Institut de Chimie de Nice, UMR CNRS, Université de Nice Sophia Antipolis 7272, 06108 Nice Cedex 2, France.
Cell Mol Life Sci. 2012 Dec;69(24):4205-13. doi: 10.1007/s00018-012-1116-0. Epub 2012 Aug 29.
The molecular features that dominate the binding mode of agonists by a broadly tuned olfactory receptor are analyzed through a joint approach combining cell biology, calcium imaging, and molecular modeling. The odorant/receptor affinities, estimated through statistics accrued during molecular dynamics simulations, are in accordance with the experimental ranking. Although in many systems receptors recognize their target through a network of oriented interactions, such as H-bonding, the binding by broadly tuned olfactory receptors is dominated by non-polar terms. We show how such a feature allows chemicals belonging to different chemical families to similarly activate the receptors through compensations of interactions within the binding site.
通过结合细胞生物学、钙成像和分子建模的联合方法,分析了广泛调谐的嗅觉受体与激动剂结合模式占主导地位的分子特征。通过分子动力学模拟过程中累积的统计数据来估计配体/受体亲和力,这与实验排序一致。尽管在许多系统中,受体通过定向相互作用(如氢键)的网络来识别其靶标,但广泛调谐的嗅觉受体的结合主要由非极性项主导。我们展示了这种特征如何允许属于不同化学家族的化学物质通过在结合位点内的相互作用补偿来类似地激活受体。