Application of an integrated physical and functional screening approach to identify inhibitors of the Wnt pathway

Abstract Large‐scale proteomic approaches have been used to study signaling pathways. However, identification of biologically relevant hits from a single screen remains challenging due to limitations inherent in each individual approach. To overcome these limitations, we implemented an integrated, m...

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Main Authors: Bryan W Miller, Garnet Lau, Chris Grouios, Emanuela Mollica, Miriam Barrios‐Rodiles, Yongmei Liu, Alessandro Datti, Quaid Morris, Jeffrey L Wrana, Liliana Attisano
Format: Article
Language:English
Published: Springer Nature 2009-10-01
Series:Molecular Systems Biology
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Online Access:https://doi.org/10.1038/msb.2009.72
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author Bryan W Miller
Garnet Lau
Chris Grouios
Emanuela Mollica
Miriam Barrios‐Rodiles
Yongmei Liu
Alessandro Datti
Quaid Morris
Jeffrey L Wrana
Liliana Attisano
author_facet Bryan W Miller
Garnet Lau
Chris Grouios
Emanuela Mollica
Miriam Barrios‐Rodiles
Yongmei Liu
Alessandro Datti
Quaid Morris
Jeffrey L Wrana
Liliana Attisano
author_sort Bryan W Miller
collection DOAJ
description Abstract Large‐scale proteomic approaches have been used to study signaling pathways. However, identification of biologically relevant hits from a single screen remains challenging due to limitations inherent in each individual approach. To overcome these limitations, we implemented an integrated, multi‐dimensional approach and used it to identify Wnt pathway modulators. The LUMIER protein–protein interaction mapping method was used in conjunction with two functional screens that examined the effect of overexpression and siRNA‐mediated gene knockdown on Wnt signaling. Meta‐analysis of the three data sets yielded a combined pathway score (CPS) for each tested component, a value reflecting the likelihood that an individual protein is a Wnt pathway regulator. We characterized the role of two proteins with high CPSs, Ube2m and Nkd1. We show that Ube2m interacts with and modulates β‐catenin stability, and that the antagonistic effect of Nkd1 on Wnt signaling requires interaction with Axin, itself a negative pathway regulator. Thus, integrated physical and functional mapping in mammalian cells can identify signaling components with high confidence and provides unanticipated insights into pathway regulators.
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spelling doaj-art-c93cae2ed5fc49f2a5aad7c0004c5e492025-08-24T11:59:09ZengSpringer NatureMolecular Systems Biology1744-42922009-10-015111310.1038/msb.2009.72Application of an integrated physical and functional screening approach to identify inhibitors of the Wnt pathwayBryan W Miller0Garnet Lau1Chris Grouios2Emanuela Mollica3Miriam Barrios‐Rodiles4Yongmei Liu5Alessandro Datti6Quaid Morris7Jeffrey L Wrana8Liliana Attisano9Department of Biochemistry, University of TorontoDepartment of Biochemistry, University of TorontoBanting and Best Department of Medical Research, University of TorontoDepartment of Biochemistry, University of TorontoCentre for Systems Biology, Samuel Lunenfeld Research Institute, Mount Sinai HospitalCentre for Systems Biology, Samuel Lunenfeld Research Institute, Mount Sinai HospitalSamuel Lunenfeld Research Institute, Mount Sinai HospitalDonnelly Centre for Cellular and Biomolecular Research, University of TorontoCentre for Systems Biology, Samuel Lunenfeld Research Institute, Mount Sinai HospitalDepartment of Biochemistry, University of TorontoAbstract Large‐scale proteomic approaches have been used to study signaling pathways. However, identification of biologically relevant hits from a single screen remains challenging due to limitations inherent in each individual approach. To overcome these limitations, we implemented an integrated, multi‐dimensional approach and used it to identify Wnt pathway modulators. The LUMIER protein–protein interaction mapping method was used in conjunction with two functional screens that examined the effect of overexpression and siRNA‐mediated gene knockdown on Wnt signaling. Meta‐analysis of the three data sets yielded a combined pathway score (CPS) for each tested component, a value reflecting the likelihood that an individual protein is a Wnt pathway regulator. We characterized the role of two proteins with high CPSs, Ube2m and Nkd1. We show that Ube2m interacts with and modulates β‐catenin stability, and that the antagonistic effect of Nkd1 on Wnt signaling requires interaction with Axin, itself a negative pathway regulator. Thus, integrated physical and functional mapping in mammalian cells can identify signaling components with high confidence and provides unanticipated insights into pathway regulators.https://doi.org/10.1038/msb.2009.72cancer biologysignal transductionsystems biology
spellingShingle Bryan W Miller
Garnet Lau
Chris Grouios
Emanuela Mollica
Miriam Barrios‐Rodiles
Yongmei Liu
Alessandro Datti
Quaid Morris
Jeffrey L Wrana
Liliana Attisano
Application of an integrated physical and functional screening approach to identify inhibitors of the Wnt pathway
Molecular Systems Biology
cancer biology
signal transduction
systems biology
title Application of an integrated physical and functional screening approach to identify inhibitors of the Wnt pathway
title_full Application of an integrated physical and functional screening approach to identify inhibitors of the Wnt pathway
title_fullStr Application of an integrated physical and functional screening approach to identify inhibitors of the Wnt pathway
title_full_unstemmed Application of an integrated physical and functional screening approach to identify inhibitors of the Wnt pathway
title_short Application of an integrated physical and functional screening approach to identify inhibitors of the Wnt pathway
title_sort application of an integrated physical and functional screening approach to identify inhibitors of the wnt pathway
topic cancer biology
signal transduction
systems biology
url https://doi.org/10.1038/msb.2009.72
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