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Site-Specific Protein Labeling in the Pharmaceutical Industry: Experiences from Novartis Drug Discovery

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Book cover Site-Specific Protein Labeling

Part of the book series: Methods in Molecular Biology ((MIMB,volume 1266))

Abstract

Chemically modified proteins play an important role in several fields of pharmaceutical R&D, starting from various activities in drug discovery all the way down to biopharmaceuticals with improved properties such as antibody–drug conjugates. In the first part of the present chapter the significance and use of labeled proteins in biophysical methods, biochemical and cellular assays, in vivo imaging, and biopharmaceuticals is reviewed in general. In this context, the most relevant methods for site-specific modification of proteins and their application are also described. In the second part of the chapter, in-house (Novartis) results and experience with different techniques for selective protein labeling are discussed, with a focus on chemical or enzymatic (Avi-tag) biotinylation of proteins and their application in biophysical and biochemical assays. It can be concluded that while modern methods of site-specific protein labeling offer new possibilities for pharmaceutical R&D, classical methods are still the mainstay mainly due to being well established. However, site-specific protein labeling is expected to increase in importance, in particular for antibody–drug conjugates and other chemically modified biopharmaceuticals.

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Acknowledgements

I would like to thank the following colleagues: Jutta Blank, Marjo, Goette, Christian Bergsdorf, and Rainer Kneuer who gave valuable input and discussion in terms of performed experiments and general approaches in their respective field of expertise.

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Authors and Affiliations

  1. Center for Proteomic Chemistry, Novartis Institutes for Biomedical Research, Novartis Campus, 4056, Basel, Switzerland

    Lukas Leder

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  1. Lukas Leder
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Correspondence to Lukas Leder .

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Editors and Affiliations

  1. Department of Chemistry, École Normale Supérieure, Paris, France

    Arnaud Gautier

  2. Sensitive Farbstoffe GbR, Munich, Germany

    Marlon J. Hinner

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Leder, L. (2015). Site-Specific Protein Labeling in the Pharmaceutical Industry: Experiences from Novartis Drug Discovery. In: Gautier, A., Hinner, M. (eds) Site-Specific Protein Labeling. Methods in Molecular Biology, vol 1266. Humana Press, New York, NY. https://doi.org/10.1007/978-1-4939-2272-7_2

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