The DOI matches its Crossref record; 102 of the 102 references it cites were found in a registry or an index.
Site-Specific Antibody–Drug Conjugates: The Nexus of Bioorthogonal Chemistry, Protein Engineering, and Drug Development
Open accessAbstract
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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Cites
Characterization of Mammalian Selenoproteomes
Kryukov, G. V., Castellano, S., Novoselov, S. V., Lobanov, A. V., Zehtab, O., Guigó, R., & Gladyshev, V. N. (2003) · Science · doi:10.1126/science.1083516 · Cited by 2,351
Adding New Chemistries to the Genetic Code
Liu, C. C., & Schultz, P. G. (2010) · Annual Review of Biochemistry · doi:10.1146/annurev.biochem.052308.105824 · Cited by 1,725
Targeting HER2-Positive Breast Cancer with Trastuzumab-DM1, an Antibody–Cytotoxic Drug Conjugate
Lewis Phillips, G. D., Li, G., Dugger, D. L., Crocker, L. M., Parsons, K. L., Mai, E., Blättler, W. A., Lambert, J. M., Chari, R. V. J., Lutz, R. J., et al. (2008) · Cancer Research · doi:10.1158/0008-5472.can-08-1776 · Cited by 1,676
Site-specific conjugation of a cytotoxic drug to an antibody improves the therapeutic index
Junutula, J. R., Raab, H., Clark, S., Bhakta, S., Leipold, D. D., Weir, S., Chen, Y., Simpson, M., Tsai, S. P., Dennis, M. S., et al. (2008) · Nature Biotechnology · doi:10.1038/nbt.1480 · Cited by 1,382
Effects of Drug Loading on the Antitumor Activity of a Monoclonal Antibody Drug Conjugate
Hamblett, K. J., Senter, P. D., Chace, D. F., Sun, M. M. C., Lenox, J., Cerveny, C. G., Kissler, K. M., Bernhardt, S. X., Kopcha, A. K., Zabinski, R. F., et al. (2004) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-04-0789 · Cited by 1,247
Development of potent monoclonal antibody auristatin conjugates for cancer therapy
Doronina, S. O., Toki, B. E., Torgov, M. Y., Mendelsohn, B. A., Cerveny, C. G., Chace, D. F., DeBlanc, R. L., Gearing, R. P., Bovee, T. D., Siegall, C. B., et al. (2003) · Nature Biotechnology · doi:10.1038/nbt832 · Cited by 1,206
Parekh, R. B., Dwek, R. A., Sutton, B. J., Fernandes, D. L., Leung, A., Stanworth, D., Rademacher, T. W., Mizuochi, T., Taniguchi, T., Matsuta, K., et al. (1985) · Nature · doi:10.1038/316452a0 · Cited by 1,170
Cellular Incorporation of Unnatural Amino Acids and Bioorthogonal Labeling of Proteins
Lang, K., & Chin, J. W. (2014) · Chemical Reviews · doi:10.1021/cr400355w · Cited by 1,035
Shen, B.-Q., Xu, K., Liu, L., Raab, H., Bhakta, S., Kenrick, M., Parsons-Reponte, K. L., Tien, J., Yu, S.-F., Mai, E., et al. (2012) · Nature Biotechnology · doi:10.1038/nbt.2108 · Cited by 1,008
Antibody–Drug Conjugates: An Emerging Concept in Cancer Therapy
Chari, R. V. J., Miller, M. L., & Widdison, W. C. (2014) · Angewandte Chemie International Edition · doi:10.1002/anie.201307628 · Cited by 930
Cited by
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Beck, A., Goetsch, L., Dumontet, C., & Corvaïa, N. (2017) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2016.268 · Cited by 2,271
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Fu, Z., Li, S., Han, S., Shi, C., & Zhang, Y. (2022) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-022-00947-7 · Cited by 1,643
Transport of drugs from blood vessels to tumour tissue
Dewhirst, M. W., & Secomb, T. W. (2017) · Nature Reviews Cancer · doi:10.1038/nrc.2017.93 · Cited by 749
Scinto, S. L., Bilodeau, D. A., Hincapie, R., Lee, W., Nguyen, S. S., Xu, M., am Ende, C. W., Finn, M. G., Lang, K., Lin, Q., et al. (2021) · Nature Reviews Methods Primers · doi:10.1038/s43586-021-00028-z · Cited by 592
Redox-based reagents for chemoselective methionine bioconjugation
Lin, S., Yang, X., Jia, S., Weeks, A. M., Hornsby, M., Lee, P. S., Nichiporuk, R. V., Iavarone, A. T., Wells, J. A., Toste, F. D., et al. (2017) · Science · doi:10.1126/science.aal3316 · Cited by 513
Metadata
- 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
- OpenAlex
- W1984111577
- Cited by
- 605
- References
- 102
- FWCI
- 36.80
- Type
- journal article
- Language
- en
- Open access
- hybrid
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