New HT service accelerates cellular target screening

The service extends its capabilities so it can comfortably undertake selectivity profiling against a panel of key indicators, such as HERG(human ether-a-go-go related gene) and Na(v) 1.5 making the pre-screening process an even more valuable first step.

Ion channels play an important role in cell signalling, electrical excitability and fluid transport, and are drug targets themselves in a number of indications, including heart disease, diabetes, autoimmune diseases and migraine. Small molecules that block or open ion channels are considered to be promising drug candidates.

In addition, some ion channels on heart muscle cells are associated with toxicology problems, and candidates drugs are routinely screened against them.

Clients can have their own libraries screened, or they can opt to buy SoftFocus Ion Channel libraries from BioFocus. BioFocus has developed a method for the design ofits Ion Channel libraries, that uses a chemo-genomic approach which links X-ray structures, primary sequence alignment, and mutagenesis data directly to SAR.

Using this approach BioFocus is able to define the key helicaldomains and drug binding regions within the channel pore. This "Helical Domain Recognition Analysis" approach builds upon BioFocus' Thematic Analysis, to give not only a far higher than average hit rate, but also a fast track to SAR.

Julie Frearson, divisional director of biology at BioFocus​ said: This new service makes it easier and cost effective for pharmaceutical companies to take the first step into the promising field of ion channel screening."​

"The current 'gold standard', electrophysiology, provides a great deal of information, but it is time consuming and not suited to needs of high-throughput screening. However, if electrophysiology is used as a follow-up to our initial pre-screening and our selectivity profiling panel, companies can match their most valuable resources to the on-going generation of promising leads and candidates."​