Branches on the α-C Atom of Cyclosporin A Residue 3 Result in Direct Calcineurin Inhibition and Rapid Cyclophilin 18 Binding

✍ Scribed by Yixin Zhang; Ria Raumgrass; Mike Schutkowski; Gunter Fischer

• Publisher: John Wiley and Sons
• Year: 2004
• Tongue: English
• Weight: 119 KB
• Volume: 5
• Category: Article
• ISSN: 1439-4227
• DOI: 10.1002/cbic.200400020

✦ Synopsis

It no longer takes two. We report on cyclosporin A (CsA) derivatives that inhibit calcineurin protein phosphatase activity without first forming a binary complex with cyclophilin 18. Furthermore, these derivatives are rapid binding inhibitors for cyclophilin 18, whereas CsA is a slow binding inhibitor.