Conformationally homogeneous heterocyclic pseudotetrapeptides as three-dimensional scaffolds for rational drug design: Receptor-selective somatostatin analogues
| Authors |
|
|---|---|
| Publication date | 2009 |
| Journal | Angewandte Chemie, International Edition |
| Volume | Issue number | 48 | 26 |
| Pages (from-to) | 4725-4729 |
| Organisations |
|
| Abstract | A would-be amide: A 1,4-disubstituted 1,2,3-triazole was used as a surrogate for a trans amide bond to create a library of 16 diastereomeric pseudotetrapeptides as beta-turn mimetics. High-resolution structural analysis indicated that these scaffolds adopt distinct, rigid, conformationally homogeneous beta-turn-like structures (see example), some of which bind somatostatin receptor subtypes selectively, and some of which show broad-spectrum activity. |
| Document type | Article |
| Published at | https://doi.org/10.1002/anie.200805901 |
| Permalink to this page | |