Article | March 12, 2008

Compound Screening And Characterization Using Label-Free Interaction Analysis

Source: GE Healthcare Life Sciences
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By Markku D. Hämäläinen, Senior Scientist in Chemometrics, and Fredrik Sundberg, Director of Strategic Market Development GE Healthcare

Surface plasmon resonance (SPR) detection could serve as a complement — or alternative — to high-throughput screening (HTS) in modern drug discovery.

The process of bringing new drugs successfully to market continues to present an enormous challenge. Despite recent significant investment in approaches such as high-throughput screening (HTS), attrition rates during later development phases remain high, resulting in costly failures. HTS involves the rapid analysis of very large compound libraries, but in many cases, the majority of hits identified are falsepositives and the compounds do not bind to the intended functional binding site on the target. Moreover, these are predominantly equilibriumbased assays that cannot deliver comprehensive binding data that may be highly relevant for the in vivo therapeutic performance of the drug. Adding to the challenge, some target classes (e.g. proteases), as well as particularly difficult individual drug targets (e.g. those with unknown or unstable functional partners), are unsuitable for HTS assays and require an alternative approach.