ArticleJournal of medicinal chemistry2008
Ring size in octreotide amide modulates differently agonist versus antagonist binding affinity and selectivity.
Article in Journal of medicinal chemistry, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
12 citing papers in PubMed, 24 citations in OpenAlex.
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- Theranostic system for ratiometric fluorescence monitoring of peptide-guided targeted drug delivery.RSC advances · 2019Article
- Peptide-based imaging agents for cancer detection.Advanced drug delivery reviews · 2017Review
- Activation of Brain Somatostatin Signaling Suppresses CRF Receptor-Mediated Stress Response.Frontiers in neuroscience · 2017Review
- 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
- Prospective of ⁶⁸Ga-radiopharmaceutical development.Theranostics · 2013Review
- Modulation of the adaptive response to stress by brain activation of selective somatostatin receptor subtypes.Peptides · 2013Review
- [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
- Central somatostatin receptor 1 activation reverses acute stress-related alterations of gastric and colonic motor function in mice.Neurogastroenterology and motility · 2011Article
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
Abstract
H-DPhe (2)-c[Cys (3)-Phe (7)-DTrp (8)-Lys (9)-Thr (10)-Cys (14)]-Thr (15)-NH2 (1) (a somatostatin agonist, SRIF numbering) and H-Cpa (2)-c[DCys (3)-Tyr (7)-DTrp (8)-Lys (9)-Thr (10)-Cys (14)]-Nal (15)-NH2 (4) (a somatostatin antagonist) are based on the structure of octreotide that binds to three somatostatin receptor subtypes (sst 2/3/5) with significant binding affinity. Analogues of 1 and 4 were synthesized with norcysteine (Ncy), homocysteine (Hcy), or D-homocysteine (DHcy) at positions 3 and/or 14. Introducing Ncy at positions 3 and 14 constrained the backbone flexibility, resulting in loss of binding affinity at all sst s. The introduction of Hcy at positions 3 and 14 improved selectivity for sst 2 as a result of significant loss of binding affinity at the other sst s. Substitution by DHcy at position 3 in the antagonist scaffold (5), on the other hand, resulted in a significant loss of binding affinity at sst 2 and sst 3 as compared to the different affinities of the parent compound (4). The 3D NMR structures of the analogues in dimethylsulfoxide are consistent with the observed binding affinities.
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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.