens | |
| additional information | re-feeding after fasting inhibits AMPK activity in multiple hypothalamic regions. Diet-induced obesity mice have suppressed AMPK activity in the paraventricular nucleus of the hypothalamus, AMPK is suppressed to the level in leptin-treated chow-fed mice, and there is no further effect of leptin. In mice, diet-induced obesity alters the effect of leptin on AMPK activity not only in the hypothalamus, but also in the skeletal muscle. Adiponectin-deficient mice show decreased AMPK phosphorylation in the arcuate nucleus. In leptin-over-expressing transgenic mice on a high fat diet, muscle AMPK phosphorylation and acetyl-CoA carboxylase phosphorylation are reduced compared with standard diet leptin-over-expressing transgenic mice and are comparable to high fat diet-non-transgenic mice. Leptin i.c.v., in addition to transgenic hyperleptinaemia, is not able to restore the impaired AMPK signalling because of the induced generalised leptin resistance | Mus musculus | |
| additional information | lower basal AMPK activity in paraventricular nucleus may be due to effects of hyperinsulinaemia and/or hyperglycaemia, which suppress AMPK activity in multiple hypothalamic nuclei | Rattus norvegicus | |
| propylthiouracil | inhibits stimulation by thyroid hormones | Rattus norvegicus | |
| sucrose | sucrose-drinking animals have lower hypothalamic AMPK activity compared to saline-drinking control rats | Rattus norvegicus | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
- |
- |
| Rattus norvegicus | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| brain | AMPK is widely expressed throughout the brain, including several areas controlling food intake and neuroendocrine function | Mus musculus | - |
| hindbrain | - |
Mus musculus | - |
| hypothalamus | - |
Mus musculus | - |
| hypothalamus | dorso-mediobasal | Rattus norvegicus | - |
| liver | - |
Homo sapiens | - |
| additional information | arcuate nucleus | Mus musculus | - |
| additional information | arcuate nucleus | Rattus norvegicus | - |
| muscle | - |
Homo sapiens | - |
| myotube | - |
Homo sapiens | - |
| neuron | - |
Rattus norvegicus | - |
| neuron | mainly neuronal distribution of the various AMPK isoforms | Mus musculus | - |
| paraventricular nucleus | - |
Mus musculus | - |
| paraventricular nucleus | - |
Rattus norvegicus | - |
| plasma | - |
Rattus norvegicus | - |
| skeletal muscle | - |
Rattus norvegicus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + acetyl-CoA carboxylase | - |
Mus musculus | ADP + [acetyl-CoA carboxylase]phosphate | - |
? | |
| ATP + acetyl-CoA carboxylase | - |
Rattus norvegicus | ADP + [acetyl-CoA carboxylase]phosphate | - |
? | |
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 |
Expression
| Organism | Comment | Expression |
|---|---|---|
| Rattus norvegicus | 3 days of recurrent insulin-induced hypoglycaemia results in an increase in the gene expression of alpha1- and alpha2AMPK in the whole hypothalamus and in the dorso-mediobasal hypothalamus | up |
General Information
| General Information | Comment | Organism |
|---|---|---|
| malfunction | Agouti-related peptide alpha2 AMPK-KO mice show decreased body weight even though there are no changes in food intake or energy expenditure and, the difference in body weight is lost when the animals are fed a high fat diet. Pro-opiomelanocortin alpha2 AMPK-KO animals show increased body weight and adiposity, which is further enhanced by a high fat diet | Mus musculus |
| physiological function | AMPK mediates cold-induced resistance to anorexigenic signalling in the hypothalamus. Activation of AMPK can contribute to hyperphagia. Inhibition of AMPK inhibits the hypoglycaemia-induced increase in the counter-regulatory hormones glucagon, corticosterone and catecholamines, causing a severe and prolonged hypoglycaemia | Rattus norvegicus |
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