Platforms for high-throughput screening of Wnt/Frizzled antagonists

Alexey Koval; Vladimir L. Katanaev

doi:10.1016/j.drudis.2012.07.007

Platforms for high-throughput screening of Wnt/Frizzled antagonists

Alexey Koval, Vladimir L. Katanaev^*

^*Corresponding author for this work

Research output: Contribution to journal › Review article › peer-review

30 Citations (Scopus)

Abstract

Signaling cascades initiated by Wnt lipoglycoproteins and their receptors of the Frizzled family regulate many aspects of animal development and physiology. Improper activation of this signaling promotes carcinogenic transformation and metastasis. Development of agents blocking the Wnt-Frizzled signaling is of prime interest for drug discovery. Despite certain progress no such agents are as yet brought to the market or even to clinical trials. One reason for these delays might be the use of suboptimal readout assays. In this article we overview existing and developing assay platforms to screen for Wnt-Frizzled antagonists. Among those, G protein-activating assays built on the emerging GPCR properties of Frizzleds are highlighted.

Original language	English
Pages (from-to)	1316-1322
Number of pages	7
Journal	Drug Discovery Today
Volume	17
Issue number	23-24
DOIs	https://doi.org/10.1016/j.drudis.2012.07.007
Publication status	Published - Dec 2012
Externally published	Yes

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10.1016/j.drudis.2012.07.007

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title = "Platforms for high-throughput screening of Wnt/Frizzled antagonists",

abstract = "Signaling cascades initiated by Wnt lipoglycoproteins and their receptors of the Frizzled family regulate many aspects of animal development and physiology. Improper activation of this signaling promotes carcinogenic transformation and metastasis. Development of agents blocking the Wnt-Frizzled signaling is of prime interest for drug discovery. Despite certain progress no such agents are as yet brought to the market or even to clinical trials. One reason for these delays might be the use of suboptimal readout assays. In this article we overview existing and developing assay platforms to screen for Wnt-Frizzled antagonists. Among those, G protein-activating assays built on the emerging GPCR properties of Frizzleds are highlighted.",

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AU - Katanaev, Vladimir L.

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AB - Signaling cascades initiated by Wnt lipoglycoproteins and their receptors of the Frizzled family regulate many aspects of animal development and physiology. Improper activation of this signaling promotes carcinogenic transformation and metastasis. Development of agents blocking the Wnt-Frizzled signaling is of prime interest for drug discovery. Despite certain progress no such agents are as yet brought to the market or even to clinical trials. One reason for these delays might be the use of suboptimal readout assays. In this article we overview existing and developing assay platforms to screen for Wnt-Frizzled antagonists. Among those, G protein-activating assays built on the emerging GPCR properties of Frizzleds are highlighted.

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Platforms for high-throughput screening of Wnt/Frizzled antagonists

Abstract

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