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PROTAC-Induced Proteolytic Targeting

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Ubiquitin Family Modifiers and the Proteasome

Part of the book series: Methods in Molecular Biology ((MIMB,volume 832))

Abstract

Small-molecule modulators of protein activity are increasingly being utilized as tools to examine the functional roles of proteins. Operating at the post-translational level, these molecules provide enhanced temporal and spatial control and mitigate the potential for compensatory responses in comparison with classical genetic approaches. Proteolysis targeting chimeric molecules, or PROTACs, are small molecules that inhibit the function of their target proteins by targeting them for degradation by the ubiquitin proteasome system. This chapter summarizes strategies for PROTAC preparation and characterization.

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Acknowledgments

This work was supported by NIH grants R01 CA128903 and R01 ES014849 to KBK.

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Correspondence to Kyung-Bo Kim .

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© 2012 Springer Science+Business Media, LLC

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Carmony, K.C., Kim, KB. (2012). PROTAC-Induced Proteolytic Targeting. In: Dohmen, R., Scheffner, M. (eds) Ubiquitin Family Modifiers and the Proteasome. Methods in Molecular Biology, vol 832. Humana Press. https://doi.org/10.1007/978-1-61779-474-2_44

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  • DOI: https://doi.org/10.1007/978-1-61779-474-2_44

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  • Publisher Name: Humana Press

  • Print ISBN: 978-1-61779-473-5

  • Online ISBN: 978-1-61779-474-2

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