New sst4/5-selective somatostatin peptidomimetics based on a constrained tryptophan scaffold

Feytens, Debby; Cescato, Renzo; Reubi, Jean Claude; Tourwé, Dirk (2007). New sst4/5-selective somatostatin peptidomimetics based on a constrained tryptophan scaffold. Journal of medicinal chemistry, 50(14), pp. 3397-401. Easton, Pa.: American Chemical Society 10.1021/jm070246f

Full text not available from this repository. (Request a copy)

The synthesis and biological evaluation of four peptidomimetic analogs of somatostatin based on a constrained Trp residue, 3-amino-indolo[2,3-c]azepin-2-one (Aia), are reported. It is shown that dipeptidomimetics with a D-Aia-Lys sequence, functionalized with N- and C-terminal aromatic substituents, display a good selectivity for both sst4 and sst5. This study allowed us to identify a new highly potent sst5 agonist with good selectivity over the other receptors, except versus sst4.

Item Type:

Journal Article (Original Article)

Division/Institute:

04 Faculty of Medicine > Service Sector > Institute of Pathology

UniBE Contributor:

Cescato, Renzo and Reubi, Jean-Claude

ISSN:

0022-2623

ISBN:

17559206

Publisher:

American Chemical Society

Language:

English

Submitter:

Factscience Import

Date Deposited:

04 Oct 2013 14:54

Last Modified:

04 May 2014 23:15

Publisher DOI:

10.1021/jm070246f

PubMed ID:

17559206

Web of Science ID:

000247760400028

URI:

https://boris.unibe.ch/id/eprint/22745 (FactScience: 36407)

Actions (login required)

Edit item Edit item
Provide Feedback