Developments in SPR Fragment Screening
| Autor: | Martine Pugnière, Alain Chavanieu |
|---|---|
| Přispěvatelé: | Institut des Biomolécules Max Mousseron [Pôle Chimie Balard] (IBMM), Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)-Université de Montpellier (UM)-Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM), Institut de Recherche en Cancérologie de Montpellier (IRCM - U1194 Inserm - UM), CRLCC Val d'Aurelle - Paul Lamarque-Institut National de la Santé et de la Recherche Médicale (INSERM)-Université de Montpellier (UM) |
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Magnetic Resonance Spectroscopy education [SDV.CAN]Life Sciences [q-bio]/Cancer Nanotechnology Crystallography X-Ray 01 natural sciences 03 medical and health sciences MESH: Drug Discovery Fragment (logic) Drug Discovery Humans Immobilized proteins Surface plasmon resonance MESH: Humans MESH: Magnetic Resonance Spectroscopy Chemistry Drug discovery fragment screening Surface Plasmon Resonance MESH: Crystallography X-Ray MESH: Surface Plasmon Resonance 0104 chemical sciences 010404 medicinal & biomolecular chemistry 030104 developmental biology molecular interaction Fragment-based drug design Protein target Biosensor [SDV.MHEP]Life Sciences [q-bio]/Human health and pathology |
| Zdroj: | Expert Opinion on Drug Discovery Expert Opinion on Drug Discovery, Informa Healthcare, 2016, 11 (5), pp.489-499. ⟨10.1517/17460441.2016.1160888⟩ |
| ISSN: | 1746-045X 1746-0441 |
| DOI: | 10.1517/17460441.2016.1160888 |
| Popis: | International audience; 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. |
| Databáze: | OpenAIRE |
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