Multifocal Signal Modulation Therapy by Celecoxib: A Strategy for Managing Castration-Resistant Prostate Cancer

Int J Mol Sci. 2019 Dec 3;20(23):6091. doi: 10.3390/ijms20236091.

Abstract

Background: Prostate cancer (PCa) is a significant health concern throughout the world. Standard therapy for advanced disease consists of anti-androgens, however, almost all prostate tumors become castration resistant (CRPC). Progression from androgen-sensitive PCa to CRPC is promoted by inflammatory signaling through cyclooxygenase-2 (COX-2) expression and ErbB family receptors/AKT activation, compensating androgen receptor inactivity.

Methods: Making use of CRPC cell lines, we investigated the effects of the anti-inflammatory drug celecoxib. Biochemical data obtained using immunoblotting, enzyme-linked immunosorbent assay (ELISA), invasion, and xenografts were further integrated by bioinformatic analyses.

Results: Celecoxib reduced cell growth and induced apoptosis through AKT blockade, cleavage of poly (ADP-ribose) polymerase-1 (PARP-1), and proteasomal degradation of the anti-apoptotic protein Mcl-1. Epidermal growth factor receptor (EGFR), ErbB2, and ErbB3 degradation, and heterogeneous nuclear ribonucleoprotein K (hnRNP K) downregulation, further amplified the inhibition of androgen signaling. Celecoxib reduced the invasive phenotype of CRPC cells by modulating NF-κB activity and reduced tumor growth in mice xenografts when administered in association with the anti-EGFR receptor antibody cetuximab. Bioinformatic analyses on human prostate cancer datasets support the relevance of these pathways in PCa progression.

Conclusions: Signaling nodes at the intersection of pathways implicated in PCa progression are simultaneously modulated by celecoxib treatment. In combination therapies with cetuximab, celecoxib could represent a novel therapeutic strategy to curb signal transduction during CRPC progression.

Keywords: ErbB family; apoptosis; castration-resistant prostate cancer; celecoxib; inflammation; signaling.

MeSH terms

  • Amphiregulin / metabolism
  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Apoptosis / drug effects
  • Apoptosis / genetics
  • Celecoxib / pharmacology
  • Celecoxib / therapeutic use*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Proliferation / genetics
  • Cetuximab / pharmacology
  • Cetuximab / therapeutic use
  • Down-Regulation / drug effects
  • Drug Resistance, Neoplasm / drug effects
  • Epidermal Growth Factor / metabolism
  • Gene Expression Regulation, Neoplastic / drug effects
  • Heterogeneous-Nuclear Ribonucleoprotein K / metabolism
  • Humans
  • Male
  • Mice, SCID
  • NF-kappa B / metabolism
  • Neoplasm Invasiveness
  • Phosphorylation / drug effects
  • Prostatic Neoplasms, Castration-Resistant / drug therapy*
  • Prostatic Neoplasms, Castration-Resistant / genetics
  • Prostatic Neoplasms, Castration-Resistant / pathology
  • Proto-Oncogene Proteins c-akt / metabolism
  • Receptor, ErbB-2 / metabolism
  • Receptors, Androgen / metabolism
  • Signal Transduction* / drug effects
  • Xenograft Model Antitumor Assays
  • p38 Mitogen-Activated Protein Kinases / metabolism

Substances

  • AR protein, human
  • Amphiregulin
  • Heterogeneous-Nuclear Ribonucleoprotein K
  • NF-kappa B
  • Receptors, Androgen
  • Epidermal Growth Factor
  • ERBB2 protein, human
  • Receptor, ErbB-2
  • Proto-Oncogene Proteins c-akt
  • p38 Mitogen-Activated Protein Kinases
  • Celecoxib
  • Cetuximab