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Biophysical techniques for ligand screening and drug design.

Abstract : Biophysical methods are currently involved in drug design in two ways: the qualitative detection of small molecule binding to a target (hit identification), and the quantitative determination of physical parameters associated to binding (hit-to-lead progression). In the first case, efforts have been made toward miniaturization, automation, and speed-up of the screening process allowing a higher throughput. In the second one, sophisticated applications have been developed to derive detailed relevant information. Preferably, several methods are used in combination to avoid bias and/or limitations associated with a single one, often together with computational methods. New developments should allow important systems overlooked so far to be studied: membrane proteins, intrinsically unstructured proteins, as well as in-cell studies.
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Submitted on : Friday, December 4, 2009 - 12:00:52 PM
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Jean-Paul Renaud, Marc-André Delsuc. Biophysical techniques for ligand screening and drug design.. Current Opinion in Pharmacology, Elsevier, 2009, 9 (5), pp.622-8. ⟨10.1016/j.coph.2009.06.008⟩. ⟨inserm-00438664⟩



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