Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie, FL 34987, USA.
Molecules. 2013 May 30;18(6):6408-24. doi: 10.3390/molecules18066408.
In the past 20 years, synthetic combinatorial methods have fundamentally advanced the ability to synthesize and screen large numbers of compounds for drug discovery and basic research. Mixture-based libraries and positional scanning deconvolution combine two approaches for the rapid identification of specific scaffolds and active ligands. Here we present a quantitative assessment of the screening of 32 positional scanning libraries in the identification of highly specific and selective ligands for two formylpeptide receptors. We also compare and contrast two mixture-based library approaches using a mathematical model to facilitate the selection of active scaffolds and libraries to be pursued for further evaluation. The flexibility demonstrated in the differently formatted mixture-based libraries allows for their screening in a wide range of assays.
在过去的 20 年中，合成组合方法从根本上提高了合成和筛选大量化合物的能力，以用于药物发现和基础研究。基于混合物的文库和位置扫描解卷积结合了两种方法，用于快速鉴定特定支架和活性配体。在这里，我们对 32 个位置扫描文库的筛选进行了定量评估，以鉴定两种甲酰肽受体的高度特异性和选择性配体。我们还使用数学模型比较和对比了两种基于混合物的文库方法，以方便选择要进一步评估的活性支架和文库。不同格式的基于混合物的文库的灵活性允许它们在广泛的测定中进行筛选。
