Q07912

Background

Protein Name
Activated CDC42 kinase 1
Gene Name
TNK2
Organism
Homo sapiens

Annotations

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.

Mapping Statistics

Site Maximum Consensus Site Population Minimum Consensus Site Population Median Consensus Site Population
MPP 28 2 18.0
AAS 19 8 14.0
MT3 16 3 9.0
ATP 23 2 16.0
DEF 3 3 3.0
DFG 16 6 10.0
DRS 16 4 12.0
PIF 15 13 14.0

Mapping Results

PDB ID Maximum Consensus Site Population
MPP site AAS site MT3 site LBP site ATP site DEF site DFG site CMP site PMP site EDI site DRS site PDIG site PIF site
Total Druggable Structures per Site 10 3 1 0 8 0 1 0 0 0 1 0 0
3EQP 23 16 0 0 18 3 0 0 0 0 0 0 15
4ID7 16 19 15 0 17 0 0 0 0 0 0 0 14
3EQR 18 18 9 0 22 0 12 0 0 0 0 0 0
1U54 26 0 0 0 20 0 8 0 0 0 0 0 0
1U46 28 15 0 0 23 0 9 0 0 0 16 0 0
4EWH 26 9 0 0 17 0 15 0 0 0 0 0 0
4HZR 20 13 0 0 17 0 9 0 0 0 0 0 0
1U4D 20 14 0 0 20 0 16 0 0 0 12 0 0
4HZS 17 0 16 0 13 0 0 0 0 0 4 0 0
AFQ07912 20 0 0 0 0 0 15 0 0 0 0 0 0