Therapeutic potential of β-arrestin-and G protein-biased agonists

EJ Whalen, S Rajagopal, RJ Lefkowitz - Trends in molecular medicine, 2011 - cell.com
Members of the seven-transmembrane receptor (7TMR), or G protein-coupled receptor
(GPCR), superfamily represent some of the most successful targets of modern drug therapy …

International Union of Basic and Clinical Pharmacology. CV. Somatostatin receptors: structure, function, ligands, and new nomenclature

T Günther, G Tulipano, P Dournaud, C Bousquet… - Pharmacological …, 2018 - ASPET
Somatostatin, also known as somatotropin-release inhibitory factor, is a cyclopeptide that
exerts potent inhibitory actions on hormone secretion and neuronal excitability. Its …

Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery

T Kenakin, LJ Miller - Pharmacological reviews, 2010 - ASPET
It is useful to consider seven transmembrane receptors (7TMRs) as disordered proteins able
to allosterically respond to a number of binding partners. Considering 7TMRs as allosteric …

Radiolabeled somatostatin receptor antagonists are preferable to agonists for in vivo peptide receptor targeting of tumors

M Ginj, H Zhang, B Waser, R Cescato… - Proceedings of the …, 2006 - National Acad Sciences
Targeting neuroendocrine tumors expressing somatostatin receptor subtypes (sst) with
radiolabeled somatostatin agonists is an established diagnostic and therapeutic approach in …

Are radiogallium-labelled DOTA-conjugated somatostatin analogues superior to those labelled with other radiometals?

P Antunes, M Ginj, H Zhang, B Waser, RP Baum… - European journal of …, 2007 - Springer
Purpose Gallium-68 is a metallic positron emitter with a half-life of 68 min that is ideal for the
in vivo use of small molecules, such as [68 Ga-DOTA, Tyr 3] octreotide, in the diagnostic …

[HTML][HTML] Overview of radiolabeled somatostatin analogs for cancer imaging and therapy

R Eychenne, C Bouvry, M Bourgeois, P Loyer… - Molecules, 2020 - mdpi.com
Identified in 1973, somatostatin (SST) is a cyclic hormone peptide with a short biological half-
life. Somatostatin receptors (SSTRs) are widely expressed in the whole body, with five …

PET tracers for somatostatin receptor imaging of neuroendocrine tumors: current status and review of the literature

CB Johnbeck, U Knigge, A Kjær - Future oncology, 2014 - Future Medicine
Neuroendocrine tumors have shown rising incidence mainly due to higher clinical
awareness and better diagnostic tools over the last 30 years. Functional imaging of …

PET of somatostatin receptor–positive tumors using 64Cu-and 68Ga-somatostatin antagonists: the chelate makes the difference

M Fani, L Del Pozzo, K Abiraj, R Mansi… - Journal of nuclear …, 2011 - Soc Nuclear Med
Somatostatin-based radiolabeled peptides have been successfully introduced into the clinic
for targeted imaging and radionuclide therapy of somatostatin receptor (sst)–positive tumors …

Bombesin receptor antagonists may be preferable to agonists for tumor targeting

R Cescato, T Maina, B Nock… - Journal of Nuclear …, 2008 - Soc Nuclear Med
Two bombesin analogs, Demobesin 4 and Demobesin 1, were characterized in vitro as
gastrin-releasing peptide (GRP) receptor agonist and antagonist, respectively, and were …

Peptide-based probes for cancer imaging

JC Reubi, HR Maecke - Journal of nuclear medicine, 2008 - Soc Nuclear Med
Receptors for regulatory peptides are overexpressed in a variety of human cancers. They
represent the molecular basis for in vivo imaging with radiolabeled peptide probes …