title: Combining functional genomics and chemical biology to identify targets of bioactive compounds.
abstract: Genome sequencing projects have revealed thousands of suspected genes, challenging researchers to develop efficient large-scale functional analysis methodologies. Determining the function of a gene product generally requires a means to alter its function. Genetically tractable model organisms have been widely exploited for the isolation and characterization of activating and inactivating mutations in genes encoding proteins of interest. Chemical genetics represents a complementary approach involving the use of small molecules capable of either inactivating or activating their targets. Saccharomyces cerevisiae has been an important test bed for the development and application of chemical genomic assays aimed at identifying targets and modes of action of known and uncharacterized compounds. Here we review yeast chemical genomic assays strategies for drug target identification.
authors.affiliation: Banting and Best Department of Medical Research and Department of Molecular Genetics, The Donnelly Centre, University of Toronto, 160 College St., Toronto, ON, Canada M5S 3E1.
authors.forename: Cheuk Hei
authors.initials: CH
authors.lastname: Ho
authors.forename: Jeff
authors.initials: J
authors.lastname: Piotrowski
authors.forename: Scott J
authors.initials: SJ
authors.lastname: Dixon
authors.forename: Anastasia
authors.initials: A
authors.lastname: Baryshnikova
authors.forename: Michael
authors.initials: M
authors.lastname: Costanzo
authors.forename: Charles
authors.initials: C
authors.lastname: Boone
mesh_terms: D000818:Animals; D001671:Biochemistry / Q000379:methods*; D055808:Drug Discovery; D025141:Drug Resistance, Fungal; D023281:Genomics / Q000379:methods*; D006801:Humans; D009154:Mutation; D012441:Saccharomyces cerevisiae / Q000737:chemistry* / Q000235:genetics