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Frank, S; Durovic, S; Kostner, K; Kostner, GM.
Inhibitors for the in vitro assembly of Lp(a).
Arterioscler Thromb Vasc Biol. 1995; 15(10):1774-1780 Doi: 10.1161/01.ATV.15.10.1774 [OPEN ACCESS]
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Leading authors Med Uni Graz: Frank Sasa; Kostner Gerhard
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Abstract:: Lp(a) is composed of an LDL-like core and the glycoprotein apo(a). Current evidence strongly suggests that the assembly of this atherogenic lipoprotein proceeds outside the liver cells in a two-step fashion. In the first step, a loose complex is formed involving kringle-4 motifs in apo(a) and one or more Lys side chains in apoB-100. In the second step, this complex is stabilized by a disulfide bridge. Indications are that Lp(a) assembly is critical in the determination of plasma apo(a) concentrations. Therefore, we searched for substances that interfere with the first step of Lp(a) assembly. epsilon-Aminohexoic acid (epsilon-AHA), known as an inhibitor from earlier assembly studies, had an IC50 of 4.8 mmol/L. The IC50 of Pro, HO-p-aminobenzene sulfonamide, Lys, N-epsilon-acetyl-Lys, taurine, Glu, serotonin, and benzamidine were all > 20 mmol/L. gamma-Aminobutyric acid, spermine, and spermidine exhibited IC50 on the same order of magnitude as epsilon-AHA. The substances with the highest inhibitory action were tranexamic acid and delta-aminovaleric acid. Seven of eight patients treated in a pilot study with tranexamic acid (Cyclocapron) responded with a decrease of plasma apo(a) of 18.5 +/- 8.2%. We suggest that substances that interfere with the Lp(a) assembly are worth pursuing further for their usefulness as therapeutic agents in reducing high plasma Lp(a) concentrations.
Find related publications in this database (using NLM MeSH Indexing): Adult -; Antifibrinolytic Agents - pharmacology; Base Sequence - pharmacology; Cell Line - pharmacology; Female - pharmacology; Humans - pharmacology; Lipoprotein(a) - antagonists and inhibitors; Male - antagonists and inhibitors; Middle Aged - antagonists and inhibitors; Molecular Sequence Data - antagonists and inhibitors; Recombinant Proteins - antagonists and inhibitors; Tranexamic Acid - pharmacology
Find related publications in this database (Keywords): Tranexamic Acid; Fibrinolysis; Drug Treatment; Atherosclerosis; Recombinant Apo(A)