AZ looks at Almac’s Flexyte platform for drug discovery

By Gareth Macdonald

- Last updated on GMT

Related tags Signal transduction

UK drug major AstraZeneca will evaluate Almac’s antibody and radiolabelling-free Flexyte kinase assay platform for drug discovery operations.

Almac’s Flexxyte system, developed with Edinburgh Instruments, uses the principle of “fluorescence lifetime,” the length of time a molecule remains excited, to measure activity of protein kinase targets when they encounter drug candidates.

Protein kinases, particularly those that interact with serine and threonine residues, are among the most promising drug targets due to their role in the development of diseases ranging from cancer and diabetes to neurodegenerative conditions.

As a result, drugmakers are increasingly focused on evaluating compounds that can modulate the function of these enzymes, and thus, the pathology of some of the most significant, and therefore potentially lucrative, diseases known to man.

However, in practice such evaluations can be complicated, requiring the development of specific antibodies to the target in question. The process can also be prone to “false positive” results as due to background interference or inherent fluorescence of the candidate compounds being screened.

Additionally, many commercially available fluorescent dyes have very limited half-lives, making them unusable for assay reporting purposes during compound screening, which is where Almac believes its technology has the advantage.

According to a poster presented at the MIPTEC conference in Basel, Switzerland last year, the Flexyte system is based on a range of long half-life dyes derived 9-aminoacridine (9AA), that provide a measurable way of recording kinase activity.

The Northern Ireland-based contract services firm claimed that by “avoiding radioactivity, antibodies and associated costs, [the technology enables homogenous, robust and reliable assays … and will allow miniaturization, and multiplexing, while maintaining an information-rich output.”

Almac Sciences president Stephen Barr said the firm is “delighted that AstraZeneca have shown this level of interest in our proprietal protein kinase assay platform,​ “adding it “indicates the potential of fluorescence lifetime as a reporting modality for kinase assays.”

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