title: Multidimensional GPCR profiling and screening using impedance-based label-free and real-time assay.
abstract: GPCRs constitute one of the most sought-after targets in drug discovery because they are associated with conditions ranging from cardiovascular diseases, autoimmune diseases, inflammation, cancer, and diseases of the nervous system. Moreover, they are one of the most amenable targets for drug discovery because they can be modulated by small molecules, peptides, proteins, and antibodies. Therefore it may not come as a surprise that close to 40 % of the drugs that are currently on the market are targeting GPCRs. It has become evident that GPCR signaling is highly complex and may involve multiple or a subset of pathways depending on the interaction of a GPCR with an agonist or antagonist. It is imperative that any functional screening for GPCR activity integrates this complexity. In this assay protocol, we describe how the xCELLigence RTCA HT impedance-based platform which can be used for functional cell-based GPCR assays can be utilized for GPCR screening.
authors.affiliation: ACEA Biosciences, 6779 Mesa Ridge Rd., San Diego, CA, 92121, USA.
authors.forename: Ning
authors.initials: N
authors.lastname: Ke
authors.forename: Khanh
authors.initials: K
authors.lastname: Nguyen
authors.forename: Jeffery
authors.initials: J
authors.lastname: Irelan
authors.forename: Yama A
authors.initials: YA
authors.lastname: Abassi
mesh_terms: D058647:Adrenergic alpha-2 Receptor Agonists / Q000494:pharmacology*; D058669:Adrenergic alpha-2 Receptor Antagonists / Q000494:pharmacology*; D000818:Animals; D019540:Area Under Curve; D000068438:Brimonidine Tartrate; D016466:CHO Cells; D003412:Cricetulus; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D017097:Electric Impedance; D006367:HeLa Cells; D057166:High-Throughput Screening Assays; D006801:Humans; D011810:Quinoxalines / Q000494:pharmacology*; D018341:Receptors, Adrenergic, alpha-2 / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism; D015398:Signal Transduction; D015016:Yohimbine / Q000494:pharmacology*
chemical_list: D058647:Adrenergic alpha-2 Receptor Agonists; D058669:Adrenergic alpha-2 Receptor Antagonists; D011810:Quinoxalines; D018341:Receptors, Adrenergic, alpha-2; D011994:Recombinant Proteins; D015016:Yohimbine; D000068438:Brimonidine Tartrate