Design, synthesis and characterization of a fluorescently labeled functional analog of full-length human ghrelin
Mengjie Liu, Emily A Whitfield, Linda J Fothergill, John B Furness, John D Wade, Sebastian GB Furness, Mohammed Akhter Hossain
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | ACADEMIC PRESS INC ELSEVIER SCIENCE | Published : 2020
Human ghrelin receptor (GHSR) is a recognized prospective target in the diagnosis and therapy of multiple cancer types. To gain a better understanding of this receptor signaling system, we have synthesized a novel full-length ghrelin analog that is fluorescently labeled at the side-chain of a C-terminal cysteine extension. This analog exhibited nanomolar affinity and potency for the ghrelin receptor. It shows comparable efficacy with that of endogenous ghrelin. The fluorescently-labeled ghrelin analog is a valuable tool for in vitro imaging of cell lines that express ghrelin receptor.
Awarded by Autralian Research Council (ARC)
Awarded by National Health & Medical Research Council (Australia) (NHMRC)
SGBF is an Autralian Research Council (ARC) Future Fellow (FT180100543) and JDW is an National Health & Medical Research Council (Australia) (NHMRC) Principal Research Fellow (APP1117483). Studies at the Florey Institute were supported by the Victorian Government's Operational Infrastructure Support Program.