Background: Pancreatic cancer (PC) requires new therapeutic strategies. We identified that inhibition of βIII-tubulin (shRNA) in PC cells decreased tumour growth and metastases in mice [1]. However, since there are no inhibitors of βIII-tubulin, we developed a nanoparticle to deliver βIII-tubulin siRNA to mouse pancreatic tumours [2].
Aims: (1) To assess the effect of therapeutic inhibition of βIII-tubulin using nanoparticle-siRNA on pancreatic tumour growth in mice. (2) To investigate the pro-apoptotic pathways controlled by βIII-tubulin in PC cells.
Methods: In vivo: Mice with orthotopic MiaPaCa-2 tumours (n=10/group) were treated (5-weeks post-implantation) with nanoparticle+βIII-tubulin-siRNA or control-siRNA for 3.5-weeks. Tumour volume was measured and cleaved caspase-8 assessed in tumours. In vitro: PC cells (MiaPaCa-2, PANC1) were treated ±βIII-tubulin-siRNA ±caspase-8 or 9 inhibitors and caspase-8/9 activities and apoptosis measured. Sensitivity to extrinsic-apoptosis inducers (TRAIL, TNFα, FasL) were tested (proliferation, apoptosis).
Results: Nanoparticle+βIII-tubulin-siRNA reduced PC tumour growth (103±17.5mm3; p<0.05) versus controls (194.9±31.2mm3). Silencing βIII-tubulin in PC cells significantly increased the activity of caspase-8 (MiaPaCa-2: 53±13% increase vs control, *p<0.05) and caspase-9 (45±9% increase vs control, *p<0.01). However, βIII-tubulin knockdown-induced apoptosis was only blocked by inhibiting caspase-8. Furthermore, knockdown of βIII-tubulin combined with TRAIL, TNFα or FasL increased apoptosis, and reduced cell proliferation. Inhibition of βIII-tubulin in vivo also increased caspase-8 cleavage in PC tumours.
Conclusions: Nanomedicine/siRNA inhibition of βIII-tubulin represents a potential new class of PC therapeutics. Our novel results demonstrated βIII-tubulin-siRNA in PC cells activates extrinsic-apoptosis and sensitises to inducers of extrinsic-apoptosis. βIII-tubulin inhibition thus represents a three-pronged attack on PC cells by changing the way cells respond to (1) a chemotherapeutic (TRAIL), (2) immune cytokines (FasL and TNFα) and (3) pancreatic stellate cell secretions (TNFα).
References:
[1] McCarroll, J.A., et al. Oncotarget, 2015. 6(4): p. 2235-49.
[2] Teo, J., et al. Biomacromolecules, 2016. 17(7): p. 2337-51.