Paweł Kozielewicz, Konrad Owczarek, Joanna J. Sajkowska‑Kozielewicz

Class F GPCR – activation mechanism and pharmacology
2019-08-31

In the review, we characterize G protein-coupled receptors (GPCRs). These proteins are targeted by approximately 35% of currently marketed drugs. Here, we focus on Class F receptors (Frizzleds, FZDs). First, we describe the ternary complex model that defines activation mechanism shared among different receptor classes. Next, we summarize the recent progress that has been made in the Class F research using resonance energy transfer-based tools. We demonstrate that these efforts corroborate the idea that Class F receptors are indeed GPCRs. Given the clinical significance of GPCRs, medicinal chemistry strategies are now required to unravel the full therapeutic potential of targeting FZDs pharmacologically.

Keywords: GPCR, Frizzled, BRET, FRET, G protein, ternary complex model, SMO.

© Farm Pol, 2019, 75(8): 451–456