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Site-Specific Antibody–Drug Conjugates: The Nexus of Bioorthogonal Chemistry, Protein Engineering, and Drug Development

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Agarwal, Paresh, Bertozzi, Carolyn R.·2015·Bioconjugate Chemistry

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Abstract

Antibody-drug conjugates (ADCs) combine the specificity of antibodies with the potency of small molecules to create targeted drugs. Despite the simplicity of this concept, generation of clinically successful ADCs has been very difficult. Over the past several decades, scientists have learned a great deal about the constraints on antibodies, linkers, and drugs as they relate to successful construction of ADCs. Once these components are in hand, most ADCs are prepared by nonspecific modification of antibody lysine or cysteine residues with drug-linker reagents, which results in heterogeneous product mixtures that cannot be further purified. With advances in the fields of bioorthogonal chemistry and protein engineering, there is growing interest in producing ADCs by site-specific conjugation to the antibody, yielding more homogeneous products that have demonstrated benefits over their heterogeneous counterparts in vivo. Here, we chronicle the development of a multitude of site-specific conjugation strategies for assembly of ADCs and provide a comprehensive account of key advances and their roots in the fields of bioorthogonal chemistry and protein engineering.

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Improving the Serum Stability of Site-Specific Antibody Conjugates with Sulfone Linkers
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Sortase-mediated modification of αDEC205 affords optimization of antigen presentation and immunization against a set of viral epitopes
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Bioorthogonal chemistry
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Redox-based reagents for chemoselective methionine bioconjugation
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See all 605

Authors: Agarwal, P., & Bertozzi, C. R.
Venue: Bioconjugate Chemistry
Publisher: American Chemical Society (ACS)
Published: 2015-01-30
Volume: 26
Issue: 2
Pages: 176-192
ISSN: 1043-1802 (ISSN-L)
1520-4812
DOI: 10.1021/bc5004982
OpenAlex: W1984111577
Cited by: 605
References: 102
FWCI: 36.80
Type: journal article
Language: en
Open access: hybrid

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Site-Specific Antibody–Drug Conjugates: The Nexus of Bioorthogonal Chemistry, Protein Engineering, and Drug Development

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