Conway Institute of Biomolecular & Biomedical Research, School of Medicine and Medical Science, University College Dublin, Belfield, Dublin 4, Ireland.
Drug Discov Today. 2010 Sep;15(17-18):749-56. doi: 10.1016/j.drudis.2010.06.006. Epub 2010 Jun 18.
Off-target hits of drugs can lead to serious adverse effects or, conversely, to unforeseen alternative medical utility. Selectivity profiling against large panels of potential targets is essential for the drug discovery process to minimize attrition and maximize therapeutic utility. Lately, it has become apparent that drug promiscuity (polypharmacology) goes well beyond target families; therefore, lowering the profiling costs and expanding the coverage of targets is an industry-wide challenge to improve predictions. Here, we review current and promising drug profiling alternatives and commercial solutions in these exciting emerging fields.
药物的脱靶作用可能导致严重的不良反应，或者相反地产生意想不到的其他医学用途。针对大量潜在靶点进行选择性分析对于药物发现过程至关重要，可最大限度地减少损耗并提高治疗效果。最近，药物的混杂性（多药理学）显然远远超出了靶家族的范围；因此，降低分析成本并扩大靶点覆盖范围是提高预测能力的全行业挑战。在这里，我们回顾了当前和有前途的药物分析替代方法和商业解决方案，这些方法和解决方案在这些令人兴奋的新兴领域中具有广阔的前景。
