Yin Shuangye, Biedermannova Lada, Vondrasek Jiri, Dokholyan Nikolay V
Department of Biochemistry and Biophysics, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
J Chem Inf Model. 2008 Aug;48(8):1656-62. doi: 10.1021/ci8001167. Epub 2008 Aug 2.
Virtual screening is becoming an important tool for drug discovery. However, the application of virtual screening has been limited by the lack of accurate scoring functions. Here, we present a novel scoring function, MedusaScore, for evaluating protein-ligand binding. MedusaScore is based on models of physical interactions that include van der Waals, solvation, and hydrogen bonding energies. To ensure the best transferability of the scoring function, we do not use any protein-ligand experimental data for parameter training. We then test the MedusaScore for docking decoy recognition and binding affinity prediction and find superior performance compared to other widely used scoring functions. Statistical analysis indicates that one source of inaccuracy of MedusaScore may arise from the unaccounted entropic loss upon ligand binding, which suggests avenues of approach for further MedusaScore improvement.
虚拟筛选正成为药物发现的一项重要工具。然而,虚拟筛选的应用一直受到缺乏准确评分函数的限制。在此,我们提出一种用于评估蛋白质-配体结合的新型评分函数——美杜莎评分(MedusaScore)。美杜莎评分基于包括范德华力、溶剂化作用和氢键能在内的物理相互作用模型。为确保评分函数具有最佳的可转移性,我们在参数训练中未使用任何蛋白质-配体实验数据。然后,我们测试了美杜莎评分在对接诱饵识别和结合亲和力预测方面的表现,发现其性能优于其他广泛使用的评分函数。统计分析表明,美杜莎评分不准确的一个原因可能是配体结合时未考虑到的熵损失,这为进一步改进美杜莎评分指明了方向。