title: Quenching resonance energy transfer (QRET): a single-label technique for inhibitor screening and interaction studies.
abstract: The increased number of therapeutic targets has led to a growing need for screening methods enabling possible inhibitor compound selection. Information for new therapeutic targets has been found mostly from sequencing of the human genome but this knowledge cannot be directly converted into clinically relevant drug molecules. After target identification, the multistep drug development process takes many years and hundreds of millions of dollars are spent without certainty of the outcome. The first and the most critical step in the drug development process is hit selection. The optimal high throughput screening method should provide the highest possible number of true positive hits for further studies and lead discovery. The result should be achieved with low material consumption in a rapid and automated process. Radioactive label based methods are sensitive, but due to the problems arising from the radioactivity, luminescence-based methods have become increasingly popular in screening. In this review, the time-resolved luminescence based quenching resonance energy transfer (QRET) technique is discussed for primary screening.
authors.affiliation: Institute of Biomedicine, Department of Cell Biology and Anatomy, University of Turku, Kiinamyllynkatu 10, 3rd Floor, FI-20520 Turku, Finland. Electronic address: kari.kopra@utu.fi.
authors.forename: Kari
authors.initials: K
authors.lastname: Kopra
authors.affiliation: Institute of Biomedicine, Department of Cell Biology and Anatomy, University of Turku, Kiinamyllynkatu 10, 3rd Floor, FI-20520 Turku, Finland.
authors.forename: Harri
authors.initials: H
authors.lastname: Härmä
mesh_terms: D004353:Drug Evaluation, Preclinical / Q000379:methods*; D031541:Fluorescence Resonance Energy Transfer / Q000379:methods*; D028581:Lanthanoid Series Elements / Q000032:analysis / Q000737:chemistry*; D057054:Molecular Imaging / Q000379:methods*; D025941:Protein Interaction Mapping / Q000379:methods*; D013194:Staining and Labeling / Q000379:methods
chemical_list: D028581:Lanthanoid Series Elements