Targeting G protein coupled receptor-related pathways as emerging molecular therapies

Abstract

G protein coupled receptors (GPCRs) represent the most important targets in modern pharmacology because of the different functions they mediate, especially within brain and peripheral nervous system, and also because of their functional and stereochemical properties. In this paper, we illustrate, via a variety of examples, novel advances about the GPCR-related molecules that have been shown to play diverse roles in GPCR pathways and in pathophysiological phenomena. We have exemplified how those GPCRs' pathways are, or might constitute, potential targets for different drugs either to stimulate, modify, regulate or inhibit the cellular mechanisms that are hypothesized to govern some pathologic, physiologic, biologic and cellular or molecular aspects both in vivo and in vitro. Therefore, influencing such pathways will, undoubtedly, lead to different therapeutical applications based on the related pharmacological implications. Furthermore, such new properties can be applied in different fields. In addition to offering fruitful directions for future researches, we hope the reviewed data, together with the elements found within the cited references, will inspire clinicians and researchers devoted to the studies on GPCR's properties.

Keywords: G protein coupled receptors; Molecular therapy; Potential target; Signaling pathway.

Figure 1

Signaling of biased ligands which have the ability to stimulate specifically either G protein (A) or β-arrestin (B) functions via the selectivity they have at the receptor level and the therapeutic implications it might have. (The biased ligands binding will stimulate either β-arrestin activation or G protein activation).