ArticleBiopolymers2008
Three-dimensional consensus structure of sst2-selective somatostatin (SRIF) antagonists by NMR.
Article in Biopolymers, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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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
5 citing papers in PubMed.
- The Structural Basis of Peptide Binding at Class A G Protein-Coupled Receptors.Molecules (Basel, Switzerland) · 2021Review
- DOTA-Derivatives of Octreotide Dicarba-Analogs with High Affinity for Somatostatin sstFrontiers in chemistry · 2017Article
- Prospective of ⁶⁸Ga-radiopharmaceutical development.Theranostics · 2013Review
- Novel, potent, and radio-iodinatable somatostatin receptor 1 (sst1) selective analogues.Journal of medicinal chemistry · 2009Article
- Ring size in octreotide amide modulates differently agonist versus antagonist binding affinity and selectivity.Journal of medicinal chemistry · 2008Article
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
The three-dimensional NMR structures of seven octapeptide analogs of somatostatin (SRIF), based on octreotide, with the basic sequence H-Cpa/Phe2-c[DCys3-Xxx7-DTrp/DAph(Cbm)8-Lys9-Thr10-Cys14]-Yyy-NH2 (the numbering refers to the position in native SRIF), with Xxx7 being Aph(Cbm)/Tyr/Agl(NMe,benzoyl) and Yyy being Nal/DTyr/Thr, are presented here. Most of these analogs exhibit potent and highly selective binding to sst2 receptors, and all of the analogs are antagonists inhibiting receptor signaling. Based on their consensus 3D structure, the pharmacophore of the sst2-selective antagonist has been defined. The pharmacophore involves the side chains of Cpa2, DTrp/DAph(Cbm)8, and Lys9, with the backbone for most of the sst2-selective antagonists comprised a Type-II' beta-turn. Hence, the sst2-selective antagonist pharmacophore is very similar to the sst2-selective agonist pharmacophore previously described.
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Registered trials
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