Chip Chops Time off Drug Discovery Process

A next-generation optical screening platform that is set to accelerate the drug discovery process and uses far less quantities of reagents has been developed by Cambridge company Genapta in collaboration with GlaxoSmithKline (GSK) after just eighteen months of development time.


Julian White

The biochip, based on tiny microfluidic channels less than 50 micrometers in diameter, has a novel equipment configuration that can quantify the transient binding of putative drug compounds as they interact with an array of protein targets held on the chip-usually brain and liver proteins. According to Genapta's Julian White, the new configuration works "within the challenging circumstances of the pulsed flow environment of a developmental drug discovery platform". In other words, GSK can use the biochip to screen a vast number of compounds rapidly by passing wave after wave of compounds in solution over the surface of the chip. Any molecules in the mix that bind to the protein targets are revealed by fluorescence.

At the core of the biochip is an optical head slightly larger than a box of matches which has many of the functions of the sophisticated confocal microscope used by molecular biologists to investigate proteins and cell components. The system itself uses a combination of Genapta's novel fiber optic core and industry standard techniques, such as Fluorescence Resonance Energy Transfer (FRET) and fluorescence polarization, to measure how well a compound binds to a protein target. Those compounds that bind the longest produce the strongest signal and so can be singled out for further investigation.

"We have been working closely with GSK over the last eighteen months to deliver new platform technologies to match their needs," adds White. "We are pleased to say that this has been successful and the customer can now assess compound potency with our platform."

The Genapta team has also developed a set of complementary tools to exploit the new technology and now supplies turnkey biochemistry systems to GSK. White points out that the devices have allowed GSK to accelerate the development of its microfluidic platform to the point where it can screen compounds with orders of magnitude less reagent than existing systems.