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Potential functional and pathological side effects related to off-target pharmacological activity

机译:与非靶标药理活动相关的潜在功能和病理副作用

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摘要

Most pharmaceutical companies test their discovery-stage proprietary molecules in a battery of in vitro pharmacology assays to try to determine off-target interactions. During all phases of drug discovery and development, various questions arise regarding potential side effects associated with such off-target pharmacological activity. Here we present a scientific literature curation effort undertaken to determine and summarize the most likely functional and pathological outcomes associated with interactions at 70 receptors, enzymes, ion channels and transporters with established links to adverse effects. To that end, the scientific literature was reviewed using an on-line database, and the most commonly reported effects were summarized in tabular format. The resultant table should serve as a practical guide for research scientists and clinical investigators for the prediction and interpretation of adverse side effects associated with molecules interacting with components of this screening battery. (C) 2017 Elsevier Inc. All rights reserved.
机译:大多数制药公司在体外药理学测定的电池中测试他们的发现阶段专有分子,以试图确定偏离靶标相互作用。在药物发现和发展的所有阶段,出现关于与这种偏离目标药理活性相关的潜在副作用的各种问题。在这里,我们提出了一种科学的文学策策,以确定和总结与70个受体,酶,离子通道和转运蛋白的相互作用相关的最有可能的功能和病理结果,其具有与不利影响的共同的联系。为此,使用在线数据库进行审查科学文献,并且最常见的效果以表格格式总结。结果表应作为研究科学家和临床研究人员的实用指南,用于预测和解释与与该筛选电池组分相互作用的分子相关的不良副作用。 (c)2017年Elsevier Inc.保留所有权利。

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