Development of a [⁶⁸Ga]-ghrelin analogue for PET imaging of the ghrelin receptor (GHS-R1a).

ABSTRACT: The ghrelin receptor is a member of the growth hormone secretagogue receptor (GHS-R) family and is present at low concentrations in tissues such as the brain, kidney, cardiovascular system, and prostate. The ghrelin receptor plays an important role in cellular proliferation, apoptosis, invasion, and migration associated with the progression of many cancers, including prostate, breast, ovarian, testicular, and intestinal carcinomas. Ghrelin, the endogenous ligand, is a 28 amino acid peptide (IC₅₀ = 3.1 nM) known to have poor in vivo stability. Herein, we report the synthesis and evaluation of [Dpr³(octanoyl),Lys¹⁹(Ga-DOTA)]ghrelin(1-19). This new ghrelin analogue has a binding affinity (IC₅₀ = 5.9 nM) comparable to that of natural ghrelin.

SUBMITTER: Charron CL 

PROVIDER: S-EPMC6194486 | biostudies-literature | 2018 Oct

REPOSITORIES: biostudies-literature