Cover Picture: A Cyclic CCK8 Analogue Selective for the Cholecystokinin Type A Receptor: Design, Synthesis, NMR Structure and Binding Measurements (ChemBioChem 11/2003)

✍ Scribed by Stefania De Luca; Raffaele Ragone; Chiara Bracco; Giuseppe Digilio; Luigi Aloj; Diego Tesauro; Michele Saviano; Carlo Pedone; Giancarlo Morelli

• Publisher: John Wiley and Sons
• Year: 2003
• Tongue: English
• Weight: 21 KB
• Volume: 4
• Category: Article
• ISSN: 1439-4227
• DOI: 10.1002/cbic.200390114

✦ Synopsis

Abstract

The cover picture shows a molecular model of the interaction between the new CCK8 analogue, Cycle29,34[Dpr29,Lys34]‐CCK8 (shown as a CPK model) and the receptor fragment CCK~A~‐R(1–47) (represented by a pink ribbon). The introduction of the cyclic constraint between the Dpr29 sidechain and the CCK8 C terminus (Lys34) decreases the flexibility of the molecule to stabilize the bioactive conformation of Cycle29,34[Dpr29,Lys34]‐CCK8. The Trp30 and Met31 side chains are in favorable orientations for interaction with the CCKA receptor. Expansions of the aromatic/amide regions of the ^1^H NMR spectra of Cycle29,34[Dpr29,Lys34]‐CCK8 in aqueous solution (top) and in presence of dodecylphosphocholine‐d~38~ micelles (bottom) are shown in the inset. Further details can be found in the article by Morelli and co‐workers on p. 1176 ff.