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Literature summary extracted from

  • Roskoski, R.Jr.
    Structure and regulation of Kit protein-tyrosine kinase - the stem cell factor receptor (2005), Biochem. Biophys. Res. Commun., 338, 1307-1315.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.10.1 additional information activation mechanism, overview Homo sapiens
2.7.10.1 stem cell factor soluble and membrane-bound glycoprotein, activating ligand of the stem cell receptor i.e. the Kit protein-tyrosine kinase, stem cell factor ligand binding induces receptor dimerization and tyrosine kinase activation Homo sapiens

Application

EC Number Application Comment Organism
2.7.10.1 pharmacology the enzyme is a target for anticancer drugs, such as STI-571 Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.7.10.1 additional information gain-of-function mutations of Kit receptor are associated with several neoplasms including acute myelogenous leukemia, gastrointestinal stromal tumors, mastocytomas, and nasal T-cell lymphomas, mutations and associated tumor types, overview Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.10.1 additional information enzyme inhibition by the juxtamembrane domain in cis by maintaining the control alphaC-helix and the activation loop in their active conformations, the juxtamembrane also inhibits receptor dimerization Homo sapiens
2.7.10.1 STI-571 specific protein-tyrosine kinase inhibitor binds to an inactive Kit receptor form, utilized in tumor treatment, binding structure Homo sapiens

Localization

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

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.10.1 Mg2+ as MgATP2- 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 stem cell factor and Kit receptor are essential playing important roles in e.g. gametogenesis, hematopoiesis, mast cell development and function, and melanogenesis, complete absence is lethal, enzyme deficiencies lead to defects in white and red blood cell production, to hypopigmentation, and to sterility, Kit receptor signaling regulation by autophosphorylation and dephosphorylation via a phosphatase, regulation mechanism, overview ADP + a [protein]-L-tyrosine phosphate
-
 ?

Organism

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

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
2.7.10.1 phosphoprotein tyrosine autophosphorylation of the Kit receptor activated by stem cell factor ligand binding and subsequent dimerization, Kit receptor signaling regulation by autophosphorylation and dephosphorylation via a phosphatase Homo sapiens

Reaction

EC Number Reaction Comment Organism Reaction ID
2.7.10.1 ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate active site structure, activation mechanism Homo sapiens
a

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.10.1 embryo
-
 Homo sapiens
-
2.7.10.1 embryonic stem cell
-
 Homo sapiens
-

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 stem cell factor and Kit receptor are essential playing important roles in e.g. gametogenesis, hematopoiesis, mast cell development and function, and melanogenesis, complete absence is lethal, enzyme deficiencies lead to defects in white and red blood cell production, to hypopigmentation, and to sterility, Kit receptor signaling regulation by autophosphorylation and dephosphorylation via a phosphatase, regulation mechanism, overview Homo sapiens ADP + a [protein]-L-tyrosine phosphate
-
 ?

Subunits

EC Number Subunits Comment Organism
2.7.10.1 dimer activated Kit receptor Homo sapiens
2.7.10.1 More the Kit receptor consists of an extracellular domain, a transmembrane segment, a juxtamembrane segment, and a protein kinase domain with an insert of about 80 amino acid residues, structure-function analysis, stem cell factor ligand binding induces receptor dimerization and tyrosine kinase activation Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
2.7.10.1 KIT
-
 Homo sapiens
2.7.10.1 Kit protein-tyrosine kinase
-
 Homo sapiens
2.7.10.1 stem cell receptor
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.10.1 ATP as MgATP2-, binding structure of ATP and product ADP Homo sapiens