Fragment screening by surface plasmon resonance.

ABSTRACT: Fragment-based drug discovery is a validated approach for the discovery of drug candidates. However, the weak affinity of fragment compounds requires highly sensitive biophysical techniques, such as nuclear magnetic resonance (NMR) or X-ray crystallography, to identify hits. Thus the advantages of screening small fragment libraries are partly offset by the high cost of biophysical analyses. Here we present a method for biosensor-based fragment screening using surface plasmon resonance (SPR). In order to reduce the false positive detection rate we present a novel method of data analysis that incorporates multiple referencing with ligand efficiency. By implementing all necessary steps for assay design, data analysis and interpretation, SPR-based fragment screening has potential to eliminate

SUBMITTER: Navratilova I 

PROVIDER: S-EPMC4007845 | biostudies-literature | 2010 Apr

REPOSITORIES: biostudies-literature