Design, Synthesis, and in Vitro Evaluation of Dipeptide-Based Antibody Minor Groove Binder Conjugates

Antibody−drug conjugates (ADCs) were prepared consisting of DNA minor groove binder drugs (MGBs) attached to monoclonal antibodies (mAbs) through peptide linkers designed to release drugs inside the lysosomes of target cells. The site of linker attachment on the MGB was at the 5-position on the B-ri...

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Veröffentlicht in:	Journal of medicinal chemistry 2005-03, Vol.48 (5), p.1344-1358
Hauptverfasser:	Jeffrey, Scott C, Torgov, Michael Y, Andreyka, Jamie B, Boddington, Laura, Cerveny, Charles G, Denny, William A, Gordon, Kristine A, Gustin, Darin, Haugen, Jennifer, Kline, Toni, Nguyen, Minh T, Senter, Peter D
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antibodies, Monoclonal - chemistry Antineoplastic agents Antineoplastic Agents, Alkylating - chemical synthesis Antineoplastic Agents, Alkylating - chemistry Antineoplastic Agents, Alkylating - pharmacology Aza Compounds - chemical synthesis Aza Compounds - chemistry Aza Compounds - pharmacology Biological and medical sciences Cathepsin B - chemistry Cell Line, Tumor Cyclopropanes - chemical synthesis Cyclopropanes - chemistry Cyclopropanes - pharmacology Dipeptides - chemistry DNA - chemistry Drug Design Drug Screening Assays, Antitumor General aspects Humans Immunoconjugates - chemistry Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Medical sciences Mice Pharmacology. Drug treatments Structure-Activity Relationship
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