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Literature summary extracted from

  • Zang, M.; Zuccollo, A.; Hou, X.; Nagata, D.; Walsh, K.; Herscovitz, H.; Brecher, P.; Ruderman, N.B.; Cohen, R.A.
    AMP-activated protein kinase is required for the lipid-lowering effect of metformin in insulin-resistant human HepG2 cells (2004), J. Biol. Chem., 279, 47898-47905.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.31 AMP dependent on Homo sapiens
2.7.11.31 metformin increases the activating phosphorylation of the enzyme at Thr172 of the alpha-subunit by 3.6fold Homo sapiens
2.7.11.31 additional information phosphorylation activates the enzyme Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.31 expression of mutant enzymes in Escherichia coli and, via adenovirus transfection, in Hep-G2 cells Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.7.11.31 K45R site-directed mutagenesis, a dominant-negative mutant, expression leads to accumulation of lipids in cells Homo sapiens
2.7.11.31 T172D site-directed mutagenesis, constitutively active mutant of AMPK, insensitive to metformin Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.31 additional information insulin-resistance caused by high levels of D-glucose in the cell decreases the enzyme activity Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.27 ATP + [acetyl-CoA carboxylase] Homo sapiens AMPKalpha negatively regulates activity of acetyl-CoA carboxylase and hepatic lipid content ADP + [acetyl-CoA carboxylase] phosphate
-
 ?
2.7.11.31 ATP + acetyl-CoA carboxylase Homo sapiens the enzyme is involved in the regulation of hepatic lipids via its downstream effector acetyl-CoA carboxylase, enzyme inhibition leads to an increased level of triacylglycerols and accumulation of lipids, metformin decreases lipid accumulation, induced by high D-glucose levels, by activating the enzyme, the enzyme functions as energy intracellular sensor ADP + phosphorylated acetyl-CoA carboxylase
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.27 Homo sapiens
-
-
-
2.7.11.31 Homo sapiens
-
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
2.7.11.31 phosphoprotein the enzyme is phosphorylated at Thr172 of its alpha-subunit, phosphorylation activates the enzyme, metformin increases the enzyme phosphorylation Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.31 Hep-G2 cell hepatoma cell line Homo sapiens
-
2.7.11.31 liver
-
 Homo sapiens
-
2.7.11.31 skeletal muscle
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.27 ATP + [acetyl-CoA carboxylase]
-
 Homo sapiens ADP + [acetyl-CoA carboxylase] phosphate
-
 ?
2.7.11.27 ATP + [acetyl-CoA carboxylase] AMPKalpha negatively regulates activity of acetyl-CoA carboxylase and hepatic lipid content Homo sapiens ADP + [acetyl-CoA carboxylase] phosphate
-
 ?
2.7.11.31 ATP + acetyl-CoA carboxylase the enzyme is involved in the regulation of hepatic lipids via its downstream effector acetyl-CoA carboxylase, enzyme inhibition leads to an increased level of triacylglycerols and accumulation of lipids, metformin decreases lipid accumulation, induced by high D-glucose levels, by activating the enzyme, the enzyme functions as energy intracellular sensor Homo sapiens ADP + phosphorylated acetyl-CoA carboxylase
-
 ?
2.7.11.31 ATP + acetyl-CoA carboxylase phosphorylation at Ser79, phosphorylation inhibits the acetyl-CoA carboxylase Homo sapiens ADP + phosphorylated acetyl-CoA carboxylase
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.27 AMPKalpha
-
 Homo sapiens
2.7.11.31 AMP-activated protein kinase
-
 Homo sapiens
2.7.11.31 AMPK
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.31 ATP
-
 Homo sapiens