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Literature summary extracted from

  • Holland, W.; Morrison, T.; Chang, Y.; Wiernsperger, N.; Stith, B.J.
    Metformin (Glucophage) inhibits tyrosine phosphatase activity to stimulate the insulin receptor tyrosine kinase (2004), Biochem. Pharmacol., 67, 2081-2091.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.10.1 metformin i.e. N,N-dimethylbiguanide or N,N-dimethylimidodicarbonimidic diamide, activates the insulin receptor tyrosine kinase by phosphorylation at Tyr1150 and Tyr1151, and indirectly via inhibition of protein tyrosine phosphatase 1B, metformin does not alter the order of substrate phosphorylation by the insulin receptor tyrosine kinase Homo sapiens
2.7.10.1 metformin i.e. N,N-dimethylbiguanide or N,N-dimethylimidodicarbonimidic diamide, activates the insulin receptor tyrosine kinase by phosphorylation, and indirectly via inhibition of protein tyrosine phosphatase, metformin does not alter the order of substrate phosphorylation by the insulin receptor tyrosine kinase Xenopus laevis
2.7.10.1 additional information activation of the insulin receptor by phosphorylation via its tyrosine kinase activity Homo sapiens
2.7.10.1 additional information activation of the insulin receptor by phosphorylation via its tyrosine kinase activity Xenopus laevis

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.10.1 additional information inhibition of the insulin receptor tyrosine kinase and insulin action by dephosphorylation at Tyr1150 and Tyr1151 via protein tyrosine phosphatase 1B Homo sapiens
2.7.10.1 additional information inhibition of the insulin receptor tyrosine kinase and insulin action by dephosphorylation Xenopus laevis

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.7.10.1 membrane
-
 Homo sapiens 16020
-
2.7.10.1 membrane
-
 Xenopus laevis 16020
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.10.1 Mg2+
-
 Homo sapiens
2.7.10.1 Mn2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.10.1 ATP + a [protein]-L-tyrosine Homo sapiens
-
 ADP + a [protein]-L-tyrosine phosphate
-
 ?
2.7.10.1 ATP + a [protein]-L-tyrosine Xenopus laevis
-
 ADP + a [protein]-L-tyrosine phosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.10.1 Homo sapiens
-
-
-
2.7.10.1 Xenopus laevis
-
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
2.7.10.1 phosphoprotein autophosphorylation of the insulin receptor via its protein tyrosine kinase activity, metformin activates the insulin receptor tyrosine kinase by phosphorylation at Tyr1150 and Tyr1151 Homo sapiens
2.7.10.1 phosphoprotein autophosphorylation of the insulin receptor via its protein tyrosine kinase activity, metformin activates the insulin receptor tyrosine kinase by phosphorylation at Tyr1150 and Tyr1151 Xenopus laevis

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.10.1 oocyte stage IV Xenopus laevis
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.10.1 ATP + a [protein]-L-tyrosine
-
 Homo sapiens ADP + a [protein]-L-tyrosine phosphate
-
 ?
2.7.10.1 ATP + a [protein]-L-tyrosine
-
 Xenopus laevis ADP + a [protein]-L-tyrosine phosphate
-
 ?
2.7.10.1 ATP + insulin receptor substrate 1-L-tyrosine peptide derived from the regulatory domain of insulin receptor Homo sapiens ADP + insulin receptor substrate 1-L-tyrosine phosphate
-
 ?
2.7.10.1 additional information autophosphorylation of the insulin receptor via its protein tyrosine kinase activity, regulation mechanism Homo sapiens ?
-
 ?
2.7.10.1 additional information autophosphorylation of the insulin receptor via its protein tyrosine kinase activity, regulation mechanism Xenopus laevis ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.10.1 insulin receptor kinase
-
 Homo sapiens
2.7.10.1 insulin receptor kinase
-
 Xenopus laevis
2.7.10.1 insulin receptor tyrosine kinase
-
 Homo sapiens
2.7.10.1 insulin receptor tyrosine kinase
-
 Xenopus laevis

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.10.1 7.4
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.10.1 ATP
-
 Homo sapiens