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Literature summary for 2.7.10.1 extracted from

  • McLaughlin, S.; Smith, S.O.; Hayman, M.J.; Murray, D.
    An electrostatic engine model for autoinhibition and activation of the epidermal growth factor receptor (EGFR/ErbB) family (2005), J. Gen. Physiol., 126, 41-53.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
Calmodulin ligand-binding induced dimerization enables transautophosphorylation of ErbB1 which results in enhanced intracellular Ca2+ concentration activating calmodulin which reverses autoinhibition by net charge changes in the juxtamembranes Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expressed in COS-1 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information autoinhibition mechanism based on a structural model including the 2 juxtamembranes and the protein tyrosine kinase domain binding electrostatically to acidic lipids in the plasma membrane restricting access to the substrate tyrosines, reversible by ligand-binding induced dimerization and subsequent transautophosphorylation and Ca2+/calmodulin induced net charge changes in the juxtamembranes Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information lipid ligand-binding kinetics of ErbB1, plasma membrane binding kinetics of enzyme-derived peptides, overview Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
Homo sapiens 16020
-

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ ligand-binding induced dimerization enables transautophosphorylation of ErbB1 which results in enhanced intracellular cytoplasmic Ca2+ concentration activating calmodulin which reverses autoinhibition by net charge changes in the juxtamembranes Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens enzyme regulation via reversible autophosphorylation, binding to plasma membrane of enzyme and enzyme-derived peptides, overview ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P00533 ErbB1
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein ligand-binding induced dimerization enables transautophosphorylation of ErbB1 which results in enhanced intracellular Ca2+ concentration activating calmodulin which reverses autoinhibition by net charge changes in the juxtamembranes, activation Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information enzyme regulation via reversible autophosphorylation, binding to plasma membrane of enzyme and enzyme-derived peptides, overview Homo sapiens ?
-
?

Subunits

Subunits Comment Organism
dimer ligand-binding induced dimerization Homo sapiens
More ligand-binding induced dimerization enables transautophosphorylation of ErbB1 which results in enhanced intracellular Ca2+ concentration activating calmodulin which reverses autoinhibition by net charge changes in the juxtamembranes, activation, structural model Homo sapiens

Synonyms

Synonyms Comment Organism
Egfr
-
Homo sapiens
epidermal growth factor receptor
-
Homo sapiens
ERBB1
-
Homo sapiens
More the enzymes belong to the epidermal growth factor receptor family, i.e. EGFR/ErbB family Homo sapiens