Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.10.1 extracted from

  • Roskoski, R.Jr.
    The ErbB/HER receptor protein-tyrosine kinases and cancer (2004), Biochem. Biophys. Res. Commun., 319, 1-11.
    View publication on PubMed
Search for more literature for 2.7.10.1

Application

Application Comment Organism
pharmacology ErbB family receptor kinases are targets for anticancer drugs, e.g. gefitinib or erlotinib in the treatment of non-small lung cancer or colorectal cancer, treatment with therapeutic antibodies in case of breast cancer Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
genes encoding ErbB receptor protein-tyrosine kinase 1-4 are located on different chromosomes Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information null mutations of any of the ErbB family enzymes result in embryonic lethality Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
OSI-774 i.e. erlotinib, inhibits EGF receptor protein tyrosine kinase, binding to EGF receptor kinase, structure overview, anticancer drug Homo sapiens
ZD1839 i.e. gefitinib, reversible inhibition of ErbB1, competitive to ATP, binding to EGF receptor kinase, structure overview, anticancer drug Homo sapiens

Localization

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

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ MgATP- Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + a [protein]-L-tyrosine Homo sapiens regulation mechanisms and ligand binding, ligand binding induces a conformational change, overview ADP + a [protein]-L-tyrosine phosphate
-
 ?
additional information Homo sapiens ErbB family enzymes are absolutely required for viability of embryos ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 several isozymes of both ErbB receptor protein-tyrosine kinase and HER receptor protein-tyrosine kinase
-

Posttranslational Modification

Posttranslational Modification Comment Organism
glycoprotein ErbB family proteins are N-glycosylated to about 20% of their mass, deglycosylation causes loss of 70% protein tyrosine kinase activity Homo sapiens
phosphoprotein phosphorylation at tyrosine residues, autophosphorylation of the ErbB receptor dimer Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
bladder high expression level of ErbB1 receptor Homo sapiens
-
breast high expression level of ErbB1 receptor Homo sapiens
-
kidney high expression level of ErbB1 receptor Homo sapiens
-
non-small cell lung cancer cell high expression level of ErbB1 receptor Homo sapiens
-
prostate cancer cell high expression level of ErbB1 receptor Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + a [protein]-L-tyrosine
-
 Homo sapiens ADP + a [protein]-L-tyrosine phosphate
-
 ?
ATP + a [protein]-L-tyrosine regulation mechanisms and ligand binding, ligand binding induces a conformational change, overview Homo sapiens ADP + a [protein]-L-tyrosine phosphate
-
 ?
additional information ErbB family enzymes are absolutely required for viability of embryos Homo sapiens ?
-
 ?

Subunits

Subunits Comment Organism
dimer dimerization of ErbB receptor results in activation, trans-autophosphorylation, and initiation of signaling occurs Homo sapiens
More the ErbB family enzymes possess a single transmembrane segment, a growth-factor-binding ectodomain, an intracellular protein-tyrosine kinase catalytic domain, and a tyrosine-containing cytoplasmic tail, domain structure overview, enzyme activation involves major rotation of the ectodomain Homo sapiens

Synonyms

Synonyms Comment Organism
EGF receptor protein-tyrosine kinase
-
 Homo sapiens
Egfr
-
 Homo sapiens
epidermal growth factor receptor
-
 Homo sapiens
ErbB receptor protein-tyrosine kinase
-
 Homo sapiens
HER receptor protein-tyrosine kinase
-
 Homo sapiens
More WebB and HER receptor protein-tyrosine kinase, as well as epidermal growth factor receptor belong to the ErbB family, overview Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP MgATP- Homo sapiens