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Article Dans Une Revue Expert Opinion on Drug Discovery Année : 2016

Developments in SPR Fragment Screening


INTRODUCTION: Fragment-based approaches have played an increasing role alongside high-throughput screening in drug discovery for 15 years. The label-free biosensor technology based on surface plasmon resonance (SPR) is now sensitive and informative enough to serve during primary screens and validation steps. AREAS COVERED: In this review, the authors discuss the role of SPR in fragment screening. After a brief description of the underlying principles of the technique and main device developments, they evaluate the advantages and adaptations of SPR for fragment-based drug discovery. SPR can also be applied to challenging targets such as membrane receptors and enzymes. EXPERT OPINION: The high-level of immobilization of the protein target and its stability are key points for a relevant screening that can be optimized using oriented immobilized proteins and regenerable sensors. Furthermore, to decrease the rate of false negatives, a selectivity test may be performed in parallel on the main target bearing the binding site mutated or blocked with a low-off-rate ligand. Fragment-based drug design, integrated in a rational workflow led by SPR, will thus have a predominant role for the next wave of drug discovery which could be greatly enhanced by new improvements in SPR devices.
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Dates et versions

hal-02295396 , version 1 (24-09-2019)



Alain Chavanieu, Martine Pugnière. Developments in SPR Fragment Screening. Expert Opinion on Drug Discovery, 2016, 11 (5), pp.489-499. ⟨10.1517/17460441.2016.1160888⟩. ⟨hal-02295396⟩
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