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Antibody-Drug Conjugates pp 189–203Cite as

Engineering THIOMABs for Site-Specific Conjugation of Thiol-Reactive Linkers

Part of the Methods in Molecular Biology book series (MIMB,volume 1045)

Abstract

Antibody conjugates are used in many therapeutic and research applications and are generated by chemically linking a cysteine or lysine residue to potent chemotherapeutic drugs or other functional groups through a flexible linker. Recently, we have engineered THIOMABs (antibodies with engineered reactive cysteine residues) for site-specific conjugation and showed that these antibody conjugates display homogeneous labeling with optimal in vitro and in vivo characteristics. Here, we describe protocols for engineering, selection, and site-specific conjugation of THIOMABs with thiol-reactive linkers.

Key words

  • Antibody conjugate
  • THIOMAB
  • Site-specific conjugation
  • Antibody–drug conjugate (ADC)
  • Engineered ADCs

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Authors and Affiliations

  1. Genentech Inc., South San Francisco, CA, USA

    Sunil Bhakta, Helga Raab & Jagath R. Junutula

Authors
  1. Sunil Bhakta
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  2. Helga Raab
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  3. Jagath R. Junutula
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Editor information

Editors and Affiliations

  1. Lonza Ltd, Visp, Switzerland

    Laurent Ducry

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Bhakta, S., Raab, H., Junutula, J.R. (2013). Engineering THIOMABs for Site-Specific Conjugation of Thiol-Reactive Linkers. In: Ducry, L. (eds) Antibody-Drug Conjugates. Methods in Molecular Biology, vol 1045. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-62703-541-5_11

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  • DOI: https://doi.org/10.1007/978-1-62703-541-5_11

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  • Publisher Name: Humana Press, Totowa, NJ

  • Print ISBN: 978-1-62703-540-8

  • Online ISBN: 978-1-62703-541-5

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