SAR by ILOEs: An NMR‐Based Approach to Reverse Chemical Genetics
- 10 March 2006
- journal article
- concept
- Published by Wiley in Chemistry – A European Journal
- Vol. 12 (10) , 2658-2662
- https://doi.org/10.1002/chem.200500636
Abstract
Reverse chemical genetics is an emerging technique that makes use of small molecule inhibitors to characterize how a protein functions. In this regard, we have developed an NMR‐based approach (SAR by ILOEs) that enables the identification of high affinity ligands for a given protein target without the need of a specific assay. Our approach is of general applicability and could result very powerful in reverse chemical‐genetics studies, target validation, and lead discovery. We report a recent application on the design and synthesis of compounds that inhibit protein‐membrane interactions.Keywords
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