Q13153

Background

Protein Name
Serine/threonine-protein kinase PAK 1
Gene Name
PAK1
Organism
Homo sapiens

Annotations

Function
Protein kinase involved in intracellular signaling pathways downstream of integrins and receptor-type kinases that plays an important role in cytoskeleton dynamics, in cell adhesion, migration, proliferation, apoptosis, mitosis, and in vesicle-mediated transport processes. Can directly phosphorylate BAD and protects cells against apoptosis. Activated by interaction with CDC42 and RAC1. Functions as GTPase effector that links the Rho-related GTPases CDC42 and RAC1 to the JNK MAP kinase pathway. Phosphorylates and activates MAP2K1, and thereby mediates activation of downstream MAP kinases. Involved in the reorganization of the actin cytoskeleton, actin stress fibers and of focal adhesion complexes. Phosphorylates the tubulin chaperone TBCB and thereby plays a role in the regulation of microtubule biogenesis and organization of the tubulin cytoskeleton. Plays a role in the regulation of insulin secretion in response to elevated glucose levels. Part of a ternary complex that contains PAK1, DVL1 and MUSK that is important for MUSK-dependent regulation of AChR clustering during the formation of the neuromuscular junction (NMJ). Activity is inhibited in cells undergoing apoptosis, potentially due to binding of CDC2L1 and CDC2L2. Phosphorylates MYL9/MLC2. Phosphorylates RAF1 at 'Ser-338' and 'Ser-339' resulting in: activation of RAF1, stimulation of RAF1 translocation to mitochondria, phosphorylation of BAD by RAF1, and RAF1 binding to BCL2. Phosphorylates SNAI1 at 'Ser-246' promoting its transcriptional repressor activity by increasing its accumulation in the nucleus. In podocytes, promotes NR3C2 nuclear localization. Required for atypical chemokine receptor ACKR2-induced phosphorylation of LIMK1 and cofilin (CFL1) and for the up-regulation of ACKR2 from endosomal compartment to cell membrane, increasing its efficiency in chemokine uptake and degradation. In synapses, seems to mediate the regulation of F-actin cluster formation performed by SHANK3, maybe through CFL1 phosphorylation and inactivation. Plays a role in RUFY3-mediated facilitating gastric cancer cells migration and invasion (PubMed:25766321).

Mapping Statistics

Site
Maximum Consensus Site Population
Minimum Consensus Site Population
Median Consensus Site Population
EDI 7 4 5.5
MT3 24 2 15.0
PIF 23 6 16.5
ATP 23 3 9.0
DEF 4 4 4.0
DRS 22 21 21.0
AAS 5 4 4.5
MPP 19 2 5.0
DFG 13 1 4.0
LBP 2 2 2.0
CMP 19 10 16.0
PDIG 20 2 14.0

Mapping Results

PDB ID
Maximum Consensus Site Population
EDI site
MT3 site
PIF site
ATP site
DEF site
DRS site
AAS site
MPP site
DFG site
LBP site
CMP site
PDIG site
PMP site
Total Druggable Structures per Site 0 6 4 5 0 3 0 2 0 0 12 9 0
1F3M 0 19 0 13 0 0 5 5 2 0 0 12 0
1YHV 0 15 0 14 0 0 0 3 7 2 17 14 0
1YHW 0 0 0 16 0 0 0 2 9 0 15 19 0
2HY8 0 0 0 9 0 0 0 18 4 0 14 20 0
3FXZ 0 9 0 6 0 0 0 0 6 0 16 16 0
3FY0 0 0 0 9 0 0 0 4 7 0 14 18 0
3Q4Z 7 4 19 10 0 0 4 19 3 0 11 10 0
3Q52 0 2 0 8 0 0 0 3 5 0 15 15 0
3Q53 0 24 0 7 0 0 0 11 2 0 12 17 0
4DAW 0 0 0 7 0 0 0 5 13 0 16 14 0
4EQC 0 11 0 15 0 0 0 0 0 0 19 13 0
4O0R 0 0 0 13 0 0 0 6 10 0 18 11 0
4O0T 0 21 0 16 0 0 0 11 3 0 16 14 0
4P90 0 13 23 23 0 0 0 0 10 0 17 16 0
4ZJI 0 16 0 3 0 0 0 7 0 0 16 18 0
4ZJJ 0 16 7 0 0 0 0 0 0 0 16 18 0
4ZLO 4 14 16 4 0 0 0 3 0 0 0 4 0
4ZY4 0 0 0 15 4 0 0 0 3 0 16 10 0
4ZY5 0 0 17 13 0 21 0 0 4 0 15 5 0
4ZY6 0 0 0 4 0 22 0 4 4 0 15 6 0
5DEY 0 21 0 20 0 21 0 0 0 0 19 14 0
5DFP 0 0 0 11 0 0 0 6 0 0 16 13 0
5IME 0 0 0 17 0 0 0 0 0 0 15 17 0
AFQ13153 0 0 0 0 0 0 0 0 0 0 0 15 0