Comparison of the tissue distribution of a long-circulating glucagon-like Peptide-1 agonist determined by positron emission tomography and quantitative whole-body …

EFA Fernandes, J Wilbs, R Raavé… - ACS Pharmacology & …, 2022 - ACS Publications
Positron emission tomography (PET) is a molecular imaging modality that enables non-
invasive visualization of tracer distribution and pharmacology. Recently, peptides with long …

New Long-Acting [89Zr]Zr-DFO GLP-1 PET Tracers with Increased Molar Activity and Reduced Kidney Accumulation

J Wilbs, R Raavé, M Boswinkel, T Glendorf… - Journal of Medicinal …, 2023 - ACS Publications
Positron emission tomography (PET) imaging is used in drug development to noninvasively
measure biodistribution and receptor occupancy. Ideally, PET tracers retain target binding …

[HTML][HTML] Synthesis and evaluation of zirconium-89 labelled and long-lived GLP-1 receptor agonists for PET imaging

CB Jacobsen, R Raavé, MØ Pedersen… - Nuclear Medicine and …, 2020 - Elsevier
Introduction Lately, zirconium-89 has shown great promise as a radionuclide for PET
applications of long circulating biomolecules. Here, the design and synthesis of protracted …

Glucagonlike peptide-1 receptor imaging in individuals with type 2 diabetes

O Eriksson, I Velikyan, T Haack, M Bossart… - Journal of Nuclear …, 2022 - Soc Nuclear Med
The glucagonlike peptide-1 receptor (GLP1R) is a gut hormone receptor, intricately linked to
regulation of blood glucose homeostasis via several mechanisms. It is an established and …

First-in-class positron emission tomography tracer for the glucagon receptor

I Velikyan, T Haack, M Bossart, A Evers, I Laitinen… - EJNMMI research, 2019 - Springer
The glucagon receptor (GCGR) is emerging as an important target in anti-diabetic therapy,
especially as part of the pharmacology of dual glucagon-like peptide-1/glucagon (GLP …

Low kidney uptake of GLP-1R-targeting, beta cell-specific PET tracer, 18F-labeled [Nle14,Lys40]exendin-4 analog, shows promise for clinical imaging

K Mikkola, CB Yim, P Lehtiniemi, S Kauhanen… - EJNMMI research, 2016 - Springer
Background Several radiometal-labeled, exendin-based tracers that target glucagon-like
peptide-1 receptors (GLP-1R) have been intensively explored for β cell imaging. The main …

Evaluation of Cu-64 and Ga-68 radiolabeled glucagon-like peptide-1 receptor agonists as PET tracers for pancreatic β cell imaging

N Bandara, A Zheleznyak, K Cherukuri… - Molecular imaging and …, 2016 - Springer
Abstract Purpose Copper-64 (Cu-64) and Galium-68 (Ga-68) radiolabeled DO3A and NODA
conjugates of exendin-4 were used for preclinical imaging of pancreatic β cells via targeting …

In vivo imaging of the glucagonlike peptide 1 receptor in the pancreas with 68Ga-labeled DO3A-exendin-4

RK Selvaraju, I Velikyan, L Johansson… - Journal of Nuclear …, 2013 - Soc Nuclear Med
The glucagonlike peptide 1 receptor (GLP-1R) is mainly expressed on β-cells in the islets of
Langerhans and is therefore an attractive target for imaging of the β-cell mass. In the present …

Sulfonation of Tyrosine as a Method To Improve Biodistribution of Peptide-Based Radiotracers: Novel 18F-Labeled Cyclic RGD Analogues

MB Haskali, D Denoyer, W Noonan… - Molecular …, 2017 - ACS Publications
Control of the biodistribution of radiolabeled peptides has proven to be a major challenge in
their application as imaging agents for positron emission tomography (PET). Modification of …

Assessment of glucagon receptor occupancy by Positron Emission Tomography in non-human primates

O Eriksson, I Velikyan, T Haack, M Bossart, A Evers… - Scientific Reports, 2019 - nature.com
The glucagon receptor (GCGR) is an emerging target in anti-diabetic therapy. Reliable
biomarkers for in vivo activity on the GCGR, in the setting of dual glucagon-like peptide …