- Protein Name
- Mast/stem cell growth factor receptor Kit
- Gene Name
- KIT
- Organism
-
Homo sapiens
- Function
- 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.
| Site |
Maximum Consensus Site Population |
Minimum Consensus Site Population |
Median Consensus Site Population |
| MPP |
28 |
5 |
15.0 |
| DFG |
17 |
5 |
12.0 |
| PIF |
6 |
2 |
3.0 |
| DRS |
2 |
2 |
2.0 |
| MT3 |
15 |
2 |
13.0 |
| CMP |
8 |
8 |
8.0 |
| PDIG |
2 |
2 |
2.0 |
| ATP |
28 |
1 |
12.0 |
| PDB ID |
Maximum Consensus Site Population |
| MPP site |
DFG site |
PIF site |
DRS site |
DEF site |
EDI site |
MT3 site |
AAS site |
LBP site |
CMP site |
PDIG site |
ATP site |
PMP site |
| Total Druggable Structures per Site |
5 |
1 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
4 |
0 |
|
AFP10721
|
21 |
17 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
|
3G0E
|
15 |
0 |
0 |
0 |
0 |
0 |
15 |
0 |
0 |
0 |
0 |
8 |
0 |
|
3G0F
|
20 |
13 |
0 |
2 |
0 |
0 |
0 |
0 |
0 |
0 |
2 |
23 |
0 |
|
1T46
|
28 |
0 |
0 |
0 |
0 |
0 |
5 |
0 |
0 |
0 |
0 |
21 |
0 |
|
4U0I
|
16 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
17 |
0 |
|
4HVS
|
15 |
12 |
0 |
0 |
0 |
0 |
13 |
0 |
0 |
8 |
0 |
9 |
0 |
|
1T45
|
11 |
0 |
3 |
0 |
0 |
0 |
15 |
0 |
0 |
0 |
0 |
12 |
0 |
|
1PKG
|
21 |
5 |
6 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
28 |
0 |