Design and Synthesis of Conformationally Constrained Cyclophilin Inhibitors Showing a Cyclosporin-A Phenotype in C. elegans

Cyclophilin A (CypA) is a member of the immunophilin family of proteins and receptor for the immunosuppressant drug cyclosporin A (CsA). Here we describe the design and synthesis of a new class of small‐molecule inhibitors for CypA that are based upon a dimedone template. Electrospray mass spectrome...

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Veröffentlicht in:	Chembiochem : a European journal of chemical biology 2011-03, Vol.12 (5), p.802-810
Hauptverfasser:	Dunsmore , Colin J., Malone , Kirk J., Bailey , Kevin R., Wear, Martin A., Florance, Hannah, Shirran , Sally, Barran, Perdita E., Page, Antony P., Walkinshaw, Malcolm D., Turner , Nicholas J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Caenorhabditis elegans - drug effects Caenorhabditis elegans - metabolism Caenorhabditis elegans Proteins - antagonists & inhibitors Caenorhabditis elegans Proteins - metabolism Cyclophilin A - antagonists & inhibitors Cyclophilin A - metabolism Cyclosporine Drug Design enzyme inhibitors Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology fluorescent probes Ligands mass spectrometry medicinal chemistry Models, Molecular Protein Binding Small Molecule Libraries - chemistry Small Molecule Libraries - pharmacology Spectrometry, Mass, Electrospray Ionization
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