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Trimesinsäureamid dient als Gerüst für den lipophilen Cyclophilininhibitor 1 mit einem Rhodamin‐Fluoreszenzfarbstoff (TAMRA) und einem (D‐Glu)6‐Oligopeptidrest. Während die Affinität von 1 zu intrazellulärem Cyclophilin A sehr hoch ist, wiesen Fluoreszenzmessungen darauf hin, dass es nicht in Zellen einzudringen vermag. Die CypA‐induzierte Chemotaxis von Lymphozyten wird durch 1 gehemmt, weil extrazelluläre...
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...
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