The Role of Bitter Taste Receptors in Cancer: A Systematic Review

Abstract

Background: Since it is known that bitter taste receptors (TAS2Rs) are expressed and functionally active in various extra-oral cells, their genetic variability and functional response initiated by their activation have become of broader interest, including in the context of cancer.

Methods: A systematic research was performed in PubMed and Google Scholar to identify relevant publications concerning the role of TAS2Rs in cancer.

Results: While the findings on variations of TAS2R genotypes and phenotypes and their association to the risk of developing cancer are still inconclusive, gene expression analyses revealed that TAS2Rs are expressed and some of them are predominately downregulated in cancerous compared to non-cancerous cell lines and tissue samples. Additionally, receptor-specific, agonist-mediated activation induced various anti-cancer effects, such as decreased cell proliferation, migration, and invasion, as well as increased apoptosis. Furthermore, the overexpression of TAS2Rs resulted in a decreased tumour incidence in an in vivo study and TAS2R activation could even enhance the therapeutic effect of chemotherapeutics in vitro. Finally, higher expression levels of TAS2Rs in primary cancerous cells and tissues were associated with an improved prognosis in humans.

Conclusion: Since current evidence demonstrates a functional role of TAS2Rs in carcinogenesis, further studies should exploit their potential as (co-)targets of chemotherapeutics.

Keywords: TAS2Rs; bitter taste; bitter taste receptors; cancer risk; carcinogenesis; genetic variability.

Figure 1

This figure is adapted from Hanahan and Weinberg, 2011 [54] and highlights how agonist-mediated activation of TAS2Rs and/or by overexpression of TAS2Rs can counteract the diverse capabilities of cancerous cells and tissues, known as hallmarks of cancer. ↑: promoting effect; ↓: inhibitory effect.