Feytens, Debby; De Vlaeminck, Magali; Cescato, Renzo; Tourwé, Dirk; Reubi, Jean-Claude (2009). Highly potent 4-amino-indolo[2,3-c]azepin-3-one-containing somatostatin mimetics with a range of sst receptor selectivities. Journal of medicinal chemistry, 52(1), pp. 95-104. Easton, Pa.: American Chemical Society 10.1021/jm801205x
Full text not available from this repository. (Request a copy)The synthesis, biological evaluation, and conformational analysis of 4-amino-indolo[2,3-c]azepin-3-one (Aia)-containing SRIF mimetics are reported. Different subtype selectivities are observed depending on the N- and C-terminal substituents of the D-Aia-Lys dipeptide mimetic. An sst(5)-selective analogue with subnanomolar binding affinity was obtained that is the most potent agonist reported to date. A nonselective mimetic with high potency was also identified. This study allows a better definition of the bioactive conformation of the essential D-Trp side chain in the somatostatin pharmacophore.
Item Type: |
Journal Article (Original Article) |
|---|---|
Division/Institute: |
04 Faculty of Medicine > Service Sector > Institute of Pathology |
UniBE Contributor: |
Cescato, Renzo, Reubi-Kattenbusch, Jean-Claude |
Subjects: |
500 Science > 570 Life sciences; biology 600 Technology > 610 Medicine & health |
ISSN: |
0022-2623 |
ISBN: |
19067538 |
Publisher: |
American Chemical Society |
Language: |
English |
Submitter: |
Factscience Import |
Date Deposited: |
04 Oct 2013 15:08 |
Last Modified: |
05 Dec 2022 14:21 |
Publisher DOI: |
10.1021/jm801205x |
PubMed ID: |
19067538 |
Web of Science ID: |
000262171500011 |
URI: |
https://boris.unibe.ch/id/eprint/29979 (FactScience: 165578) |
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