Tclin KIT Mast/stem cell growth factor receptor Kit

Protein Summary

Description

Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell maintenance, gametogenesis, mast cell development, migration and function, and in melanogenesis. In response to KITLG/SCF binding, KIT can activate several signaling pathways. Phosphorylates PIK3R1, PLCG1, SH2B2/APS and CBL. Activates the AKT1 signaling pathway by phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase. Activated KIT also transmits signals via GRB2 and activation of RAS, RAF1 and the MAP kinases MAPK1/ERK2 and/or MAPK3/ERK1. Promotes activation of STAT family members STAT1, STAT3, STAT5A and STAT5B. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. KIT signaling is modulated by protein phosphatases, and by rapid internalization and degradation of the receptor. Activated KIT promotes phosphorylation of the protein phosphatases PTPN6/SHP-1 and PTPRU, and of the transcription factors STAT1, STAT3, STAT5A and STAT5B. Promotes phosphorylation of PIK3R1, CBL, CRK (isoform Crk-II), LYN, MAPK1/ERK2 and/or MAPK3/ERK1, PLCG1, SRC and SHC1. This gene encodes the human homolog of the proto-oncogene c-kit. C-kit was first identified as the cellular homolog of the feline sarcoma viral oncogene v-kit. This protein is a type 3 transmembrane receptor for MGF (mast cell growth factor, also known as stem cell factor). Mutations in this gene are associated with gastrointestinal stromal tumors, mast cell disease, acute myelogenous lukemia, and piebaldism. Multiple transcript variants encoding different isoforms have been found for this gene. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• P10721
• B5A956
• D5LXN2
• D5M931
• F5H8F8
• Q6IQ28
• Q99662
• Q9UM99
• SCFR

Gene Name

• KIT

Ensembl ID

• ENST00000288135
• ENSP00000288135
• ENSG00000157404
• ENST00000412167
• ENSP00000390987

Symbol

• SCFR
• PBT
• SCFR
• C-Kit
• CD117
• MASTC

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological process	1
molecular function	1
protein domain	1
PubMedID	1
hub protein	0.99

Protein Classes

DTO Classes

Protein / Kinase / Protein Kinase / Tk Group / Pdgfr Family / Mast/stem Cell Growth Factor Receptor Kit

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 10443.08   (req: < 5)

Gene RIFs: 1002   (req: <= 3)

Antibodies: 4953   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 10443.08   (req: >= 5)

Gene RIFs: 1002   (req: > 3)

Antibodies: 4953   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 88

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 509

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 17