Arzneimittelforschung 1999; 49(10): 873-877
DOI: 10.1055/s-0031-1300519
Originalarbeit
Editio Cantor Verlag Aulendorf (Germany)

Conformational Aspects of Human Formylpeptide Receptor Antagonists

Angelo Scatturin
a  Department of Pharmaceutical Sciences, Ferrara University, Ferrara, Italy
,
Vertuani Gianni
a  Department of Pharmaceutical Sciences, Ferrara University, Ferrara, Italy
,
Rita Pecoraro
a  Department of Pharmaceutical Sciences, Ferrara University, Ferrara, Italy
,
Alessandro Dalpiaz
a  Department of Pharmaceutical Sciences, Ferrara University, Ferrara, Italy
,
Marisa Boggian
a  Department of Pharmaceutical Sciences, Ferrara University, Ferrara, Italy
,
Maria Enrica Ferretti
b  Department of Biology, Ferrara University, Ferrara, Italy
,
Susanna Spisani
c  Department of Biochemistry and Molecular Biology, Ferrara University, Ferrara, Italy
› Author Affiliations
Further Information

Publication History

Publication Date:
28 December 2011 (online)

Summary

The conformation of several Phe-D-Leu-Phe-D-Leu-Phe analogues was analyzed using infrared absorption and circular dichroism. Their effect on human neutrophils was verified by receptor binding and chemotaxis assays. The results demonstrate that the compounds examined prefer an ordered conformation (β-turn) in amphipatic environment, and that they are able to antagonize the neutrophil functions evoked by CHO-Met-Leu-Phe.

Zusammenfassung

Konformationsstudien mit humanen Formylpeptidrezeptor-Antagonisten

Die Konformation einiger Phe-D-Leu-Phe-D-Leu-Phe-Analoga wurde mit Infrarotabsorption und Zirkulardichroismus-Spektrometrie analysiert. Ihre Wirkung auf menschliche Neutrophile wurde mittels Rezeptorbindungsaffinitätund Chemotaxis-Tests überprüft. Die Resultate zeigen, daß die untersuchten Verbindungen eine wohlgeordnete Konformation (β-turn) in amphoterischer Umgebung bevorzugen und die durch CHO-Met-Leu-Phe induzierten Neutrophilfunktionen hemmen können.