NMR in drug discovery on membrane proteins

Author:

Wirmer-Bartoschek Julia1,Bartoschek Stefan2

Affiliation:

1. Institute for Organic Chemistry & Chemical Biology, Center of Biomolecular Magnetic Resonance, Johann Wolfgang Goethe University, Max-von-Laue-Straße 7, D-60439 Frankfurt am Main, Germany

2. LGCR/Department of Parallel Synthesis & Natural Product Sciences, Sanofi-Aventis Deutschland GmbH, Industriepark Hoechst, Bldg. H811, D-65926 Frankfurt am Main, Germany.

Abstract

Drug discovery on membrane proteins is still a difficult task, despite the recognized importance of membrane proteins as drug targets. Here, we present an overview of NMR methods available for structure-based drug design on membrane proteins. NMR spectroscopy is capable of identifying potential binders in screening and defining their relative binding constants, binding stoichiometry, conformation in the binding pocket and the relative binding orientation for binders of different series. Examples are given in the review highlighting the potential of NMR spectroscopy for future progress in drug discovery on membrane proteins.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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