title: Bioorthogonal chemistry for (68) Ga radiolabelling of DOTA-containing compounds.
abstract: Copper-catalysed 'click' chemistry is a highly utilised technique for radiolabelling small molecules and peptides for imaging applications. The usefulness of these reactions falls short, however, when metal catalysis is not a practically viable route; such as when using metal chelates as radioligands. Here, we describe a method for carrying out 'click-type' radiochemistry in the presence of DOTA chelates, by combining (68) Ga radiolabelling techniques with well-established bioorthogonal reactions, which do not rely upon metal catalysis.
authors.affiliation: Comprehensive Cancer Imaging Centre, Department of Surgery & Cancer, Hammersmith Campus, Imperial College, London, UK.
authors.forename: Helen L
authors.initials: HL
authors.lastname: Evans
authors.forename: Laurence
authors.initials: L
authors.lastname: Carroll
authors.forename: Eric O
authors.initials: EO
authors.lastname: Aboagye
authors.forename: Alan C
authors.initials: AC
authors.lastname: Spivey
mesh_terms: D001386:Azides / Q000737:chemistry; D002614:Chelating Agents / Q000737:chemistry; D057930:Click Chemistry; D015195:Drug Design; D005710:Gallium Radioisotopes / Q000737:chemistry; D006573:Heterocyclic Compounds, 1-Ring / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods*; D049268:Positron-Emission Tomography; D011719:Pyrazines / Q000737:chemistry; D011854:Radiochemistry / Q000379:methods*; D019275:Radiopharmaceuticals / Q000737:chemistry*
chemical_list: D001386:Azides; D002614:Chelating Agents; D005710:Gallium Radioisotopes; D006573:Heterocyclic Compounds, 1-Ring; D011719:Pyrazines; D019275:Radiopharmaceuticals; C071349:1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
keywords: Bioorthogonal chemistry; DOTA; Gallium-68; azide; click chemistry; cyclooctyne; norbornene; strained alkene; tetrazine