Journal
BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY
Volume 126, Issue -, Pages 17-24Publisher
WILEY
DOI: 10.1111/bcpt.13235
Keywords
Frizzled; G protein-coupled receptors (GPCR); heterotrimeric G proteins; Smoothened; ternary complex model; WNT
Categories
Funding
- Swedish Research Council [2015-02899] Funding Source: Swedish Research Council
- Karolinska Institutet Funding Source: Medline
- Knut and Alice Wallenberg Foundation [KAW2008.0149] Funding Source: Medline
- Novo Nordisk Fonden [NNF17OC0026940] Funding Source: Medline
- Stiftelsen Olle Engkvist Byggmästare [2016/193] Funding Source: Medline
- Swedish Cancer Society [CAN2014/659, 833 CAN2017/561] Funding Source: Medline
- Swedish Research Council [2013-5708, 2015-02899] Funding Source: Medline
- Emil och Wera Cornells Stiftelse Funding Source: Medline
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Class F receptors, including the ten Frizzleds (FZD(1-10)) and SMO, mediate the effects of WNTs and hedgehog proteins and belong to the superfamily of G protein-coupled receptors (GPCRs). While the recent, high-resolution insight into mechanisms of GPCR activation provides a better understanding of receptor activation in Class A, B and C GPCRs, it remains unclear how Class F receptors bind their ligands, how ligand binding is translated to receptor activation and how signal initiation and specification are achieved. Here, we summarize recent efforts in elucidating Class F receptor structure and activation mechanisms and critically discuss the progress made in this area. A better understanding of the activation mechanisms of Class F receptors is required to engage in mechanism-based and structure-guided drug discovery to exploit the large therapeutic potential of targeting these receptors pharmacologically.
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