Publication details

Frizzleds and WNT/beta-catenin signaling - The black box of ligand-receptor selectivity, complex stoichiometry and activation kinetics

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Year of publication 2015
Type Article in Periodical
Magazine / Source European Journal of Pharmacology
MU Faculty or unit

Faculty of Science

Field Genetics and molecular biology
Keywords Receptor complex; Canonical signaling; GPCR; LRP5/6; Class Frizzled
Description The lipoglycoproteins of the mammalian WNT family induce beta-catenin-dependent signaling through interaction with members of the Class Frizzled receptors and LDL receptor-related protein 5/6 (LRP5/6) albeit with unknown selectivity. The 10 mammalian Frizzleds (FZDs) are seven transmembrane (7TM) spanning receptors and have recently been classified as G protein-coupled receptors (GPCRs). This review summarizes the current knowledge about WNT/FZD selectivity and functional selectivity, the role of co-receptors for signal specification, the formation of receptor complexes as well as the kinetics and mechanisms of signal initiation with focus on WNT/beta-catenin signaling. In order to exploit the true therapeutic potential of WNT/FZD signaling to treat human disease, it is clear that substantial progress in the understanding of receptor complex formation and signal specification has to precede a mechanism-based drug design targeting WNT receptors. (C) 2015 Elsevier B.V. All rights reserved
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