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LINGO1-targeted antibody-drug conjugates improve efficacy and tolerability of antineoplastic therapies in Ewing sarcoma models
Zhichuan Zhu, Yusha Liu, Yu Deng, Zhijun Li, Albert S. Baldwin, Pengda Liu
Zhichuan Zhu, Yusha Liu, Yu Deng, Zhijun Li, Albert S. Baldwin, Pengda Liu
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Research Letter Cell biology Oncology

LINGO1-targeted antibody-drug conjugates improve efficacy and tolerability of antineoplastic therapies in Ewing sarcoma models

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Abstract

Authors

Zhichuan Zhu, Yusha Liu, Yu Deng, Zhijun Li, Albert S. Baldwin, Pengda Liu

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Figure 1

LINGO1-targeted opicinumab-MMAE ADCs show anti–Ewing sarcoma efficacy with reduced toxicity in vivo.

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LINGO1-targeted opicinumab-MMAE ADCs show anti–Ewing sarcoma efficacy wi...
(A) Venn diagram showing overlapping Ewing sarcoma cell-surface markers identified from 3 independent datasets: the Human Protein Atlas (blue), Ewing sarcoma–focused surface proteomics (red), and curated EWS:FLI1 target genes (green). (B) DepMap waterfall plot demonstrating cell viability changes following CRISPR-mediated LINGO1 depletion. (C) FACS analysis of cell-surface LINGO1 expression in indicated Ewing sarcoma cells. (D) Immunoblot for apoptosis markers in MHH-ES-1 cells 3 days after opicinumab-SN38 treatment. (E and F) Tumor volumes and weights of MHH-ES-1 xenografts (n = 10) treated with indicated agents. Arrows indicate treatments. (G) Body weights of mice from E and F. n = 5. (H) MMAE biodistribution 7 days after opicinumab-MMAE treatment. n = 5. (I and J) Tumor volumes and weights of TC-32 xenografts treated with indicated agents. n = 10 (vehicle), 8 (MMAE and opicinumab-MMAE), and 9 (irinotecan). (K and L) Serum concentrations of opicinumab and opicinumab-MMAE in opicinumab-MMAE–treated mice. n = 4. (M) Alanine aminotransferase (ALT) activity on day 17 in mice from I and J. n = 4. (N) Mouse body weights from I and J. n = 5 (vehicle/irinotecan) and 4 (MMAE/opicinumab-MMAE). Data represent mean ± SEM. P values were calculated using 2-way ANOVA with Bonferroni’s test (E) or Tukey’s test (I and N), unpaired 2-tailed Mann-Whitney test (F), 1-way ANOVA with Dunnett’s test (H), and Kruskal-Wallis with Dunn’s test (J and M).

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