Issue 20, 2010

Preparation of FRET reporters to support chemical probe development

Abstract

In high throughput screening (HTS) campaigns, the quality and cost of commercial reagents suitable for pilot studies often create obstacles upon scale-up to a full screen. We faced such challenges in our efforts to implement an HTS for inhibitors of the phosphopantetheinyl transferase Sfp using an assay that had been validated using commercially available reagents. Here we demonstrate a facile route to the synthetic preparation of reactive tetraethylrhodamine and quencher probes, and their application to economically produce fluorescent and quencher-modified substrates. These probes were prepared on a scale that would allow a full, quantitative HTS of more than 350,000 compounds.

Graphical abstract: Preparation of FRET reporters to support chemical probe development

Supplementary files

Article information

Article type
Paper
Submitted
25 Jun 2010
Accepted
21 Jul 2010
First published
20 Aug 2010

Org. Biomol. Chem., 2010,8, 4601-4606

Preparation of FRET reporters to support chemical probe development

T. L. Foley, A. Yasgar, C. J. Garcia, A. Jadhav, A. Simeonov and M. D. Burkart, Org. Biomol. Chem., 2010, 8, 4601 DOI: 10.1039/C0OB00322K

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