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Updated: Jun 28, 2025

Comprehensive Analysis of Drug Response using the FLICK Assay
Published on: June 6, 2025
Frizzleds act as dynamic pharmacological entities
Gunnar Schulte1, Magdalena M Scharf1, Julien Bous1
1Section of Receptor Biology & Signaling, Dept. Physiology & Pharmacology, Karolinska Institutet, S-171 77 Stockholm, Sweden.
None:
The Frizzled family of transmembrane receptors (FZD1-10) belongs to the class F of G protein-coupled receptors (GPCRs). FZDs bind to and are activated by Wingless/Int1 (WNT) proteins. The WNT/FZD signaling system regulates crucial aspects of developmental biology and stem-cell regulation. Dysregulation of WNT/FZD communication can lead to developmental defects and diseases such as cancer and fibrosis. Recent insight into the activation mechanisms of FZDs has underlined that protein dynamics and conserved microswitches are essential for FZD-mediated information flow and build the basis for targeting these receptors pharmacologically. In this review, we summarize recent advances in our understanding of FZD activation, and how novel concepts merge and collide with existing dogmas in the field.
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