Screening for Inhibitors of the Anticancer Target and Ubiquitination Regulator CSN5 with an HTS Fluorescence Polarization Technique

Neddylation activates Cullin-RING E3 ubiquitin ligases (CRLs), and de-neddylation which is attained by COP9 signalosome (CSN) deactivates them. Keeping CRLs in their inactive mode enhances tumor suppressors. Hence, for cancer therapy, inhibition of CSN becomes a vital approach.

The development of a high-throughput de-neddylation method for CRL is described here. This method was utilized to spot inhibitors of the de-neddylating CSN. A fluorophore having an extended fluorescence lifetime was used to optimize the fluorescence polarization method.

An assay window of 130 mP was obtained by carrying out the assay in a 384 well plate, and recording it on a PHERAstar® microplate reader. The capability of the instrument for parallel identification of two polarization channels quickened the assessment. It also allowed kinetic reads. Therefore, the technique can be applied to both CSN inhibitor spotting and profiling.

About BMG Labtech

BMG LABTECH has been committed to producing microplate readers for more than twenty years. By focusing on the needs of the scientific community, the company’s innovative microplate readers have earned the company the reputation of being a technology leader in the field.

BMG LABTECH has developed a wide range of dedicated and multi-mode microplate readers for life sciences applications and high-throughput screening.

All BMG LABTECH microplate readers are "Made in Germany" and are conceived, developed, assembled, and tested entirely at our headquarters in Germany.

Since our establishment in Offenburg, Germany in 1989, BMG LABTECH has expanded to offer a worldwide sales and support network with offices in the USA, UK, Australia, Japan and France. Our subsidiaries, regional offices and distributors are committed to bringing you innovative microplate reader technology with the quality and reliability you expect from a German company.

Our staff includes engineers and scientists from the fields of biology, biochemistry, analytical chemistry, and physics.

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Last updated: Jul 31, 2018 at 3:16 AM

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