ArticleJournal of medicinal chemistry2009
Novel, potent, and radio-iodinatable somatostatin receptor 1 (sst1) selective analogues.
Article in Journal of medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 36 citations in OpenAlex.
- The role of brain somatostatin receptor 2 in the regulation of feeding and drinking behavior.Hormones and behavior · 2015Review
- Article
- Brain somatostatin receptor 2 mediates the dipsogenic effect of central somatostatin and cortistatin in rats: role in drinking behavior.American journal of physiology. Regulatory, integrative and comparative physiology · 2014Article
- Insights into structure-activity relationships of somatostatin analogs containing mesitylalanine.Molecules (Basel, Switzerland) · 2013Article
- Modulation of the adaptive response to stress by brain activation of selective somatostatin receptor subtypes.Peptides · 2013Review
- Discovery of new antagonists aimed at discriminating UII and URP-mediated biological activities: insight into UII and URP receptor activation.British journal of pharmacology · 2013Article
- [111In-DOTA]Somatostatin-14 analogs as potential pansomatostatin-like radiotracers - first results of a preclinical study.EJNMMI research · 2012Article
- Activation of somatostatin 2 receptors in the brain and the periphery induces opposite changes in circulating ghrelin levels: functional implications.Frontiers in endocrinology · 2012Article
- Novel dimeric DOTA-coupled peptidic Y1-receptor antagonists for targeting of neuropeptide Y receptor-expressing cancers.EJNMMI research · 2011Article
- Central administration of pan-somatostatin agonist ODT8-SST prevents abdominal surgery-induced inhibition of circulating ghrelin, food intake and gastric emptying in rats.Neurogastroenterology and motility · 2011Article
- Central somatostatin receptor 1 activation reverses acute stress-related alterations of gastric and colonic motor function in mice.Neurogastroenterology and motility · 2011Article
- Activation of brain somatostatin 2 receptors stimulates feeding in mice: analysis of food intake microstructure.Physiology & behavior · 2010Article
- Article
- Switch from antagonist to agonist after addition of a DOTA chelator to a somatostatin analog.European journal of nuclear medicine and molecular imaging · 2010Article
- Three-dimensional consensus structure of sst2-selective somatostatin (SRIF) antagonists by NMR.Biopolymers · 2008Article
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 2 countries.
Funding
Abstract
The proposed sst(1) pharmacophore (J. Med. Chem. 2005, 48, 523-533) derived from the NMR structures of a family of mono- and dicyclic undecamers was used to design octa-, hepta-, and hexamers with high affinity and selectivity for the somatostatin sst(1) receptor. These compounds were tested for their in vitro binding properties to all five somatostatin (SRIF) receptors using receptor autoradiography; those with high SRIF receptor subtype 1 (sst(1)) affinity and selectivity were shown to be agonists when tested functionally in a luciferase reporter gene assay. Des-AA(1,4-6,10,12,13)-[DTyr(2),DAgl(NMe,2naphthoyl)(8),IAmp(9)]-SRIF-Thr-NH(2) (25) was radio-iodinated ((125)I-25) and specifically labeled sst(1)-expressing cells and tissues. 3D NMR structures were calculated for des-AA(1,4-6,10,12,13)-[DPhe(2),DTrp(8),IAmp(9)]-SRIF-Thr-NH(2) (16), des-AA(1,2,4-6,10,12,13)-[DAgl(NMe,2naphthoyl)(8),IAmp(9)]-SRIF-Thr-NH(2) (23), and des-AA(1,2,4-6,10,12,13)-[DAgl(NMe,2naphthoyl)(8),IAmp(9),Tyr(11)]-SRIF-NH(2) (27) in DMSO. Though the analogues have the sst(1) pharmacophore residues at the previously determined distances from each other, the positioning of the aromatic residues in 16, 23, and 27 is different from that described earlier, suggesting an induced fit mechanism for sst(1) binding of these novel, less constrained sst(1)-selective family members.
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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.