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2010 ; 1
(1
): 44-8
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Fragment screening by surface plasmon resonance
#MMPMID24900174
Navratilova I
; Hopkins AL
ACS Med Chem Lett
2010[Apr]; 1
(1
): 44-8
PMID24900174
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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 all nonspecific (false positive) binders. Therefore, given the
advantages of low protein consumption, rapid assay development and kinetic and
thermodynamic validation of hits, SPR can be considered as a primary screening
technology for fragment-based drug discovery.
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