2016
DOI: 10.1016/j.bmcl.2016.08.082
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Wide application of a novel topoisomerase I inhibitor-based drug conjugation technology

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Cited by 36 publications
(17 citation statements)
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“…Researchers explored the antitumor ability of the antibody-drug conjugates (ADCs) that specifically destroyed B7-H3 positive expressing tumors, and found that established tumors and metastases were eradicated, and overall survival improved significantly, which demonstrate the anti-CD276-drug conjugates as promising reagents for highly selective broad-acting anti-cancer therapies [52]. A promising exatecan derivative (DX-8951 derivative, DXd), used for drug conjugation as DXd-ADC targeting B7-H3, showed effective antitumor efficacy as well as less adverse effects [53]. 131I-labeled anti-B7-H3 mAb (131I-4H7) had radiobiological and treatment effects on nude mice with human RCC.…”
Section: Targeting B7-h3 Therapymentioning
confidence: 95%
“…Researchers explored the antitumor ability of the antibody-drug conjugates (ADCs) that specifically destroyed B7-H3 positive expressing tumors, and found that established tumors and metastases were eradicated, and overall survival improved significantly, which demonstrate the anti-CD276-drug conjugates as promising reagents for highly selective broad-acting anti-cancer therapies [52]. A promising exatecan derivative (DX-8951 derivative, DXd), used for drug conjugation as DXd-ADC targeting B7-H3, showed effective antitumor efficacy as well as less adverse effects [53]. 131I-labeled anti-B7-H3 mAb (131I-4H7) had radiobiological and treatment effects on nude mice with human RCC.…”
Section: Targeting B7-h3 Therapymentioning
confidence: 95%
“…Trastuzumab is conjugated to the antibody via a tetrapeptide linker, Gly-Gly-Phe-Gly ( Figure 10), which is cleavable by lysozymes [69]. The linker is connected to a Cys residue of the mAb through a maleimidocarpoyl component [66] and to a self-immolative amino methylene (AM) spacer [70].…”
Section: Gly-gly-phe-glymentioning
confidence: 99%
“…There are six HER2-based ADCs in clinical trials aimed to improve the activity and maintain or enhance the T-DM1 immunity. Moreover, the utilization of the following cytotoxic drugs with different actions has been assessed: DS-8201a for the transmission of exatecan, a topoisomerase inhibitor [113][114][115][116] , and SYD985 [117,118] , a DNA-alkylating drug [119,120] , as well as ADCT-502 for the transmission of pyrrolobenzodiazepine that enters DNA minor grooves [121] .…”
Section: Adoptive Immunotherapy With Mabs and Adcsmentioning
confidence: 99%
“…This ADC shows a cell-related HER2 toxicity effect in laboratory conditions in pancreatic, breast, and gastric cancer cells. Human model studies have also indicated HER2specific activity in tumors with heterogeneous expression of HER2 [114,115] . This ADC has entered in phase 1 of clinical trial.…”
Section: Ds8201-amentioning
confidence: 99%