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

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216224%3A14310%2F15%3A00088753" target="_blank" >RIV/00216224:14310/15:00088753 - isvavai.cz</a>

Výsledek na webu

<a href="http://www.sciencedirect.com/science/article/pii/S0014299915300157" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0014299915300157</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.ejphar.2015.05.031" target="_blank" >10.1016/j.ejphar.2015.05.031</a>

Jazyk výsledku

angličtina

Název v původním jazyce

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

Popis výsledku v původním jazyce

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

Název v anglickém jazyce

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

Popis výsledku anglicky

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

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

EB - Genetika a molekulární biologie

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2015

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

European Journal of Pharmacology

ISSN

0014-2999

e-ISSN

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Svazek periodika

763

Číslo periodika v rámci svazku

September

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

5

Strana od-do

191-195

Kód UT WoS článku

000361822600009

EID výsledku v databázi Scopus

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