title: Solid-phase biological assays for drug discovery.
abstract: In the past 30 years, there has been a significant growth in the use of solid-phase assays in the area of drug discovery, with a range of new assays being used for both soluble and membrane-bound targets. In this review, we provide some basic background to typical drug targets and immobilization protocols used in solid-phase biological assays (SPBAs) for drug discovery, with emphasis on particularly labile biomolecular targets such as kinases and membrane-bound receptors, and highlight some of the more recent approaches for producing protein microarrays, bioaffinity columns, and other devices that are central to small molecule screening by SPBA. We then discuss key applications of such assays to identify drug leads, with an emphasis on the screening of mixtures. We conclude by highlighting specific advantages and potential disadvantages of SPBAs, particularly as they relate to particular assay formats.
authors.affiliation: Biointerfaces Institute, McMaster University, Hamilton, Ontario L8S 4L8, Canada; email: brennanj@mcmaster.ca.
authors.forename: Erica M
authors.initials: EM
authors.lastname: Forsberg
authors.forename: Clémence
authors.initials: C
authors.lastname: Sicard
authors.forename: John D
authors.initials: JD
authors.lastname: Brennan
mesh_terms: D000818:Animals; D001681:Biological Assay / Q000379:methods*; D055808:Drug Discovery; D057166:High-Throughput Screening Assays / Q000379:methods*; D006801:Humans; D040081:Protein Array Analysis / Q000379:methods*; D054852:Small Molecule Libraries / Q000032:analysis* / Q000737:chemistry
chemical_list: D054852:Small Molecule Libraries
keywords: bioaffinity chromatography; kinases; membrane proteins; protein microarrays