ArticleThe Biochemical journal1998
Fates of endocytosed somatostatin sst2 receptors and associated agonists.
Article in The Biochemical journal, 1998. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 63 citations in OpenAlex.
- SSTR2 receptor states and cellular metabolism modulateEANM innovation · 2026Article
- Evolution of dosimetric parameters through PRRT and potential impact on clinical practice: data from the prospective phase II LUMEN study.EJNMMI research · 2024Article
- Impact of administered amount of peptide on tumor dosimetry at the first cycle of peptide receptor radionuclide therapy (PRRT) in relation to total tumor somatostatin receptor expression.EJNMMI research · 2023Article
- A Physiologically Based Pharmacokinetic Model for In Vivo Alpha Particle Generators Targeting Neuroendocrine Tumors in Mice.Pharmaceutics · 2021Article
- Distinct In Vitro Binding Profile of the Somatostatin Receptor Subtype 2 Antagonist [Pharmaceuticals (Basel, Switzerland) · 2021Article
- Receptor depletion and recovery in small-intestinal neuroendocrine tumors and normal tissues after administration of a single intravenous dose of octreotide measured byEJNMMI research · 2021Article
- Combination treatments to enhance peptide receptor radionuclide therapy of neuroendocrine tumours.European journal of nuclear medicine and molecular imaging · 2020Review
- Synthesis and preclinical investigation ofMolecular biology reports · 2019Article
- Preparation and biological evaluation of (64)Cu labeled Tyr(3)-octreotate using a phosphonic acid-based cross-bridged macrocyclic chelator.Bioconjugate chemistry · 2012Article
- G-protein coupled receptor resensitization-appreciating the balancing act of receptor function.Current molecular pharmacology · 2012Article
- Evaluation of copper-64-labeled somatostatin agonists and antagonist in SSTr2-transfected cell lines that are positive and negative for p53: implications for cancer therapy.Nuclear medicine and biology · 2012Article
- Magainin 2 in action: distinct modes of membrane permeabilization in living bacterial and mammalian cells.Biophysical journal · 2008Article
- Endothelin-converting enzyme-1 degrades internalized somatostatin-14.Endocrinology · 2008Article
- PET/CT with Gluc-Lys-([(18)F]FP)-TOCA: correlation between uptake, size and arterial perfusion in somatostatin receptor positive lesions.European journal of nuclear medicine and molecular imaging · 2008Article
- [123I]Mtr-TOCA, a radioiodinated and carbohydrated analogue of octreotide: scintigraphic comparison with [111In]octreotide.European journal of nuclear medicine and molecular imaging · 2006Article
- DOTA-NOC, a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5 for labelling with various radiometals.European journal of nuclear medicine and molecular imaging · 2003Article
- Non-invasive gamma camera imaging of gene transfer using an adenoviral vector encoding an epitope-tagged receptor as a reporter.Gene therapy · 2003Article
- Ligand internalization and recycling by human recombinant somatostatin type 4 (h sst(4)) receptors expressed in CHO-K1 cells.British journal of pharmacology · 2001Article
- Kinetic analysis of the internalization and recycling of [3H]TRH and C-terminal truncations of the long isoform of the rat thyrotropin-releasing hormone receptor-1.The Biochemical journal · 2000Article
- Somatostatin-induced control of cytosolic free calcium in pituitary tumour cells.British journal of pharmacology · 2000Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
Abstract
Somatostatin agonists are rapidly and efficiently internalized with the somatostatin sst2 receptor. The fate of internalized agonists and receptors is of critical importance because the rate of ligand recycling back to the cell surface can limit the amount of radioligand accumulated inside the cells, whereas receptor recycling might be of vital importance in providing the cell surface with dephosphorylated, resensitized receptors. Furthermore the accumulation of radioisotope-conjugated somatostatin agonists inside cancer cells resulting from receptor-mediated internalization has been used as a treatment for cancers that overexpress somatostatin receptors. In the present study, radio-iodinated agonists at the sst2 somatostatin receptor were employed to allow quantitative analysis of the fate of endocytosed agonist. After endocytosis, recycling back to the cell surface was the main pathway for both 125I-labelled somatostatin-14 (SRIF-14) and the more stable agonist 125I-labelled cyclo(N-Me-Ala-Tyr-d-Trp-Lys-Abu-Phe) (BIM-23027; Abu stands for aminobutyric acid), accounting for 75-85% of internalized ligand when re-endocytosis of radioligand was prevented. We have shown that there is a dynamic cycling of both somatostatin agonist ligands and receptors between the cell surface and internal compartments both during agonist treatment and after surface-bound agonist has been removed, unless steps are taken to prevent the re-activation of receptors by recycled agonist. Internalization leads to increased degradation of 125I-labelled SRIF-14 but not 125I-labelled BIM-23027. The concentration of recycled agonist accumulating in the extracellular medium was sufficient to re-activate the receptor, as measured both by the inhibition of forskolin-stimulated adenylate cyclase and the recovery of surface receptor number after internalization.
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Registered trials
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