A Cyclosporin Derivative Discriminates between Extracellular and Intracellular Cyclophilins | Zendy

Malešević Miroslav | Zendy; Kühling Jan | Zendy; Erdmann Frank | Zendy; Balsley Molly A. | Zendy; Bukrinsky Michael I. | Zendy; Constant Stephanie L. | Zendy; Fischer Gunter | Zendy

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A Cyclosporin Derivative Discriminates between Extracellular and Intracellular Cyclophilins

Author(s) -

Malešević Miroslav,

Kühling Jan,

Erdmann Frank,

Balsley Molly A.,

Bukrinsky Michael I.,

Constant Stephanie L.,

Fischer Gunter

Publication year - 2010

Publication title -

angewandte chemie international edition

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 5.831

H-Index - 550

eISSN - 1521-3773

pISSN - 1433-7851

DOI - 10.1002/anie.200904529

Subject(s) - cypa , cyclophilin a , cyclophilin , extracellular , intracellular , oligopeptide , chemistry , rhodamine , biochemistry , microbiology and biotechnology , fluorescence , biophysics , computational biology , biology , peptide , physics , quantum mechanics , gene

Trimesic acid amide serves as a scaffold for a lipophilic cyclophilin inhibitor, a fluorescent rhodamine dye (TAMRA), and a ( D ‐Glu) 6 oligopeptide residue. Although the affinity of 1 for intracellular cyclophilin A (CypA) is very high, fluorescence measurements indicate complete exclusion from the cell. CypA‐induced chemotaxis of lymphocytes is inhibited by 1 since extracellular cyclophilins are responsible for the physiological signal.

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