- Protein Name
- Activated CDC42 kinase 1
- Gene Name
- TNK2
- Organism
-
Homo sapiens
- Function
- Non-receptor tyrosine-protein and serine/threonine-protein kinase that is implicated in cell spreading and migration, cell survival, cell growth and proliferation. Transduces extracellular signals to cytosolic and nuclear effectors. Phosphorylates AKT1, AR, MCF2, WASL and WWOX. Implicated in trafficking and clathrin-mediated endocytosis through binding to epidermal growth factor receptor (EGFR) and clathrin. Binds to both poly- and mono-ubiquitin and regulates ligand-induced degradation of EGFR, thereby contributing to the accumulation of EGFR at the limiting membrane of early endosomes. Downstream effector of CDC42 which mediates CDC42-dependent cell migration via phosphorylation of BCAR1. May be involved both in adult synaptic function and plasticity and in brain development. Activates AKT1 by phosphorylating it on 'Tyr-176'. Phosphorylates AR on 'Tyr-267' and 'Tyr-363' thereby promoting its recruitment to androgen-responsive enhancers (AREs). Phosphorylates WWOX on 'Tyr-287'. Phosphorylates MCF2, thereby enhancing its activity as a guanine nucleotide exchange factor (GEF) toward Rho family proteins. Contributes to the control of AXL receptor levels. Confers metastatic properties on cancer cells and promotes tumor growth by negatively regulating tumor suppressor such as WWOX and positively regulating pro-survival factors such as AKT1 and AR.
| Site |
Maximum Consensus Site Population |
Minimum Consensus Site Population |
Median Consensus Site Population |
| MPP |
28 |
2 |
18.0 |
| DFG |
16 |
6 |
10.0 |
| PIF |
15 |
13 |
14.0 |
| DRS |
16 |
4 |
12.0 |
| DEF |
3 |
3 |
3.0 |
| MT3 |
16 |
3 |
9.0 |
| AAS |
19 |
8 |
14.0 |
| ATP |
23 |
2 |
16.0 |
| 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 |
10 |
1 |
0 |
1 |
0 |
0 |
1 |
3 |
0 |
0 |
0 |
8 |
0 |
|
1U46
|
28 |
9 |
0 |
16 |
0 |
0 |
0 |
15 |
0 |
0 |
0 |
23 |
0 |
|
4HZS
|
17 |
0 |
0 |
4 |
0 |
0 |
16 |
0 |
0 |
0 |
0 |
13 |
0 |
|
4HZR
|
20 |
9 |
0 |
0 |
0 |
0 |
0 |
13 |
0 |
0 |
0 |
17 |
0 |
|
1U54
|
26 |
8 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
20 |
0 |
|
1U4D
|
20 |
16 |
0 |
12 |
0 |
0 |
0 |
14 |
0 |
0 |
0 |
20 |
0 |
|
AFQ07912
|
20 |
15 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
|
3EQR
|
18 |
12 |
0 |
0 |
0 |
0 |
9 |
18 |
0 |
0 |
0 |
22 |
0 |
|
4ID7
|
16 |
0 |
14 |
0 |
0 |
0 |
15 |
19 |
0 |
0 |
0 |
17 |
0 |
|
4EWH
|
26 |
15 |
0 |
0 |
0 |
0 |
0 |
9 |
0 |
0 |
0 |
17 |
0 |
|
3EQP
|
23 |
0 |
15 |
0 |
3 |
0 |
0 |
16 |
0 |
0 |
0 |
18 |
0 |