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Literature DB >> 17004728

Design, synthesis, and incorporation of a beta-turn mimetic in angiotensin II forming novel pseudopeptides with affinity for AT1 and AT2 receptors.

Ulrika Rosenström¹, Christian Sköld, Gunnar Lindeberg, Milad Botros, Fred Nyberg, Anders Karlén, Anders Hallberg.

Abstract

A benzodiazepine-based beta-turn mimetic has been designed, synthesized, and incorporated into angiotensin II. Comparison of the mimetic with beta-turns in crystallized proteins showed that it most closely resembles a type II beta-turn. The compounds exhibited high to moderate binding affinity for the AT2 receptor, and one also displayed high affinity for the AT1 receptor. Molecular modeling showed that the high-affinity compounds could be incorporated into a previously derived model of AT2 receptor ligands.

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Year: 2006 PMID： 17004728 DOI： 10.1021/jm051222g

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

9 in total

Design, synthesis, and incorporation of a beta-turn mimetic in angiotensin II forming novel pseudopeptides with affinity for AT1 and AT2 receptors.

1. Design of RNA-targeting macrocyclic peptides.

Review 2. Classification of scaffold-hopping approaches.

3. 1,4-Thienodiazepine-2,5-diones via MCR (II): scaffold hopping by Gewald and Ugi-deprotection-cyclization strategy.

Review 4. The Angiotensin AT₂ Receptor: From a Binding Site to a Novel Therapeutic Target.

Review 5. Privileged diazepine compounds and their emergence as bromodomain inhibitors.

6. Synthesis of a novel fused pyrrolodiazepine-based library with anti-cancer activity.

Review 7. Structure-Based Design of Inhibitors of Protein-Protein Interactions: Mimicking Peptide Binding Epitopes.

Review 8. Isocyanide-based multicomponent reactions towards cyclic constrained peptidomimetics.

9. N-Aryl Isoleucine Derivatives as Angiotensin II AT2 Receptor Ligands.

Design, synthesis, and incorporation of a beta-turn mimetic in angiotensin II forming novel pseudopeptides with affinity for AT1 and AT2 receptors.

1. Design of RNA-targeting macrocyclic peptides.

Review 2. Classification of scaffold-hopping approaches.

3. 1,4-Thienodiazepine-2,5-diones via MCR (II): scaffold hopping by Gewald and Ugi-deprotection-cyclization strategy.

Review 4. The Angiotensin AT2 Receptor: From a Binding Site to a Novel Therapeutic Target.

Review 5. Privileged diazepine compounds and their emergence as bromodomain inhibitors.

6. Synthesis of a novel fused pyrrolodiazepine-based library with anti-cancer activity.

Review 7. Structure-Based Design of Inhibitors of Protein-Protein Interactions: Mimicking Peptide Binding Epitopes.

Review 8. Isocyanide-based multicomponent reactions towards cyclic constrained peptidomimetics.

9. N-Aryl Isoleucine Derivatives as Angiotensin II AT2 Receptor Ligands.

Review 4. The Angiotensin AT₂ Receptor: From a Binding Site to a Novel Therapeutic Target.