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

  title={Design and characterization of a fluorescent ghrelin analog for imaging the growth hormone secretagogue receptor 1a},
  author={Rebecca McGirr and Mark S. McFarland and Jillian McTavish and Leonard G. Luyt and Savita Dhanvantari},
  journal={Regulatory Peptides},

Figures and Tables from this paper

Structure-Activity Study of Ghrelin(1-8) Resulting in High Affinity Fluorine-Bearing Ligands for the Ghrelin Receptor.
This paper reports on ghrelin(1-8) analogues bearing modifications at residues 1, 3, 4, and 8, which is not only the highest affinity gh Relin analogue reported but also the shortest ghrelIn analogue capable of binding GHS-R1a with better affinity than ghrel in(1 -28).
Development of a [68Ga]-ghrelin analogue for PET imaging of the ghrelin receptor (GHS-R1a).
This is the first example of ghrelin receptor PET imaging in a xenograft model using a peptide derived directly from the endogenous ligand and serves as motivation for developing more effective gh Relin-based radiopeptides.
Development of a ghrelin receptor inverse agonist for positron emission tomography
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 octanoylated
Stapled ghrelin peptides as fluorescent imaging probes
It is postulate that the lead stapled peptide can be used as a cancer cell‐specific fluorescent stain with potential research and clinical applications as compared to immunohistochemical approaches.
Development and Characterization of an 18F-labeled Ghrelin Peptidomimetic for Imaging the Cardiac Growth Hormone Secretagogue Receptor
This study synthesized and characterized a novel ghrelin peptidomimetic tracer, an 18F-labeled analogue of G-7039, for positron emission tomography (PET) imaging of cardiac GHSR1a, which is a potential biomarker for heart failure.
Novel and Conventional Receptors for Ghrelin, Desacyl-Ghrelin, and Pharmacologically Related Compounds
Benefits mediated through GRLRs or UAG receptors include adipocyte lipid accumulation, myoblast differentiation, osteoblast proliferation, insulin release, cardioprotection, coronary artery constriction, vascular endothelial cell proliferation, and tumor cell proliferation.
Characterization of an 18F-Growth Hormone Secretagogue Probe for Positron Emission Tomography Imaging of the Growth Hormone Secretagogue Receptor
The specificity of the novel tracer [1-Nal, Lys(4-[F]-FB)]G-7039 to target GHSR1a using Positron Emission Tomography (PET) is characterized, suggesting that there may be a ghrelin/GHSR 1a system in the heart that is regulated independently of systemic ghrelins, and that GHSr1a does not play a significant role in cardiac metabolism in healthy mice.
A Decade’s Progress in the Development of Molecular Imaging Agents Targeting the Growth Hormone Secretagogue Receptor
High-affinity analogues of ghrelin, the endogenous ligand for the GHSR, as well as small molecule inhibitors have been developed and evaluated both in vitro and in pre-clinical models to provide insights into its role in biological processes related to these disease states.


Fluorine and rhenium substituted ghrelin analogues as potential imaging probes for the growth hormone secretagogue receptor.
These fluorine and rhenium derivatives demonstrate the ability to modify the Ser-3 side chain of ghrelin in order to create imaging probes for the GHSR.
Structure-function studies on the new growth hormone-releasing peptide, ghrelin: minimal sequence of ghrelin necessary for activation of growth hormone secretagogue receptor 1a.
The entire sequence of ghrelin is not necessary for activity: the Gly-Ser-Ser(n-octanoyl)-Phe segment appears to constitute the "active core" required for agonist potency at hGHSR1a.
Structural Divergence of Human Ghrelin
Plasma levels of immunoreactive ghrelin after total gastrectomy in three patients were reduced to approximately half of their pre-gastrectomy values, after which they gradually increased, which suggests that the stomach is the major source of circulating gh Relin and that other tissues compensate for the loss of ghrelIn production after gast rectomy.
Ghrelin is a growth-hormone-releasing acylated peptide from stomach
The occurrence of ghrelin in both rat and human indicates that GH release from the pituitary may be regulated not only by hypothalamic GHRH, but also by ghrelIn, a peptide specifically releases GH both in vivo and in vitro.
Heterogeneity of Ghrelin/Growth Hormone Secretagogue Receptors
This review highlights the most recently discovered features of GHS-R1a and the emerging evidence for a novel group of receptors that are not of the GHS1a type; these appear involved in the transduction of the multiple levels of information provided by GHS and ghrelin.
[125I-His(9)]-ghrelin, a novel radioligand for localizing GHS orphan receptors in human and rat tissue: up-regulation of receptors with athersclerosis.
The characterized for the first time the binding of human [125I-His(9)]-ghrelin to normal human and rat tissue and demonstrated expression of this 'orphan' receptor that has previously been predicted to exist from mRNA are characterized and it is discovered that [125-Ghrelin density is significantly increased in atherosclerosis.