title: Light-assisted small-molecule screening against protein kinases.
abstract: High-throughput live-cell screens are intricate elements of systems biology studies and drug discovery pipelines. Here, we demonstrate an optogenetics-assisted method that avoids the need for chemical activators and reporters, reduces the number of operational steps and increases information content in a cell-based small-molecule screen against human protein kinases, including an orphan receptor tyrosine kinase. This blueprint for all-optical screening can be adapted to many drug targets and cellular processes.
authors.affiliation: Institute of Science and Technology Austria (IST Austria), Klosterneuburg, Austria.
authors.forename: Álvaro
authors.identifier: http://orcid.org/0000-0002-5409-8571
authors.initials: Á
authors.lastname: Inglés-Prieto
authors.affiliation: Institute of Science and Technology Austria (IST Austria), Klosterneuburg, Austria.
authors.forename: Eva
authors.initials: E
authors.lastname: Reichhart
authors.affiliation: CeMM-Research Center for Molecular Medicine of the Austrian Academy of Sciences, Vienna, Austria.
authors.forename: Markus K
authors.initials: MK
authors.lastname: Muellner
authors.affiliation: Institute of Science and Technology Austria (IST Austria), Klosterneuburg, Austria.
authors.forename: Matthias
authors.initials: M
authors.lastname: Nowak
authors.affiliation: CeMM-Research Center for Molecular Medicine of the Austrian Academy of Sciences, Vienna, Austria.
authors.forename: Sebastian M B
authors.initials: SM
authors.lastname: Nijman
authors.affiliation: Institute of Cancer Research, Department of Medicine I, Comprehensive Cancer Center Vienna, Medical University of Vienna, Vienna, Austria.
authors.forename: Michael
authors.initials: M
authors.lastname: Grusch
authors.affiliation: Institute of Science and Technology Austria (IST Austria), Klosterneuburg, Austria.
authors.forename: Harald
authors.initials: H
authors.lastname: Janovjak
mesh_terms: D057809:HEK293 Cells; D057166:High-Throughput Screening Assays; D006801:Humans; D008027:Light; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D011494:Protein Kinases / Q000378:metabolism*; D054852:Small Molecule Libraries / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D047428:Protein Kinase Inhibitors; D054852:Small Molecule Libraries; D011494:Protein Kinases