title: Label-Free Cell Phenotypic Identification of D-Luciferin as an Agonist for GPR35.
abstract: D-Luciferin (also known as beetle or firefly luciferin) is one of the most widely used bioluminescent reporters for monitoring in vitro or in vivo luciferase activity. The identification of several natural phenols and thieno[3,2-b]thiophene-2-carboxylic acid derivatives as agonists for GPR35, an orphan G protein-coupled receptor, had motivated us to examine the pharmacological activity of D-Luciferin, given that it also contains phenol and carboxylic acid moieties. Here, we describe label-free cell phenotypic assays that ascertain D-Luciferin as a partial agonist for GPR35. The agonistic activity of D-Luciferin at the GPR35 shall evoke careful interpretation of biological data when D-Luciferin or its analogues are used as probes.
authors.affiliation: Medical Laboratory Science, Jefferson College of Health Science/Carilion Roanoke Memorial Hospital, Quest Diagnostic Lab, Carilion Clinic Health System, Roanoke, VA, USA.
authors.forename: Heidi
authors.initials: H
authors.lastname: Hu
authors.affiliation: Biochemical Technologies, Science and Technology Division, Corning Incorporated, Corning, NY, 14831, USA.
authors.forename: Huayun
authors.initials: H
authors.lastname: Deng
authors.affiliation: Biochemical Technologies, Science and Technology Division, Corning Incorporated, Corning, NY, 14831, USA. fangy2@corning.com.
authors.forename: Ye
authors.initials: Y
authors.lastname: Fang
mesh_terms: D052160:Benzothiazoles / Q000737:chemistry / Q000494:pharmacology*; D015374:Biosensing Techniques; D018929:Cell Culture Techniques; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D006801:Humans; D008163:Luminescent Measurements / Q000379:methods; D021381:Protein Transport; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000037:antagonists & inhibitors / Q000378:metabolism; D000071557:beta-Arrestins / Q000378:metabolism
chemical_list: D052160:Benzothiazoles; C532924:D-luciferin; C111379:GPR35 protein, human; D043562:Receptors, G-Protein-Coupled; D000071557:beta-Arrestins
keywords: Bioluminescence; D-Luciferin; Dynamic mass redistribution; G protein-coupled receptor; GPR35; Resonant waveguide grating biosensor