A Decade's Progress in the Development of Molecular Imaging Agents Targeting the Growth Hormone Secretagogue Receptor

MD Childs, LG Luyt - Molecular Imaging, 2020 - journals.sagepub.com
The growth hormone secretagogue receptor 1a (GHSR), also called the ghrelin receptor, is
a G protein-coupled receptor known to play an important metabolic role in the regulation of …

Advances in the development of nonpeptide small molecules targeting ghrelin receptor

G Giorgioni, F Del Bello, W Quaglia… - Journal of Medicinal …, 2022 - ACS Publications
Ghrelin is an octanoylated peptide acting by the activation of the growth hormone
secretagogue receptor, namely, GHS-R1a. The involvement of ghrelin in several …

[HTML][HTML] Development of a ghrelin receptor inverse agonist for positron emission tomography

R Bergmann, C Chollet, S Els-Heindl, M Ullrich… - Oncotarget, 2021 - ncbi.nlm.nih.gov
Imaging of Ghrelin receptors in vivo provides unique potential to gain deeper understanding
on Ghrelin and its receptors in health and disease, in particular, in cancer. Ghrelin, an …

Fluorine and rhenium substituted ghrelin analogues as potential imaging probes for the growth hormone secretagogue receptor

D Rosita, MA DeWit, LG Luyt - Journal of medicinal chemistry, 2009 - ACS Publications
In our effort to create imaging probes targeting the growth hormone secretagogue receptor
(GHSR), we now report on the design and synthesis of fluorine and rhenium containing …

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

CL Charron, MS McFarland, S Dhanvantari, LG Luyt - Medchemcomm, 2018 - pubs.rsc.org
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 …

Traceable peptidic ligands that target ghrelin receptors

M Liu, J Wade, MA Hossain - Current Protein and Peptide …, 2020 - ingentaconnect.com
Ghrelin is a 28-amino acid octanoylated peptide hormone that is implicated in many
physiological and pathophysiological processes. Specific visualization of ghrelin and its …

Design and characterization of a fluorescent ghrelin analog for imaging the growth hormone secretagogue receptor 1a

R McGirr, MS McFarland, J McTavish, LG Luyt… - Regulatory peptides, 2011 - Elsevier
Ghrelin is a 28-amino acid peptide hormone produced in the stomach. It binds to the growth
hormone secretagogue receptor 1a (GHS-R1a), a class A G-protein-coupled receptor. In the …

Synthesis and in vivo evaluation of (S)-6-(4-fluorophenoxy)-3-((1-[11C] methylpiperidin-3-yl) methyl)-2-o-tolylquinazolin-4 (3H)-one, a potential PET tracer for growth …

R Potter, AG Horti, HT Ravert, DP Holt, P Finley… - Bioorganic & medicinal …, 2011 - Elsevier
The peptide hormone ghrelin mediates through action on its receptor, the growth hormone
secretagogue receptor (GHSR), and is known to play an important role in a variety of …

Discovery of Ghrelin (1–8) analogues with Improved Stability and Functional Activity for PET Imaging

MD Childs, A Chandrabalan, D Hodgson… - ACS Pharmacology & …, 2023 - ACS Publications
The highest affinity ghrelin-based analogue for fluorine-18 positron emission
tomography,[Inp1, Dpr3 (6-FN), 1Nal4, Thr8] ghrelin (1–8) amide (1), has remarkable …

Developing new PET tracers to image the growth hormone secretagogue receptor 1a (GHS-R1a)

K Kawamura, M Fujinaga, Y Shimoda… - Nuclear Medicine and …, 2017 - Elsevier
IntroductionThe growth hormone secretagogue receptor 1a (GHS-R1a) is the orphan G-
protein-coupled receptor, and its endogenous ligand is ghrelin. GHS-R1a contributes to …