The mathematics of a successful deconvolution: a quantitative assessment of mixture-based combinatorial libraries screened against two formylpeptide receptors.
The mathematics of a successful deconvolution: a quantitative assessment of mixture-based combinatorial libraries screened against two formylpeptide receptors.
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DOI：
10.3390/molecules18066408
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发表时间：
2013-05-30
期刊：
影响因子：
--
通讯作者：
Pinilla C
中科院分区：
文献类型：
--
作者：
Santos RG;Appel JR;Giulianotti MA;Edwards BS;Sklar LA;Houghten RA;Pinilla C
在过去的20年里，合成组合方法从根本上提高了合成和筛选大量化合物用于药物发现和基础研究的能力。基于混合物的文库和位置扫描去卷积联合收割机结合了两种用于快速鉴定特定支架和活性配体的方法。在这里，我们提出了一个定量评估的32个位置扫描库的筛选，在两个甲酰肽受体的高度特异性和选择性的配体的识别。我们还比较和对比两种基于混合物的库方法，使用数学模型，以方便选择活性支架和库进行进一步评估。在不同格式的基于混合物的文库中展示的灵活性允许在广泛的测定中对其进行筛选。
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.
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影响因子：
--
作者：
Giulianotti, Marc A.;Debevec, Ginamarie;Houghten, Richard A.
通讯作者：
Houghten, Richard A.
影响因子：
82.9
作者：
Pinilla, Clemencia;Appel, Jon R.;Houghten, Richard A.
通讯作者：
Houghten, Richard A.
影响因子：
2.7
作者：
Ranjit, Dev K.;Rideout, Marc C.;Segall, Anca M.
通讯作者：
Segall, Anca M.
影响因子：
4.5
作者：
Reilley, Kate J.;Giulianotti, Marc;Houghten, Richard A.
通讯作者：
Houghten, Richard A.
影响因子：
10.3
作者：
Zhou, Y;Bian, XW;Wang, JM
通讯作者：
Wang, JM