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      Peptides with 6-Aminohexanoic Acid: Synthesis and Evaluation as Plasmin Inhibitors

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          Abstract

          Fifteen new peptide derivatives of ɛ-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, NH 2 and NH–(CH 2) 5–NH 2. 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–NH 2 which inhibited the amidolytic activity of plasmin (IC 50 = 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 DL D-1, breast MCF-7 and MDA-MB-231 cell lines.

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          Most cited references 59

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          Thrombelastography/thromboelastometry.

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          The term thrombelastograph (TEG) was used to describe the trace produced from the measurement of the viscoelastic changes associated with fibrin polymerization. Recently the term rotational thromboelastometry has been applied to the output of the ROTEM instrument. Since its first description in 1948, the TEG/ROTEM has been successfully used in the near patient assessment of haemostasis. The greatest use has been the application of TEG-guided transfusion of blood components in hepatic and more widely in cardiac surgery. Recent years have seen a renewed interest in the technology with applications for both pharmaceutical monitoring and patient screening being described. The present review gives a broad overview of the developments and applications related to thrombelastography/thromboelastometry.
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            The plasminogen activator/plasmin system.

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              Effects of the pH dependence of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide-formazan absorption on chemosensitivity determined by a novel tetrazolium-based assay.

              The tetrazolium dye, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), is reduced by live but not dead cells, and this reaction is used as the end point in a rapid drug-screening assay. It can also be used for accurate determinations of drug sensitivity but only if a quantitative relationship is established between cell number and MTT-formazan production. We have shown that reduction of MTT to MTT-formazan by cells is dependent on the amount of MTT in the incubation medium. The concentration required to give maximal MTT-formazan production differs widely between cell lines. The absorption spectrum of MTT-formazan varies with cell number and with pH. At a low cell density or a high pH, the absorption maximum is at a wavelength of 560 to 570 nm. However, at a high cell density or a low pH, there are two absorption maxima; one at 510 nm and a second at about 570 nm. Measurements of absorbance at 570 nm underestimate MTT-formazan production and, hence, cell number at high cell densities. This error can result in a 10-fold underestimation of chemosensitivity. Addition of a buffer at pH 10.5 to the solubilized MTT-formazan product can overcome the effects of both cell density and culture medium on the absorption spectrum. Provided that sufficient MTT is used and the pH of the MTT-formazan product is controlled, dye reduction can be used to estimate cell numbers in a simple chemosensitivity assay the results of which agree well with a commonly used clonogenic assay.
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                Author and article information

                Contributors
                agnieszka.markowska@umb.edu.pl
                Journal
                Int J Pept Res Ther
                Int J Pept Res Ther
                International Journal of Peptide Research and Therapeutics
                Springer Netherlands (Dordrecht )
                1573-3149
                1573-3904
                19 September 2016
                19 September 2016
                2017
                : 23
                : 2
                : 235-245
                Affiliations
                [1 ]ISNI 0000000122482838, GRID grid.48324.39, Department of Organic Chemistry, , Medical University of Bialystok, ; Mickiewicza 2A Str, 15-222 Białystok, Poland
                [2 ]ISNI 0000000122482838, GRID grid.48324.39, Department of Physical Chemistry, , Medical University of Bialystok, ; Mickiewicza 2A Str, 15-222 Białystok, Poland
                [3 ]ISNI 0000000122482838, GRID grid.48324.39, Department of Medicinal Chemistry, , Medical University of Bialystok, ; Mickiewicza 2A Str, 15-222 Białystok, Poland
                Article
                9555
                10.1007/s10989-016-9555-3
                5401710
                © The Author(s) 2016

                Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License ( http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made.

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                © Springer Science+Business Media New York 2017

                Biochemistry

                antifibrinolytics, 6-aminohexanoic acid, plasmin inhibitors

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