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SAR by ILOEs: an NMR-based approach to reverse chemical genetics.

Becattini B, Pellecchia M

The Burnham Institute, 10901 North Torrey Pines Rd. La Jolla, CA 92037, USA.

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.

Published 15 March 2006 in Chemistry, 12(10): 2658-62.
Full-text of this article is available online (may require subscription).

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NMR Research Today Archive:

Volume 1 (2005)
  Issue 1 (September)
  Issue 2 (October)
  Issue 3 (November)
  Issue 4 (December)

Volume 2 (2006)
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Volume 3 (2007)
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Volume 4 (2008)
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NMR Books

Pocket Atlas of Sectional Anatomy, Computed Tomography and Magnetic Resonance Imaing, Vol. 1: Head and Neck

Pocket Atlas of Sectional Anatomy, Computed Tomography and Magnetic Resonance Imaing, Vol. 1: Head and Neck