Newly-developed device that can complete perfectly high throughput screening

Screening a library of compounds and choosing compounds having the desired biological activity are one of selected and effective methods of developing new drugs, but this method requires large, expensive and complicated equipment. Today, the Scripps Research Institute (TSRI) of Brian M. Paegel team designed a core part of a screening system, will reduce the size and cost of screening equipment several orders of magnitude.

The current high-throughput screening systems typically occupy 10,000 square feet of space or more, and the need to spend millions of dollars. They rely heavily on libraries of compounds can retrieve robot apparatus, each of the compounds into “assay microplate” separate hole and determining the biological activity of each compound. Such a system is amazing screening efficiency, but its cost is also amazing, limit their large-scale application.

Paegel said, "This device we developed is very small, but the function can be comparable to high-throughput screening of compounds."

They use the "one-bead-one-compound (OBOC)" library, where each bead is connected one compound. This library preparation is quick and inexpensive, basically as laboratory consumables. "Building a compound that contains millions of OBOC library probably only spends a week and $ 500," senior researcher Paegel laboratory Alexander K. Price said, is the first author of this paper.

The compound even in the microbeads into the micro filter apparatus is still a technical problem. Paegel and Price designed a desktop device in order to meet these challenges, and can filter OBOC library. The microfluidic device based on the principle of inkjet printing technology and manufacturing, "Hopper suspension" before using the inventive team, OBOC library beads were introduced into tiny droplets conducted specific tests (e.g. enzyme activity assay). These droplets than high-volume throughput screening about 100,000 volumes of test used less.

Then, the device with UV-induced photochemical reaction, the compound released from each bead, after the reaction period, recording the results of each droplet.

Them this device is named LIGHTSABR (Light-Induced and Graduated High-Throughput Screening after Bead Release). The key innovation is that it allows the user to adjust the amount of ultraviolet radiation to change the beads were released compounds in order to adjust the dose of the test compound. The team by screening HIV-1 protease (which is caused by a key enzyme in HIV replication) inhibitors, successfully demonstrated this dose adjustments.

Paegel next step will be committed to the promotion and Price LIGHTSABR system. "Around the world, hundreds of laboratories can run their own miniaturized screening equipment, using their own test methods for drug screening for the most interesting target," Price said.

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