A new cardioprotective agent, JTV519, improves defective channel gating of ryanodine receptor in heart failure
Department of Medical Bioregulation, Division of Cardiovascular Medicine, Yamaguchi University School of Medicine, Yamaguchi 755-8505, Japan Defective interaction between FKBP12.6 and ryanodine receptors (RyR) is a possible cause of cardiac dysfunction in heart failure (HF). Here, we assess whether...
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Published in | American journal of physiology. Heart and circulatory physiology Vol. 284; no. 3; pp. H1035 - H1042 |
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Main Authors | , , , , , , , , , |
Format | Journal Article |
Language | English |
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United States
01.03.2003
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Abstract | Department of Medical Bioregulation, Division of
Cardiovascular Medicine, Yamaguchi University School of Medicine,
Yamaguchi 755-8505, Japan
Defective
interaction between FKBP12.6 and ryanodine receptors (RyR) is a
possible cause of cardiac dysfunction in heart failure (HF). Here, we
assess whether the new cardioprotective agent JTV519 can correct it in
tachycardia-induced HF. HF was induced in dogs by 4-wk rapid
ventricular pacing, and sarcoplasmic reticulum (SR) was isolated from
left ventricular muscles. In failing SR, JTV519 increased the rate of
Ca 2+ release and [ 3 H]ryanodine binding. RyR
were then labeled in a site-directed fashion with the fluorescent
conformational probe methylcoumarin acetamide. In failing SR, the
polylysine induced a rapid change in methylcoumarin acetamide
fluorescence, presumably because the channel opening preceding the
Ca 2+ release was smaller than in normal SR (consistent with
a decreased rate of Ca 2+ release in failing SR), and JTV519
increased it. In conclusion, JTV519, a new 1,4-benzothiazepine
derivative, corrected the defective channel gating in RyR (increase in
both the rapid conformational change and the subsequent
Ca 2+ release rate) in HF.
sarcoplasmic reticulum; ion channel; binding protein; excitation-contraction coupling |
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AbstractList | Defective interaction between FKBP12.6 and ryanodine receptors (RyR) is a possible cause of cardiac dysfunction in heart failure (HF). Here, we assess whether the new cardioprotective agent JTV519 can correct it in tachycardia-induced HF. HF was induced in dogs by 4-wk rapid ventricular pacing, and sarcoplasmic reticulum (SR) was isolated from left ventricular muscles. In failing SR, JTV519 increased the rate of Ca(2+) release and [(3)H]ryanodine binding. RyR were then labeled in a site-directed fashion with the fluorescent conformational probe methylcoumarin acetamide. In failing SR, the polylysine induced a rapid change in methylcoumarin acetamide fluorescence, presumably because the channel opening preceding the Ca(2+) release was smaller than in normal SR (consistent with a decreased rate of Ca(2+) release in failing SR), and JTV519 increased it. In conclusion, JTV519, a new 1,4-benzothiazepine derivative, corrected the defective channel gating in RyR (increase in both the rapid conformational change and the subsequent Ca(2+) release rate) in HF. Defective interaction between FKBP12.6 and ryanodine receptors (RyR) is a possible cause of cardiac dysfunction in heart failure (HF). Here, we assess whether the new cardioprotective agent JTV519 can correct it in tachycardia-induced HF. HF was induced in dogs by 4-wk rapid ventricular pacing, and sarcoplasmic reticulum (SR) was isolated from left ventricular muscles. In failing SR, JTV519 increased the rate of Ca 2+ release and [ 3 H]ryanodine binding. RyR were then labeled in a site-directed fashion with the fluorescent conformational probe methylcoumarin acetamide. In failing SR, the polylysine induced a rapid change in methylcoumarin acetamide fluorescence, presumably because the channel opening preceding the Ca 2+ release was smaller than in normal SR (consistent with a decreased rate of Ca 2+ release in failing SR), and JTV519 increased it. In conclusion, JTV519, a new 1,4-benzothiazepine derivative, corrected the defective channel gating in RyR (increase in both the rapid conformational change and the subsequent Ca 2+ release rate) in HF. Department of Medical Bioregulation, Division of Cardiovascular Medicine, Yamaguchi University School of Medicine, Yamaguchi 755-8505, Japan Defective interaction between FKBP12.6 and ryanodine receptors (RyR) is a possible cause of cardiac dysfunction in heart failure (HF). Here, we assess whether the new cardioprotective agent JTV519 can correct it in tachycardia-induced HF. HF was induced in dogs by 4-wk rapid ventricular pacing, and sarcoplasmic reticulum (SR) was isolated from left ventricular muscles. In failing SR, JTV519 increased the rate of Ca 2+ release and [ 3 H]ryanodine binding. RyR were then labeled in a site-directed fashion with the fluorescent conformational probe methylcoumarin acetamide. In failing SR, the polylysine induced a rapid change in methylcoumarin acetamide fluorescence, presumably because the channel opening preceding the Ca 2+ release was smaller than in normal SR (consistent with a decreased rate of Ca 2+ release in failing SR), and JTV519 increased it. In conclusion, JTV519, a new 1,4-benzothiazepine derivative, corrected the defective channel gating in RyR (increase in both the rapid conformational change and the subsequent Ca 2+ release rate) in HF. sarcoplasmic reticulum; ion channel; binding protein; excitation-contraction coupling |
Author | Oda, Tetsuro Kohno, Masateru Tokuhisa, Takahiro Okuda, Shinichi Kobayashi, Shigeki Doi, Masahiro Ohkusa, Tomoko Yano, Masafumi Kohno, Michihiro Matsuzaki, Masunori |
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BackLink | https://www.ncbi.nlm.nih.gov/pubmed/12433661$$D View this record in MEDLINE/PubMed |
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Snippet | Department of Medical Bioregulation, Division of
Cardiovascular Medicine, Yamaguchi University School of Medicine,
Yamaguchi 755-8505, Japan
Defective... Defective interaction between FKBP12.6 and ryanodine receptors (RyR) is a possible cause of cardiac dysfunction in heart failure (HF). Here, we assess whether... |
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SubjectTerms | Animals Binding, Competitive - drug effects Calcium - metabolism Calcium - pharmacokinetics Calcium Channel Blockers - pharmacology Cardiac Pacing, Artificial Cardiotonic Agents - pharmacology Cardiotonic Agents - therapeutic use Coumarins - chemistry Disease Models, Animal Dogs Fluorescent Dyes - chemistry Heart Failure - drug therapy Heart Failure - physiopathology Hemodynamics - drug effects Immunosuppressive Agents - pharmacology Ion Channel Gating - drug effects Polylysine - pharmacology Protein Conformation - drug effects Radioligand Assay Ryanodine Receptor Calcium Release Channel - chemistry Ryanodine Receptor Calcium Release Channel - drug effects Ryanodine Receptor Calcium Release Channel - metabolism Sarcoplasmic Reticulum - chemistry Sarcoplasmic Reticulum - drug effects Sarcoplasmic Reticulum - metabolism Tacrolimus - pharmacology Tacrolimus Binding Proteins - metabolism Thiazepines - pharmacology Thiazepines - therapeutic use |
Title | A new cardioprotective agent, JTV519, improves defective channel gating of ryanodine receptor in heart failure |
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