title: Dynamic mass redistribution assays decode surface influence on signaling of endogenous purinergic P2Y receptors.
abstract: Interactions with extracellular matrices (ECM) shape the signaling and functions of many types of cells and receptors, and distinct ECM coatings have been used in a wide range of substrates for drug discovery processes. Here, we investigate the influence of ECM protein coatings on the signaling of endogenous purinergic 2Y (P2Y) receptors in human embryonic kidney HEK293 cells using dynamic mass redistribution (DMR) assays enabled by label-free optical biosensor. Results showed that ECM proteins had significant impacts on the DMR characteristics, potency, and efficacy of seven P2Y agonists. This study documents the importance of surface chemistry in regulating receptor signaling.
authors: Science and Technology Division, Department of Biochemical Technologies, Corning Incorporated , Corning, New York 14831, USA.
authors: Elizabeth
authors: E
authors: Tran
authors: Haiyan
authors: H
authors: Sun
authors: Ye
authors: Y
authors: Fang
mesh_terms: D000244:Adenosine Diphosphate / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D000255:Adenosine Triphosphate / Q000378:metabolism / Q000494:pharmacology; D015374:Biosensing Techniques / Q000379:methods*; D004305:Dose-Response Relationship, Drug; D005109:Extracellular Matrix / Q000187:drug effects / Q000378:metabolism; D057809:HEK293 Cells; D006801:Humans; D058912:Purinergic P2Y Receptor Agonists / Q000378:metabolism / Q000494:pharmacology; D058921:Purinergic P2Y Receptor Antagonists / Q000378:metabolism / Q000494:pharmacology; D058470:Receptors, Purinergic P2Y / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects / Q000502:physiology*; D013499:Surface Properties / Q000187:drug effects; D014530:Uridine Diphosphate / Q000378:metabolism / Q000494:pharmacology
chemical_list: C111914:N(6)-methyl-2'-deoxyadenosine 3',5'-diphosphate; D058912:Purinergic P2Y Receptor Agonists; D058921:Purinergic P2Y Receptor Antagonists; D058470:Receptors, Purinergic P2Y; D014530:Uridine Diphosphate; D000244:Adenosine Diphosphate; D000255:Adenosine Triphosphate