Continuing challenges in targeting oligomeric GPCR-based drugs

Abstract

This chapter will focus on the therapeutic potential of oligomeric GPCR structures. We will discuss the history of these complexes and their connection with treatment. We will highlight several examples from the literature of complexes of therapeutic or theranostic opportunity. As part of this we will discuss different mechanisms that oligomers use to modulate their partner that could be taken advantage of from a drug targeting perspective. We will also discuss the challenges and hurdles to targeting such complexes.

Keywords: Bivalent ligands; G protein-coupled oligomers; GPCR cross-talk; GPCR homomers; Heteromers; Interference peptides.