Three-dimensional consensus structure of sst2-selective somatostatin (SRIF) antagonists by NMR

Grace, Christy Rani R; Erchegyi, Judit; Reubi, Jean Claude; Rivier, Jean E; Riek, Roland (2008). Three-dimensional consensus structure of sst2-selective somatostatin (SRIF) antagonists by NMR. Biopolymers, 89(12), pp. 1077-87. Hoboken, N.J.: John Wiley & Sons, Inc. 10.1002/bip.21060

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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.

Item Type:	Journal Article (Original Article)
Division/Institute:	04 Faculty of Medicine > Service Sector > Institute of Pathology
UniBE Contributor:	Reubi-Kattenbusch, Jean-Claude
Subjects:	500 Science > 570 Life sciences; biology 600 Technology > 610 Medicine & health
ISSN:	0006-3525
ISBN:	18655144
Publisher:	John Wiley & Sons, Inc.
Language:	English
Submitter:	Factscience Import
Date Deposited:	04 Oct 2013 15:02
Last Modified:	05 Dec 2022 14:19
Publisher DOI:	10.1002/bip.21060
PubMed ID:	18655144
Web of Science ID:	000260403600004
URI:	https://boris.unibe.ch/id/eprint/27060 (FactScience: 101616)