Most proteins in the human body are difficult targets for small-molecule drugs. This problem may have been overcome with the discovery of molecules that induce protein degradation, suggesting fresh, modular approaches to drug discovery.
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References
Neklesa, T. K. et al. Nature Chem. Biol. 7, 538–543 (2011).
Tae, H. S. et al. ChemBioChem 13, 538–541 (2012).
Long, M. J. C., Gollapalli, D. R. & Hedstrom, L. Chem. Biol. 19, 629–637 (2012).
Russ, A. P. & Lampel, S. Drug Discov. Today 10, 1607–1610 (2005).
Kauffman, M. G., Molineaux, C. J., Kirk, C. J. & Crews, C. M. in Cancer: Principles & Practice of Oncology (eds DeVita, V. T. Jr, Lawrence, T. S. & Rosenberg, S. A.) 441–449 (Lippincott Williams & Wilkins, 2011).
Schneekloth, J. S. Jr et al. J. Am. Chem. Soc. 126, 3748–3754 (2004).
Kleiner, R. E., Dumelin, C. E. & Liu, D. R. Chem. Soc. Rev. 40, 5707–5717 (2011).
Clark, M. A. et al. Nature Chem. Biol. 5, 647–654 (2009).
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Neklesa, T., Crews, C. Greasy tags for protein removal. Nature 487, 308–309 (2012). https://doi.org/10.1038/487308a
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DOI: https://doi.org/10.1038/487308a
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