Sharma Neha, Barbon Stephanie M, Lalonde Tyler, Maar Ryan R, Milne Mark, Gilroy Joe B, Luyt Leonard G
Department of Chemistry, University of Western Ontario 1151 Richmond Street London Ontario N6A 5B7 Canada
London Regional Cancer Program, Lawson Health Research Institute 800 Commissioners Road East London Ontario N6A 5W9 Canada.
RSC Adv. 2020 May 19;10(32):18970-18977. doi: 10.1039/d0ra02104k. eCollection 2020 May 14.
Two new fluorescence imaging probes have been synthesized by incorporating a versatile alkyne-substituted boron difluoride formazanate precursor with peptides through copper-catalyzed alkyne-azide cycloaddition. The formazanate dye was appended to a C-terminal amino acid of ghrelin for imaging the growth hormone secretagogue receptor (GHSR-1a). To demonstrate versatile bioconjugation chemistry, the formazanate dye was added to the N-terminus of bombesin for targeting the gastrin releasing peptide receptor (GRPR). These are the first examples of using this emerging class of dyes, boron difluoride formazanates, for the labelling of biomolecules.
通过铜催化的炔烃-叠氮环加成反应，将一种通用的炔烃取代的二氟化硼甲脒前体与肽结合，合成了两种新型荧光成像探针。将甲脒染料连接到胃饥饿素的C端氨基酸上，用于成像生长激素促分泌素受体（GHSR-1a）。为了证明通用的生物共轭化学，将甲脒染料添加到蛙皮素的N端，用于靶向胃泌素释放肽受体（GRPR）。这些是使用这类新兴染料——二氟化硼甲脒——标记生物分子的首批实例。
