Hanley Ronan P, Horvath Shanti, An Jianghong, Hof Fraser, Wulff Jeremy E
Department of Chemistry, University of Victoria, PO Box 3065 STN CSC, Victoria, BC V8W 3V6, Canada.
BC Cancer Agency Genome Sciences Center, Vancouver, BC V5Z 4S6, Canada.
Bioorg Med Chem Lett. 2016 Feb 1;26(3):973-977. doi: 10.1016/j.bmcl.2015.12.050. Epub 2015 Dec 17.
Given the importance of high-throughput screening in drug discovery, the identification of compounds that interfere with assay readouts is crucial. The pursuit of false positives wastes time and money, while distracting development teams from more promising leads. In the context of TR-FRET assays, most interfering compounds are dyes or aggregators. In the course of our studies on the PD1-PDL2 interaction, we discovered that salicylic acids, an extremely common compound subclass in screening libraries, interfere with TR-FRET assays. While the precise mechanism of interference was not established, our data suggest that interaction of the salicylate with the cryptand-ligated europium FRET donor is responsible for the change in assay signal.
鉴于高通量筛选在药物发现中的重要性,识别干扰检测读数的化合物至关重要。追求假阳性会浪费时间和金钱,同时使开发团队从更有前景的线索中分心。在时间分辨荧光共振能量转移(TR-FRET)检测中,大多数干扰化合物是染料或聚集剂。在我们对PD1-PDL2相互作用的研究过程中,我们发现水杨酸(筛选文库中极其常见的一类化合物)会干扰TR-FRET检测。虽然干扰的确切机制尚未确定,但我们的数据表明,水杨酸盐与穴状配体连接的铕荧光共振能量转移供体的相互作用是检测信号变化的原因。