Peptides with 6-Aminohexanoic Acid: Synthesis and Evaluation as Plasmin Inhibitors |
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Authors: | Maciej Purwin Agnieszka Markowska Irena Bruzgo Tomasz Rusak Arkadiusz Sura?yński Urszula Jaworowska Krystyna Midura-Nowaczek |
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Institution: | 1.Department of Organic Chemistry,Medical University of Bialystok,Bia?ystok,Poland;2.Department of Physical Chemistry,Medical University of Bialystok,Bia?ystok,Poland;3.Department of Medicinal Chemistry,Medical University of Bialystok,Bia?ystok,Poland |
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Abstract: | Fifteen new peptide derivatives of ?-aminocaproic acid (EACA) containing the known fragment –Ala–Phe–Lys– with an affinity for plasmin were synthesised in the present study. The synthesis was carried out a solid phase. The following compounds were synthesised: H–Phe–Lys–EACA–X, H–d-Ala–Phe–Lys–EACA–X, H–Ala–Phe–Lys–EACA–X, H–d-Ala–Phe–EACA–X and H–Ala–Phe–EACA–X, where X = OH, NH2 and NH–(CH2)5–NH2. All peptides, except for those containing the sequence H–Ala–Phe–EACA–X, displayed higher inhibitory activity against plasmin than EACA. The most active and selective inhibitor of plasmin was the compound H–d-Ala–Phe–Lys–EACA–NH2 which inhibited the amidolytic activity of plasmin (IC50 = 0.02 mM), with the antifibrinolytic activity weaker than EACA. The resulting peptides did not affect the viability of fibroblast cells, colon cancer cell line DLD-1, breast MCF-7 and MDA-MB-231 cell lines. |
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