Drug interaction with cardiac and skeletal muscle troponin C. 1990

R N Geguchadze, and A V Krylatov, and N B Gusev
Department of Biochemistry, School of Biology, Moscow State University, USSR.

The effects of certain drugs on the binding of divalent cations to Ca(2+)-specific and Ca/Mg sites on cardiac and skeletal troponin C molecules were investigated by fluorescence and circular dichroism spectroscopy. Nicardipine and two new cardiotonic agents, APP 201-533 and DPI 201-106, interact with the N-terminal domain of troponin C, and either do not affect or, in the case of DPI 201-106, slightly increase the affinity of the Ca(2+)-specific site of troponin C for Ca2+ ion. Compound 48/80 seems to interact with the central alpha-helix of skeletal troponin C and affects the cation-binding properties of both the Ca(2+)-specific and the Ca/Mg sites of the protein. Trifluoperazine and calmidazolium (R24571) interact with the C-terminal domain of troponin C and increase the affinity of the Ca/Mg sites located there. At high concentrations these compounds interact with the N-terminal domain of troponin C and increase the affinity of the Ca(2+)-specific site. According to fluorescence spectroscopy data, R24571 induces conformational changes in troponin C similar to those evoked by troponin I. The experimental data suggest that the drugs studied act in similar ways with troponin C and calmodulin.

UI MeSH Term Description Entries
D007093 Imidazoles Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
D008274 Magnesium A metallic element that has the atomic symbol Mg, atomic number 12, and atomic weight 24.31. It is important for the activity of many enzymes, especially those involved in OXIDATIVE PHOSPHORYLATION.
D009132 Muscles Contractile tissue that produces movement in animals. Muscle Tissue,Muscle,Muscle Tissues,Tissue, Muscle,Tissues, Muscle
D009206 Myocardium The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow. Muscle, Cardiac,Muscle, Heart,Cardiac Muscle,Myocardia,Cardiac Muscles,Heart Muscle,Heart Muscles,Muscles, Cardiac,Muscles, Heart
D009529 Nicardipine A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents. Antagonil,Cardene,Cardene I.V.,Cardene SR,Dagan,Flusemide,Lecibral,Lincil,Loxen,Lucenfal,Nicardipine Hydrochloride,Nicardipine LA,Nicardipino Ratiopharm,Nicardipino Seid,Perdipine,Ridene,Vasonase,Y-93,Hydrochloride, Nicardipine,LA, Nicardipine,Y 93,Y93
D010879 Piperazines Compounds that are derived from PIPERAZINE.
D011485 Protein Binding The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments. Plasma Protein Binding Capacity,Binding, Protein
D011487 Protein Conformation The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain). Conformation, Protein,Conformations, Protein,Protein Conformations
D011728 Pyridones Pyridine derivatives with one or more keto groups on the ring. Pyridinones
D011817 Rabbits A burrowing plant-eating mammal with hind limbs that are longer than its fore limbs. It belongs to the family Leporidae of the order Lagomorpha, and in contrast to hares, possesses 22 instead of 24 pairs of chromosomes. Belgian Hare,New Zealand Rabbit,New Zealand Rabbits,New Zealand White Rabbit,Rabbit,Rabbit, Domestic,Chinchilla Rabbits,NZW Rabbits,New Zealand White Rabbits,Oryctolagus cuniculus,Chinchilla Rabbit,Domestic Rabbit,Domestic Rabbits,Hare, Belgian,NZW Rabbit,Rabbit, Chinchilla,Rabbit, NZW,Rabbit, New Zealand,Rabbits, Chinchilla,Rabbits, Domestic,Rabbits, NZW,Rabbits, New Zealand,Zealand Rabbit, New,Zealand Rabbits, New,cuniculus, Oryctolagus

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