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

Basic Information

ID: ALA1145409

Journal: J Med Chem

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

Authors: Feytens D, Cescato R, Reubi JC, Tourwé D.

Abstract: 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.

CiteXplore: 17559206

DOI: 10.1021/jm070246f

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