作者: Margot W. Beukers , Adriaan P. IJzerman
DOI: 10.1016/J.TIPS.2005.08.005
关键词:
摘要: G-protein-coupled receptors (GPCRs) are the major targets of today's medicines. To elucidate mechanism activation GPCRs and interaction these with their G proteins, mutagenesis studies have proven to be a powerful tool provided insight into structure function GPCRs. Random is useful in this respect particularly when combined robust screening assay that based on functional properties mutants. In article, use random yeast described compared alternative approaches such as site-directed per se, alanine/cysteine scanning another assay, receptor selection amplification technology (R-SAT). Screening randomly mutated has successful identification ligands for orphan high-throughput approaches. Moreover, it substantial G-protein coupling activation.