Search results for KIT

Showing 21 results out of 367

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Types

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Protein (3 results from a total of 114)

KIT

Identifier: R-HSA-197662
Species: Homo sapiens
Compartment: plasma membrane
Primary external reference: UniProt: KIT: P10721
Identifier: R-HSA-9669587
Species: Homo sapiens
Compartment: plasma membrane
Primary external reference: UniProt: KIT: P10721
Identifier: R-HSA-205207
Species: Homo sapiens
Compartment: plasma membrane
Primary external reference: UniProt: KIT: P10721

Reaction (3 results from a total of 82)

Identifier: R-HSA-205289
Species: Homo sapiens
Compartment: plasma membrane, cytosol, extracellular region
The cytoplasmic domain of KIT contains a bipartite kinase domain separated by 77 residues. The first part of the catalytic domain contains the ATP binding region while the second part contains an activation loop. Both parts of the domain have a number of possible autophosphorylation sites. In contrast to many other tyrosine kinases, autophosphorylation of the activation loop does not seem to be involved in the activation of the kinase activity nor it is required for full kinase activity (DiNitto et al. 2010). Instead, phosphorylation sites in the juxtamembrane region are important for activation of the kinase activity. The dimerized KIT acts as both enzyme and substrate for itself and autophosphorylates these specific tyrosine residues with in the kinases domains in trans as well as tyrosine residues outside the kinase domain. The resulting phosphotyrosine residues serve as docking sites for a number of signal transduction molecules containing Src-homology 2 (SH2) and phosphotyrosine-binding (PTB) domains. A majority of the autophosphorylation sites reside outside the kinase domain.
Identifier: R-HSA-205306
Species: Homo sapiens
Compartment: plasma membrane, extracellular region, cytosol
The protein tyrosine phosphatase SHP-1 negatively regulates KIT signaling through binding to phosphorylated Y570. It is unclear whether SHP1 directly dephosphorylates KIT or elicits dephosphorylation of the receptor indirectly by dephosphorylating and inhibiting cytosolic PTKs that act on KIT. SHP-1 may also compete with and displace SFKs or other proteins that dock to phosphorylated Y570 (Kozlowski et al, 1998).
Identifier: R-HSA-9670414
Species: Homo sapiens
Compartment: plasma membrane, cytosol
Signaling downstream of KIT mutants occurs in part through SRC family kinases, as is the case for the wild-type receptor (Paronetto et al, 2004; Krystal et al, 1998; Schittenhelm et al, 2006; Tatton et al, 2003; Timokhina et al, 1998; reviewed in Lanneartsson and Roonstrand, 2012). The dependence of different KIT mutants on SRC family signaling varies, however, with mutants such as the common D816V showing less requirement for SFK-mediated signaling (Sun et al, 2009).

DNA Sequence (1 results from a total of 1)

Identifier: R-HSA-8864691
Species: Homo sapiens
Compartment: nucleoplasm
Primary external reference: ENSEMBL: ENSG00000157404

Pathway (3 results from a total of 23)

Identifier: R-HSA-9669938
Species: Homo sapiens
KIT signaling is important in several processes including stem cell maintenance, erythropoiesis, mast cell development, lymphopoiesis, melanogenesis and maintenance of interstitial cell of Cajal (Hirota et al, 1998; Chi et al, 2010). Gain-of-function mutations in KIT have been identified at low frequency in a number of diseases, including AML, melanoma and mast and germ cell tumors, and at higher frequency in gastrointesinal stromal tumors (reviewed in Lennartsson and Roonstrand, 2012; Abbaspour Babaei et al, 2016; Roskoski, 2018).
Identifier: R-HSA-1433559
Species: Homo sapiens
SCF induced proliferation is negatively regulated by various proteins including SHP1, PKC, CBL, SOCS1, SOCS6 and LNK.
Identifier: R-HSA-9669914
Species: Homo sapiens
Dasatinib is a type II tyrosine kinase inhibitor that is active against KIT receptors with mutations in the juxtamembrane and activation loop domains, but shows only partial activity against KIT receptors with mutations at residue V654 (Schittenhelm et al, 2006; Serrano et al, 2019).

Set (3 results from a total of 39)

Identifier: R-HSA-9671494
Species: Homo sapiens
Compartment: plasma membrane
Identifier: R-HSA-9680195
Species: Homo sapiens
Compartment: plasma membrane
Identifier: R-HSA-9669738
Species: Homo sapiens
Compartment: plasma membrane

Complex (3 results from a total of 103)

Identifier: R-HSA-9670384
Species: Homo sapiens
Compartment: plasma membrane
Identifier: R-HSA-9670380
Species: Homo sapiens
Compartment: plasma membrane
Identifier: R-HSA-9670368
Species: Homo sapiens
Compartment: plasma membrane

Interactor (1 results from a total of 1)

Identifier: P21583
Species: Homo sapiens
Primary external reference: UniProt: KITLG: P21583

ChemicalDrug (3 results from a total of 3)

Identifier: R-ALL-2077524
Compartment: cytosol
Masitinib is a multi-kinase inhibitor that targets mutant and wild-type FGFR3, PDGFR and c-KIT (Dubreuil, 2009). It is currently in Phase II clinical trials for multiple myeloma (NCT00866138).
Identifier: R-ALL-2023377
Compartment: cytosol
A broad specificity ATP-competitive inhibitor of FGF-, VEGF-, PDGF- and KIT receptors that is in Phase I and II clinical trials for treatment of gastric, breast and endometrial cancers.
Identifier: R-ALL-1839035
Compartment: cytosol
A Novartis tyrosine kinase inhibitor with activity against multiple tyrosine kinase receptors including FGFRs, VEGFRs, PDGFRs, KIT, FLT3 and CSFR. TKI258 is in Phase II clinical trials for advanced breast cancer in patients with and without FGFR1 amplification (NCT00958971), for endometrial cancer with WT or activated FGFR2 mutants (NCT01379534), for relapsed myeloma with and without the t4:14 FGFR3 translocation/amplification (NCT01058434), and in bladder cancer in cases where archived material is available to check for correlation with FGFR3 mutation status (NCT00790426).

Icon (1 results from a total of 1)

KIT

Species: Homo sapiens
Curator: Karen Rothfels
Designer: Cristoffer Sevilla
KIT icon
Mast/stem cell growth factor receptor Kit
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