The delivery of therapeutic drugs to the brain remains a major pharmacology challenge. A complex system of chemical surveillance to protect the brain from endogenous and exogenous toxicants at brain barriers hinders the uptake of many compounds with significant in vitro and ex vivo therapeutic properties. Despite the advances in the field in recent years, the components of this system are not completely understood. Recently, a large group of chemo-sensing receptors, have been identified in the blood-cerebrospinal fluid barrier. Among these chemo-sensing receptors, bitter taste receptors (TAS2R) hold promise as potential drug targets, as many TAS2R bind compounds with recognized neuroprotective activity (quercetin, resveratrol, among others). Whether activation of TAS2R by their ligands contributes to their diverse biological actions described in other cells and tissues is still debatable. In this review, we discuss the potential role of TAS2R gene family as the mediators of the biological activity of their ligands for the treatment of central nervous system disorders and discuss their potential to counteract drug resistance by improving drug delivery to the brain.
Keywords: ABC transporters; Bitter taste receptors; Bitter tasting compounds; Brain barriers; Pharmaco-resistance.
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