ArticleProceedings of the National Academy of Sciences of the United States of America2000
SST3-selective potent peptidic somatostatin receptor antagonists.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 100 citations in OpenAlex.
- Somatostatin receptors shape insulin and glucagon output within the pancreatic islet in mice through direct and paracrine effects.Diabetologia · 2026Article
- Somatostatin Receptors Shape Insulin and Glucagon Output within the Pancreatic Islet through Direct and Paracrine Effects.bioRxiv : the preprint server for biology · 2025Article
- Prediction of lesion-based response to PRRT using baseline somatostatin receptor PET.Frontiers in medicine · 2025Article
- The Importance of Intra-Islet Communication in the Function and Plasticity of the Islets of Langerhans during Health and Diabetes.International journal of molecular sciences · 2024Review
- Alpha-peptide receptor radionuclide therapy using actinium-225 labeled somatostatin receptor agonists and antagonists.Frontiers in medicine · 2022Review
- Stereo- and regiodefined DNA-encoded chemical libraries enable efficient tumour-targeting applications.Nature chemistry · 2021Article
- δ-Cells: The Neighborhood Watch in the Islet Community.Biology · 2021Review
- The Difference δ-Cells Make in Glucose Control.Physiology (Bethesda, Md.) · 2018Review
- International Union of Basic and Clinical Pharmacology. CV. Somatostatin Receptors: Structure, Function, Ligands, and New Nomenclature.Pharmacological reviews · 2018Review
- Clinical and functional implication of the components of somatostatin system in gastroenteropancreatic neuroendocrine tumors.Endocrine · 2018Article
- Current Status of Radiopharmaceuticals for the Theranostics of Neuroendocrine Neoplasms.Pharmaceuticals (Basel, Switzerland) · 2017Review
- Comprehensive alpha, beta and delta cell transcriptomes reveal that ghrelin selectively activates delta cells and promotes somatostatin release from pancreatic islets.Molecular metabolism · 2016Article
- Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion.Nature medicine · 2015Article
- Novel dimeric DOTA-coupled peptidic Y1-receptor antagonists for targeting of neuropeptide Y receptor-expressing cancers.EJNMMI research · 2011Article
- Novel, potent, and radio-iodinatable somatostatin receptor 1 (sst1) selective analogues.Journal of medicinal chemistry · 2009Article
- Three-dimensional consensus structure of sst2-selective somatostatin (SRIF) antagonists by NMR.Biopolymers · 2008Article
- Design and in vitro characterization of highly sst2-selective somatostatin antagonists suitable for radiotargeting.Journal of medicinal chemistry · 2008Article
- Ring size of somatostatin analogues (ODT-8) modulates receptor selectivity and binding affinity.Journal of medicinal chemistry · 2008Article
- Structure-activity relationship studies of gonadotropin-releasing hormone antagonists containing S-aryl/alkyl norcysteines and their oxidized derivatives.Journal of medicinal chemistry · 2007Article
- Radiolabeled somatostatin receptor antagonists are preferable to agonists for in vivo peptide receptor targeting of tumors.Proceedings of the National Academy of Sciences of the United States of America · 2006Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
A family of octapeptide derivatives of somatostatin cyclized via a disulfide bridge (des-AA(1,2,4,5,12,13)[d-2Nal(8)]-somatostatin-14, ODN-8) was identified that has high affinity and selectivity for the human sst(3) somatostatin receptor subtype transfected in CCL39 cells. The binding affinity of carbamoyl-des-AA(1,2,4,5,12, 13)[d-Cys(3),Tyr(7),d-Agl(8)(Me,2-naphthoyl)]-somatostatin-14 (sst(3)-ODN-8) is equal to that of somatostatin-28 for sst(3) and less than one-thousandth that for the other four somatostatin receptor subtypes. Compound sst(3)-ODN-8 potently reverses the somatostatin-28-induced inhibition of forskolin-stimulated cAMP production (pK(B) = 9.07) and reverses the somatostatin-28-induced stimulation of phospholipase C activity (pK(i) = 9.22) in sst(3)-transfected CCL39 cells. [(125)I-Tyr(7)]sst(3)-ODN-8 selectively labels sst(3)-expressing cells with subnanomolar binding affinity (K(D) = 0.27 nM). With the use of this radioligand, sst(3)-expressing human tumors, particularly inactive pituitary adenomas, can be identified with receptor autoradiography; moreover, areas of the human lymphoreticular system express sst(3) binding sites selectively displaced by nanomolar concentrations of sst(3)-ODN-8. Based on the structure-activity relationship of selected analogs substituted at positions 3, 7, and 8, we hypothesize that the basis for sst(3) selectivity, high affinity, and possibly antagonism resides in the ring size of the analog and the unique conformational and structural character of the N-methylated amino-2-naphthoyl side chain of aminoglycine at position 8 and not in the Tyr(7) substitution or in the d-configuration at position 3. The family of labeled and unlabeled sst(3)-ODN-8 analogs represents highly innovative, potent, and specific sst(3)-selective antagonist tools for the study of sst(3)-mediated physiological and pathophysiological conditions that may suggest novel clinical applications.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.