Advancing cancer therapeutics: Development of assays for measuring RNA helicase activity

Sponsored Content by BellBrook LabsMay 14 2024Reviewed by Olivia Frost RNA helicases are a group of enzymes that bind to and alter RNA in an ATP-dependent way. They play significant roles in RNA metabolism, gene expression regulation, and innate immunity. Different RNA helicases, particularly those in the dead box helicase family, are dysregulated in cancer; however, there have been very few attempts to produce small molecule inhibitors.

Purified enzymes determined the RNA substrate, cofactor requirements, and kinetic parameters. The assays were then optimized for initial velocity detection of RNA-dependent ATPase activity with a Z’ value greater than 0.7, guaranteeing an adequate signal window for inhibitor screening and dose-response assays. Each of the helicase assays were then validated by screening a library of bioactives and perfoming follow-up dose response measurements.

Conclusions About BellBrook Labs BellBrook Labs is dedicated to providing scientists with enabling screening tools to accelerate the discovery of more effective therapies. Leveraging its two base platforms, BellBrook has developed easy-to-use assays for hundreds of drug targets. AptaFluor® Biochemical Assay Technology AptaFluor leverages a spit aptamer technology to directly detect SAH, the common product of Methyltransferases. As the most sensitive HTS methyltransferase activity assay available, AptaFluor dramatically reduces enzyme usage and allows the assay to be run at or below Km for SAM.

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