title: Biophysics in drug discovery: impact, challenges and opportunities.
abstract: Over the past 25 years, biophysical technologies such as X-ray crystallography, nuclear magnetic resonance spectroscopy, surface plasmon resonance spectroscopy and isothermal titration calorimetry have become key components of drug discovery platforms in many pharmaceutical companies and academic laboratories. There have been great improvements in the speed, sensitivity and range of possible measurements, providing high-resolution mechanistic, kinetic, thermodynamic and structural information on compound-target interactions. This Review provides a framework to understand this evolution by describing the key biophysical methods, the information they can provide and the ways in which they can be applied at different stages of the drug discovery process. We also discuss the challenges for current technologies and future opportunities to use biophysical methods to solve drug discovery problems.
authors: NovAliX, Boulevard Sébastien Brant, 67405 Illkirch Cedex, France.|Institut de Génétique et Biologie Moléculaire et Cellulaire, CNRS UMR7104/INSERM U964/Université de Strasbourg, 1 rue Laurent Fries - BP10142, 67404 Illkirch Cedex, France.|RiboStruct, 15 rue Neuve, 67540 Ostwald, France.
authors: Jean-Paul
authors: JP
authors: Renaud
authors: GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage, SG1 2NY, UK.
authors: Chun-Wa
authors: CW
authors: Chung
authors: Department of Chemistry - BMC and Science for Life Laboratory, Drug Discovery &Development Platform, Uppsala University, SE-751 05 Uppsala, Sweden.|Beactica AB, Uppsala Business Park, 754 50 Uppsala, Sweden.
authors: U Helena
authors: UH
authors: Danielson
authors: Bayer Pharma AG, Müllerstrasse 178, 13353 Berlin, Germany.
authors: Ursula
authors: U
authors: Egner
authors: Hoffmann-La Roche Ltd, Grenzacherstrasse 124, 4070 Basel, Switzerland.|leadXpro AG, PARK INNOVAARE, CH-5234 Villigen, Switzerland.
authors: Michael
authors: M
authors: Hennig
authors: University of York, Heslington, York, YO10 5DD, UK.|Vernalis (R&D), Granta Park, Cambridge, CB21 6GB, UK.
authors: Roderick E
authors: RE
authors: Hubbard
authors: Boehringer Ingelheim GmbH &Co. KG, Birkendorfer Strasse 65, 88400 Biberach, Germany.
authors: Herbert
authors: H
authors: Nar
mesh_terms: D000818:Animals; D055592:Biophysical Phenomena / Q000187:drug effects* / Q000502:physiology; D002151:Calorimetry / Q000379:methods / Q000639:trends; D015195:Drug Design; D055808:Drug Discovery / Q000379:methods* / Q000639:trends; D004353:Drug Evaluation, Preclinical / Q000379:methods / Q000639:trends; D057166:High-Throughput Screening Assays / Q000379:methods / Q000639:trends; D006801:Humans; D004364:Pharmaceutical Preparations / Q000008:administration & dosage; D020349:Surface Plasmon Resonance / Q000379:methods / Q000639:trends
chemical_list: D004364:Pharmaceutical Preparations