Structural insight into Class F receptors - What have we learnt regarding agonist-induced activation?


Journal article


G. Schulte, P. Kozielewicz
Basic & Clinical Pharmacology & Toxicology, 2019

Semantic Scholar DOI PubMed
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APA   Click to copy
Schulte, G., & Kozielewicz, P. (2019). Structural insight into Class F receptors - What have we learnt regarding agonist-induced activation? Basic &Amp; Clinical Pharmacology &Amp; Toxicology.


Chicago/Turabian   Click to copy
Schulte, G., and P. Kozielewicz. “Structural Insight into Class F Receptors - What Have We Learnt Regarding Agonist-Induced Activation?” Basic & Clinical Pharmacology & Toxicology (2019).


MLA   Click to copy
Schulte, G., and P. Kozielewicz. “Structural Insight into Class F Receptors - What Have We Learnt Regarding Agonist-Induced Activation?” Basic &Amp; Clinical Pharmacology &Amp; Toxicology, 2019.


BibTeX   Click to copy

@article{g2019a,
  title = {Structural insight into Class F receptors - What have we learnt regarding agonist-induced activation?},
  year = {2019},
  journal = {Basic & Clinical Pharmacology & Toxicology},
  author = {Schulte, G. and Kozielewicz, P.}
}

Abstract

Class F receptors, including the ten Frizzleds (FZD1-10 ) 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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