title: Fine tuning the inhibition profile of cyclosporine A by derivatization of the MeBmt residue.
abstract: Unique respect: The biological properties of four CsA derivatives were fine-tuned by tractable modifications of the MeBmt residue. The new CsA derivatives share strong inhibitory activity toward cyclophilins (Cyps), but each is unique with respect to immunosuppressive action and cellular localization. These CsA analogues can be used to study the physiological roles of extracellular Cyps.
authors.affiliation: Max Planck Research Unit for Enzymology of Protein Folding, Weinbergweg 22, 06120 Halle/Saale, Germany.
authors.forename: Erik
authors.initials: E
authors.lastname: Prell
authors.forename: Viktoria
authors.initials: V
authors.lastname: Kahlert
authors.forename: Karl Peter
authors.initials: KP
authors.lastname: Rücknagel
authors.forename: Miroslav
authors.initials: M
authors.lastname: Malešević
authors.forename: Gunter
authors.initials: G
authors.lastname: Fischer
mesh_terms: D001692:Biological Transport; D065095:Calcineurin Inhibitors; D021983:Cyclophilins / Q000037:antagonists & inhibitors; D016572:Cyclosporine / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D005110:Extracellular Space / Q000378:metabolism; D006801:Humans; D042541:Intracellular Space / Q000378:metabolism; D019169:Jurkat Cells; D013329:Structure-Activity Relationship; D013912:Threonine / Q000031:analogs & derivatives* / Q000737:chemistry*
chemical_list: D065095:Calcineurin Inhibitors; D004791:Enzyme Inhibitors; D013912:Threonine; D016572:Cyclosporine; D021983:Cyclophilins