Journal
CURRENT OPINION IN STRUCTURAL BIOLOGY
Volume 21, Issue 2, Pages 189-199Publisher
CURRENT BIOLOGY LTD
DOI: 10.1016/j.sbi.2011.01.004
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Funding
- National Institutes of Health [GM078596]
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Here off-target binding implies the binding of a small molecule of therapeutic interest to a protein target other than the primary. target for which it was intended. Increasingly such off-targeting appears to be the norm rather than the exception, rational drug design notwithstanding, and can lead to detrimental side-effects, or opportunities to reposition a therapeutic agent to treat a different condition. Not surprisingly, there is significant interest in determining a priori what off-targets exist on a proteome-wide scale. Beyond determining putative off-targets is the need to understand the impact of such binding on the complete biological system, with the ultimate goal of being able to predict the phenotypic outcome. While a very ambitious goal, some progress is being made.
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