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Screening for Novel Type 2 Ryanodine Receptor Inhibitors by Endoplasmic Reticulum Ca2+ Monitoring.

Molecular pharmacology - 1 Dec 2023

Takenaka Mai, Kodama Masami, Murayama Takashi, Ishigami-Yuasa Mari, Mori Shuichi, Ishida Ryosuke, Suzuki Junji, Kanemaru Kazunori, Sugihara Masami, Iino Masamitsu, Miura Aya, Nishio Hajime, Morimoto Sachio, Kagechika Hiroyuki, Sakurai Takashi, Kurebayashi Nagomi

Abstract excerpt

Type 2 ryanodine receptor (RyR2) is a Ca2+ release channel on the endoplasmic (ER)/sarcoplasmic reticulum that plays a central role in the excitation-contraction coupling in the heart. Hyperactivity of RyR2 has been linked to ventricular arrhythmias in patients with catecholaminergic polymorphic ventricular tachycardia and heart failure, where spontaneous Ca2+ release via hyperactivated RyR2 depolarizes diastolic...

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Identifiers

PMID: 37678938
DOI: 10.1124/molpharm.123.000720

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