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SGN-CD33A: a novel CD33-targeting antibody-drug conjugate using a pyrrolobenzodiazepine dimer is active in models of drug-resistant AML.
Mechanistic studies indicate that the cytotoxic effects of SGN-CD33A involve DNA damage with ensuing cell cycle arrest and apoptotic cell death, and suggest that S GN-CD 33A has CD33-directed antitumor activity and support clinical testing of this novel therapeutic in patients with AML.
Contribution of linker stability to the activities of anticancer immunoconjugates.
The data indicate that new linkers can be obtained with improved in vivo stability by replacing the maleimide with an acetamide, but the resulting ADCs had similar tolerability and activity profiles.
Development of orally active inhibitors of protein and cellular fucosylation
- N. Okeley, S. Alley, P. Senter
- Biology, ChemistryProceedings of the National Academy of Sciences
- 14 March 2013
Oral 2-fluorofucose treatment afforded complete protection from tumor engraftment in a syngeneic tumor vaccine model, inhibited neutrophil extravasation, and delayed the outgrowth of tumor xenografts in immune-deficient mice.
Design, synthesis, and in vitro evaluation of dipeptide-based antibody minor groove binder conjugates.
In vitro cytotoxicity assays established that the mAb-MGB drug conjugates were highly cytotoxic and effected immunologically specific cell kill at subsaturating doses.
Optimization of a PEGylated Glucuronide-Monomethylauristatin E Linker for Antibody–Drug Conjugates
This work optimized the drug-linker by minimizing the size of the PEG side chain and incorporating a self-stabilizing maleimide to prevent payload de-conjugation in vivo, enabling highly potent, homogeneous DAR 8 conjugates and is under consideration for future ADC programs.
A potent anti-CD70 antibody-drug conjugate combining a dimeric pyrrolobenzodiazepine drug with site-specific conjugation technology.
In vitro cytotoxicity experiments demonstrated that the h1F6239C-PBD was potent and immunologically specific on CD70-positive renal cell carcinoma (RCC) and non-Hodgkin lymphoma (NHL) cell lines, demonstrating that PBDs can be effectively used for antibody-targeted therapy.
Dipeptide-based highly potent doxorubicin antibody conjugates.
Development and properties of beta-glucuronide linkers for monoclonal antibody-drug conjugates.
Results demonstrate that the beta-glucuronide linker system is an effective strategy for targeting cytotoxic agents providing ADCs with high degrees of efficacy at well-tolerated doses.
Metabolic engineering of monoclonal antibody carbohydrates for antibody-drug conjugation.
A library of fucose analogues was evaluated and a thiolated analogue, 6-thiofucose, which was incorporated into the antibody carbohydrate with good efficiency and could be used for conjugation using maleimide chemistry to produce antibody-drug conjugates with pronounced cytotoxic activities and improved homogeneity compared to drug attachment through hinge disulfides.
Design, synthesis, and biological evaluation of antibody-drug conjugates comprised of potent camptothecin analogues.
ADCs bearing the potent camptothecin analogue, 7-butyl-9-amino-10,11-methylenedioxy-camptothein, were highly potent and immunologically specific on a panel of cancer cell lines in vitro, and efficacious at well-tolerated doses in a renal cell carcinoma xenograft model.