Figure 5. EREG/EGFR increases pain through a PI3K/AKT→mTOR→4E-BP1→eIF4F complex→MMP-9 signaling pathway.
(A) The signaling pathway investigated, with major proteins indicated in black and blocking drugs or mutants shown in red. (B) Treatment with wortmannin (5 μg, i.t.) blocks EREG‑induced increases in late-phase formalin-induced pain behavior (drug × drug: F1,23 = 4.7, P = 0.04). (C) Low doses of rapamycin (5 mg/kg) and CCI 779 (1 mg/kg) block EREG effects without affecting formalin-induced pain per se (rapamycin, drug × drug: F1,27 = 3.6, P = 0.04; CCI 779 drug × drug: F1,28 = 4.2, P = 0.03); higher doses (10 mg/kg) are analgesic (main effects: rapamycin, F1,28 = 22.9, P < 0.001; CCI 779, F1,28 = 30.2, P < 0.001). (D) No effect on EREG increases in formalin-induced pain behavior in SGK1/2 (Rps6kb1/Rps6kb2) double-null mutant mice (Rps6kb1/2–/–; main effect of drug: F1,18 = 25.8, P < 0.001). (E) Lack of EREG effects in 4E-BP1 (Eif4ebp1–/–) null mutant mice (genotype × drug: F1,33 = 7.1, P = 0.01). (F) Treatment with 4EGI-1 (25 μg, i.t.) blocks EREG effects (drug × drug: F1,20 = 7.6, P = 0.01). (G) Treatment with TIMP-1 (4 pmol, i.t.) blocks EREG effects (drug × drug: F1,30 = 5.6, P = 0.02). (H) Lack of EREG effects in MMP-9 null mutants (Mmp9–/–; genotype × drug: F1,20 = 16.1, P = 0.001). In all experiments, EREG was injected at 10 ng i.t. Bars in all graphs represent mean ± SEM for percentage of samples featuring licking/biting behavior; n = 6–8/drug/dose and n = 6–12/drug/genotype (dependent on breeding success). Two-way ANOVA for all panels followed by t test compared with EREG vehicle. *P < 0.05; **P < 0.01; ***P < 0.001, compared with wortmannin, rapamycin, CCI 779, 4EGI-1, or TIMP-1 vehicle, or +/+ genotype. #P < 0.05; ##P < 0.01; ###P < 0.001, compared with rapamycin/CCI 779 vehicle. †P < 0.05 compared with vehicle/vehicle group.