Antibody drug conjugates of cleavable amino-benzoyl-maytansinoids.
Bioorg Med Chem
; 28(23): 115785, 2020 12 01.
Article
em En
| MEDLINE
| ID: mdl-33099182
ABSTRACT
ADCs based on the natural product maytansine have been successfully employed clinically. In a previous report, ADCs based on hydrophilic non-cell permeable maytansinoids was presented. The authors in this report further explore the maytansine scaffold to develop tubulin inhibitors capable of cell permeation. The research resulted in amino-benzoyl-maytansinoid payloads that were further elaborated with linkers for conjugating to antibodies. This approach was applied to MUC16 tumor targeting antibodies for ovarian cancers. A positive control ADC was evaluated alongside the amino-benzoyl-maytansinoid ADC and the efficacy observed was equivalent while the isotype control ADCs had no effect.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Imunoconjugados
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Moduladores de Tubulina
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Maitansina
Limite:
Animals
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Female
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Humans
Idioma:
En
Revista:
Bioorg Med Chem
Ano de publicação:
2020
Tipo de documento:
Article