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

BRENDA support

Literature summary for 2.7.10.1 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
Search for more literature for 2.7.10.1

Activating Compound

Activating Compound Comment Organism Structure
additional information activation mechanism, overview Homo sapiens
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

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

Protein Variants

Protein Variants Comment Organism
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

Inhibitors Comment Organism Structure
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
STI-571 specific protein-tyrosine kinase inhibitor binds to an inactive Kit receptor form, utilized in tumor treatment, binding structure Homo sapiens

Localization

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

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ as MgATP2- 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 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

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
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

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

Source Tissue

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

Subunits Comment Organism
dimer activated Kit receptor Homo sapiens
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

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

Cofactor

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