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. 2018 Apr 19;315(2):G302–G317. doi: 10.1152/ajpgi.00005.2018

Table 1.

S474 PAK4 kinase phosphorylation: characteristics and interactions of PAK4 in rat pancreatic acini

Variable pS474 PAK4 Phosphorylation Concentrations and Incubation Times Reported In:
Stimulation by pancreatic secretagogues Fig. 2
    Yes Endothelin-1, CCK-8, carbachol, bombesin
Stimulation by pancreatic growth factors Fig. 2
    Yes Insulin, IGF-1, HGF, EGF, bFGF, PDGF
Stimulation by post-receptor activators Fig. 5
    Yes TPA, thapsigargin, A23187
Potency/Time course Fig. 3
EC50 of CCK-8 (nM) 0.052 ± 0.003 Fig. 3
EC50 of CCK-JMV (nM) 0.10 ± 0.01 Fig. 3
Inhibition of CCK-8-stimulated PAK4 activation
    Inhibition of 0.3 nM CCK-8 Fig. 7
        Yes p38 Inhibitor (SB202190), SFK inhibitor (PP2)
        No p44/42 inhibitor (PD98059)
    Inhibition of 1 nM CCK-8 Figs. 57
        Yes PKD inhibitor (CRT0066101, kbNB142–70), PKC (GFX109203)
        No PI3K inhibitor (wortmannin, LY294002), Ca2+ (Thapsigargin)
    Inhibition of 100 nM CCK-8 Fig. 7
        Yes p44/42 Inhibitor (PD98059)
        No p38 Inhibitor (SB202190), SFK Inhibitor (PP2)
    Inhibition by PF-3758309 Fig. 8
        PAK4 From 0.1 nM (IC50: 1.89 ± 0.02 nM)
        PAK2 Requires high doses (i.e., ≥1 µM of PF-37580309)
    Inhibition by LCH-7749944 Fig. 9
        PAK4 90% decrease at 3 s incubation with 30 µM LCH-7749944
        PAK2 No inhibition under these conditions

Results are calculated from data shown in Figs. 2, 3, 59. bFGF, basic fibroblast growth factor; CCK, cholecystokinin; EGF, epidermal growth factor; HGF, hepatocyte growth factor; IGF-1, insulin-like growth factor 1; PAK, p21-activated kinase; PDGF, platelet-derived growth factor; SFK, Src family of kinases.