Evaluation of Potency and Specificity of Cryptophycin-Loaded Antibody-Drug Conjugates
Kolmar H, Bitsch P, Dessin C, Bitsch S, Becker J, Voss J, Sharma P, Biyani N, Kochat H, Sewald N (2024)
ChemBioChem .
Zeitschriftenaufsatz
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Autor*in
Kolmar, Harald;
Bitsch, Peter;
Dessin, CedricUniBi;
Bitsch, Sebastian;
Becker, Janine;
Voss, JonaUniBi ;
Sharma, Panna;
Biyani, Neha;
Kochat, Harry;
Sewald, NorbertUniBi
Einrichtung
Abstract / Bemerkung
An enhanced variant of the antimitotic toxin cryptophycin was conjugated to the anti-Her2 monoclonal antibody (mAb) Trastuzumab upon Michael addition. Either antibodies with freed hinge-region cysteines or THIOMAB formats with engineered cysteines in the mAbs light chain were added to a maleimide derivative of cryptophycin. These Antibody-Drug Conjugates (ADCs) showed retained binding to Her2 positive tumor cells and highly efficient cell killing in double-digit pM range on high Her2-expressing SK-BR-3 cells. Two ADCs (DAR6, DAR3) showed superior cell killing of the cell lines JIMT-1 and RT112 with medium receptor expression level in comparison with a DAR6 MMAE ADC serving as reference. The observed cell cytotoxicity is target-dependent since no impact on cell viability was observed for low Her2-expressing MDA-MB468 cells. Particularly the DAR3 ADC in THIOMAB format exhibiting desirable biophysical properties and high potency emerged as a promising candidate for further in vivo investigations. © 2024 Wiley‐VCH GmbH.
Erscheinungsjahr
2024
Zeitschriftentitel
ChemBioChem
eISSN
1439-7633
Page URI
https://pub.uni-bielefeld.de/record/2994028
Zitieren
Kolmar H, Bitsch P, Dessin C, et al. Evaluation of Potency and Specificity of Cryptophycin-Loaded Antibody-Drug Conjugates. ChemBioChem . 2024.
Kolmar, H., Bitsch, P., Dessin, C., Bitsch, S., Becker, J., Voss, J., Sharma, P., et al. (2024). Evaluation of Potency and Specificity of Cryptophycin-Loaded Antibody-Drug Conjugates. ChemBioChem . https://doi.org/10.1002/cbic.202400738
Kolmar, Harald, Bitsch, Peter, Dessin, Cedric, Bitsch, Sebastian, Becker, Janine, Voss, Jona, Sharma, Panna, Biyani, Neha, Kochat, Harry, and Sewald, Norbert. 2024. “Evaluation of Potency and Specificity of Cryptophycin-Loaded Antibody-Drug Conjugates”. ChemBioChem .
Kolmar, H., Bitsch, P., Dessin, C., Bitsch, S., Becker, J., Voss, J., Sharma, P., Biyani, N., Kochat, H., and Sewald, N. (2024). Evaluation of Potency and Specificity of Cryptophycin-Loaded Antibody-Drug Conjugates. ChemBioChem .
Kolmar, H., et al., 2024. Evaluation of Potency and Specificity of Cryptophycin-Loaded Antibody-Drug Conjugates. ChemBioChem .
H. Kolmar, et al., “Evaluation of Potency and Specificity of Cryptophycin-Loaded Antibody-Drug Conjugates”, ChemBioChem , 2024.
Kolmar, H., Bitsch, P., Dessin, C., Bitsch, S., Becker, J., Voss, J., Sharma, P., Biyani, N., Kochat, H., Sewald, N.: Evaluation of Potency and Specificity of Cryptophycin-Loaded Antibody-Drug Conjugates. ChemBioChem . (2024).
Kolmar, Harald, Bitsch, Peter, Dessin, Cedric, Bitsch, Sebastian, Becker, Janine, Voss, Jona, Sharma, Panna, Biyani, Neha, Kochat, Harry, and Sewald, Norbert. “Evaluation of Potency and Specificity of Cryptophycin-Loaded Antibody-Drug Conjugates”. ChemBioChem (2024).
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