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Tox-Database.net: a curated resource for data describing chemical triggered in vitro cardiac ion channels inhibition

机译:Tox-Database.net:精选资料用于描述化学触发的体外心脏离子通道抑制作用的数据

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摘要

BackgroundDrugs safety issues are now recognized as being factors generating the most reasons for drug withdrawals at various levels of development and at the post-approval stage. Among them cardiotoxicity remains the main reason, despite the substantial effort put into in vitro and in vivo testing, with the main focus put on hERG channel inhibition as the hypothesized surrogate of drug proarrhythmic potency. The large interest in the IKr current has resulted in the development of predictive tools and informative databases describing a drug's susceptibility to interactions with the hERG channel, although there are no similar, publicly available sets of data describing other ionic currents driven by the human cardiomyocyte ionic channels, which are recognized as an overlooked drug safety target.
机译:背景技术如今,人们认识到毒品安全问题是在各个发展阶段和批准后阶段导致停药的最主要原因。尽管进行了体外和体内测试,尽管如此,但心脏毒性仍然是主要原因,其主要重点是hERG通道抑制作为假设的药物心律失常效能的替代。尽管没有相似的,可公开获得的描述人类心肌细胞离子驱动的其他离子流的数据,但对IKr电流的极大兴趣已导致描述药物对hERG通道相互作用的敏感性的预测工具和信息数据库的开发。渠道,被认为是被忽视的药物安全目标。

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