Combining 'dry' co-crystallization and in situ diffraction to facilitate ligand screening by X-ray crystallography. - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Acta crystallographica Section D : Structural biology [1993-...] Année : 2015

Combining 'dry' co-crystallization and in situ diffraction to facilitate ligand screening by X-ray crystallography.

Résumé

X-ray crystallography is an established technique for ligand screening in fragment-based drug-design projects, but the required manual handling steps - soaking crystals with ligand and the subsequent harvesting - are tedious and limit the throughput of the process. Here, an alternative approach is reported: crystallization plates are pre-coated with potential binders prior to protein crystallization and X-ray diffraction is performed directly 'in situ' (or in-plate). Its performance is demonstrated on distinct and relevant therapeutic targets currently being studied for ligand screening by X-ray crystallography using either a bending-magnet beamline or a rotating-anode generator. The possibility of using DMSO stock solutions of the ligands to be coated opens up a route to screening most chemical libraries.

Dates et versions

hal-01234554 , version 1 (27-11-2015)

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Citer

Muriel Gelin, Vanessa Delfosse, Frédéric Allemand, François Hoh, Yoann Sallaz-Damaz, et al.. Combining 'dry' co-crystallization and in situ diffraction to facilitate ligand screening by X-ray crystallography.. Acta crystallographica Section D : Structural biology [1993-..], 2015, 71 (Pt 8), pp.1777-87. ⟨10.1107/S1399004715010342⟩. ⟨hal-01234554⟩
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