title: Split Gaussia luciferase for imaging ligand-receptor binding.
abstract: Ligand binding to cell surface receptors activates signaling pathways in normal and pathologic conditions, and internalized ligand-receptor complexes may continue to signal from endosomes. Accessibility of cell surface receptors and the central function of ligand-receptor binding in signal transduction make ligand binding a prime target for therapeutic agents. We describe a Gaussia luciferase complementation method for imaging ligand-receptor binding in cell-based assays and living mice. While we illustrate this imaging method for chemokine ligand CXCL12 and its receptors CXCR4 and CXCR7, this imaging strategy can be generalized to a large number of ligand-receptor interactions.
authors.affiliation: Center for Molecular Imaging, Department of Radiology, University of Michigan, Ann Arbor, MI, USA.
authors.forename: Kathryn E
authors.initials: KE
authors.lastname: Luker
authors.forename: Gary D
authors.initials: GD
authors.lastname: Luker
mesh_terms: D000818:Animals; D054377:Chemokine CXCL12 / Q000378:metabolism*; D033342:Copepoda / Q000201:enzymology*; D057809:HEK293 Cells; D006801:Humans; D008024:Ligands; D008156:Luciferases / Q000378:metabolism*; D008163:Luminescent Measurements; D008164:Luminescent Proteins / Q000378:metabolism*; D051379:Mice; D057054:Molecular Imaging / Q000379:methods*; D011485:Protein Binding; D054387:Receptors, CXCR / Q000378:metabolism*; D019718:Receptors, CXCR4 / Q000378:metabolism*
chemical_list: C501896:ACKR3 protein, human; D054377:Chemokine CXCL12; D008024:Ligands; D008164:Luminescent Proteins; D054387:Receptors, CXCR; D019718:Receptors, CXCR4; D008156:Luciferases