Design, synthesis and characterization of a fluorescently labeled functional analog of full-length human ghrelin.

Biochem Biophys Res Commun

Florey Institute of Neuroscience and Mental Health, The University of Melbourne, Parkville, VIC, 3010, Australia; School of Chemistry, The University of Melbourne, Parkville, VIC, 3010, Australia. Electronic address:

Published: December 2020


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Article Abstract

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.

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http://dx.doi.org/10.1016/j.bbrc.2020.09.028DOI Listing

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