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Literature summary for 2.7.11.31 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

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

Cloned(Commentary)

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

Protein Variants

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

Inhibitors

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
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

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

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

Source Tissue

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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
-
?
ATP + acetyl-CoA carboxylase phosphorylation at Ser79, phosphorylation inhibits the acetyl-CoA carboxylase Homo sapiens ADP + phosphorylated acetyl-CoA carboxylase
-
?

Synonyms

Synonyms Comment Organism
AMP-activated protein kinase
-
Homo sapiens
AMPK
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens