Volume 53, Issue 40
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Cysteine‐Selective Reactions for Antibody Conjugation

Pedro M. S. D. Cal

Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649‐003 Lisboa (Portugal) http://www.ff.ul.pt/∼pedrogois/index.html

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Dr. Gonçalo J. L. Bernardes

Corresponding Author

E-mail address: gb453@cam.ac.uk

E-mail address: gbernardes@fm.ul.pt

Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW Cambridge (UK) http://gbernardes‐lab.com

Instituto de Medicina Molecular, Faculdade de Medicina da Universidade de Lisboa, Av. Prof. Egas Moniz, 1649‐028 Lisboa (Portugal)

Gonçalo J. L. Bernardes, Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW Cambridge (UK) http://gbernardes‐lab.com

Pedro M. P. Gois, Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649‐003 Lisboa (Portugal) http://www.ff.ul.pt/∼pedrogois/index.html

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Dr. Pedro M. P. Gois

Corresponding Author

E-mail address: pedrogois@ff.ul.pt

Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649‐003 Lisboa (Portugal) http://www.ff.ul.pt/∼pedrogois/index.html

Gonçalo J. L. Bernardes, Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW Cambridge (UK) http://gbernardes‐lab.com

Pedro M. P. Gois, Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649‐003 Lisboa (Portugal) http://www.ff.ul.pt/∼pedrogois/index.html

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First published: 28 July 2014
Citations: 68

P.M.S.D.C. and P.M.P.G. thank FCT (PTDC/QUI‐QUI/118315/2010, Pest‐OE/SAU/UI4013/2011, SFRH/BD/72376/2010) for financial support. G.J.L.B. is a Royal Society University Research Fellow and an FCT Investigator.

Abstract

Moving tracks from maleimide: New site‐selective protein modification reactions at cysteine have been developed. Unlike conventional maleimide conjugation, which results in a labile thioether succinimide, the new bioconjugation reactions result in stable conjugates and provide opportunities to develop a new generation of homogeneous, stable, and therapeutically useful conjugates.

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