Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis

Chemical tools to monitor drug-target engagement of endogenous enzymes are essential for preclinical target validation. Here, the authors present a chemical genetics strategy to study target engagement of endogenous kinases, achieving specific labeling and inactivation of FES kinase to provide insig...

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Main Authors:	Tom van der Wel, Riet Hilhorst, Hans den Dulk, Tim van den Hooven, Nienke M. Prins, Joost A. P. M. Wijnakker, Bogdan I. Florea, Eelke B. Lenselink, Gerard J. P. van Westen, Rob Ruijtenbeek, Herman S. Overkleeft, Allard Kaptein, Tjeerd Barf, Mario van der Stelt
Format:	Article
Language:	English
Published:	Nature Publishing Group 2020-06-01
Series:	Nature Communications
Online Access:	https://doi.org/10.1038/s41467-020-17027-5

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spelling	doaj-749ac4b664044b4d9100599885c8e0632021-06-27T11:14:07ZengNature Publishing GroupNature Communications2041-17232020-06-0111112010.1038/s41467-020-17027-5Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosisTom van der Wel0Riet Hilhorst1Hans den Dulk2Tim van den Hooven3Nienke M. Prins4Joost A. P. M. Wijnakker5Bogdan I. Florea6Eelke B. Lenselink7Gerard J. P. van Westen8Rob Ruijtenbeek9Herman S. Overkleeft10Allard Kaptein11Tjeerd Barf12Mario van der Stelt13Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University & Oncode InstitutePamGene International BVDepartment of Molecular Physiology, Leiden Institute of Chemistry, Leiden University & Oncode InstitutePamGene International BVDepartment of Molecular Physiology, Leiden Institute of Chemistry, Leiden University & Oncode InstituteDepartment of Molecular Physiology, Leiden Institute of Chemistry, Leiden University & Oncode InstituteDepartment of Bio-organic Synthesis, Leiden Institute of Chemistry, Leiden UniversityDepartment of Drug Discovery & Safety, Leiden Academic Centre for Drug Research, Leiden UniversityDepartment of Drug Discovery & Safety, Leiden Academic Centre for Drug Research, Leiden UniversityPamGene International BVDepartment of Bio-organic Synthesis, Leiden Institute of Chemistry, Leiden UniversityCovalution Biosciences BVCovalution Biosciences BVDepartment of Molecular Physiology, Leiden Institute of Chemistry, Leiden University & Oncode InstituteChemical tools to monitor drug-target engagement of endogenous enzymes are essential for preclinical target validation. Here, the authors present a chemical genetics strategy to study target engagement of endogenous kinases, achieving specific labeling and inactivation of FES kinase to provide insights into FES’ role in neutrophil phagocytosis.https://doi.org/10.1038/s41467-020-17027-5
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Tom van der Wel Riet Hilhorst Hans den Dulk Tim van den Hooven Nienke M. Prins Joost A. P. M. Wijnakker Bogdan I. Florea Eelke B. Lenselink Gerard J. P. van Westen Rob Ruijtenbeek Herman S. Overkleeft Allard Kaptein Tjeerd Barf Mario van der Stelt
spellingShingle	Tom van der Wel Riet Hilhorst Hans den Dulk Tim van den Hooven Nienke M. Prins Joost A. P. M. Wijnakker Bogdan I. Florea Eelke B. Lenselink Gerard J. P. van Westen Rob Ruijtenbeek Herman S. Overkleeft Allard Kaptein Tjeerd Barf Mario van der Stelt Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis Nature Communications
author_facet	Tom van der Wel Riet Hilhorst Hans den Dulk Tim van den Hooven Nienke M. Prins Joost A. P. M. Wijnakker Bogdan I. Florea Eelke B. Lenselink Gerard J. P. van Westen Rob Ruijtenbeek Herman S. Overkleeft Allard Kaptein Tjeerd Barf Mario van der Stelt
author_sort	Tom van der Wel
title	Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis
title_short	Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis
title_full	Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis
title_fullStr	Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis
title_full_unstemmed	Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis
title_sort	chemical genetics strategy to profile kinase target engagement reveals role of fes in neutrophil phagocytosis
publisher	Nature Publishing Group
series	Nature Communications
issn	2041-1723
publishDate	2020-06-01
description	Chemical tools to monitor drug-target engagement of endogenous enzymes are essential for preclinical target validation. Here, the authors present a chemical genetics strategy to study target engagement of endogenous kinases, achieving specific labeling and inactivation of FES kinase to provide insights into FES’ role in neutrophil phagocytosis.
url	https://doi.org/10.1038/s41467-020-17027-5
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Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis

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