Aptula Aynur O, Patlewicz Grace, Roberts David W
SEAC, Unilever Colworth, Sharnbrook, Bedford, MK44 1LQ, England.
Chem Res Toxicol. 2005 Sep;18(9):1420-6. doi: 10.1021/tx050075m.
The prediction of skin sensitization potential with minimum animal testing is currently of great importance in light of forthcoming legislation. A number of structure-activity relationships for skin sensitization have been published over the years, but their applicability has often been limited to structural classes. The concept of an applicability domain for a quantitative structure-activity relationship [(Q)SAR] is increasingly being viewed as key for the predictive application of (Q)SARs. This is particularly the case for skin sensitization if more widely applicable SARs are to be developed. In this paper, we analyze a recently published chemical data set for skin sensitization, apply reaction mechanistic criteria to domain classification, and evaluate the structure-activity trends observed within each of these mechanistic domains.
鉴于即将出台的法规,利用最少的动物试验来预测皮肤致敏潜力目前至关重要。多年来已经发表了许多关于皮肤致敏的构效关系,但它们的适用性通常仅限于结构类别。定量构效关系((Q)SAR)适用性域的概念越来越被视为(Q)SAR预测应用的关键。如果要开发更广泛适用的SARs,对于皮肤致敏尤其如此。在本文中,我们分析了最近发表的一组皮肤致敏化学数据集,将反应机理标准应用于域分类,并评估在每个这些机理域内观察到的构效趋势。