亚铁活化药物偶联在kras驱动的肿瘤中实现有效的MAPK阻断

The Tokushima journal of experimental medicine Pub Date : 2022-03-09 DOI:10.1084/jem.20210739

Honglin Jiang, Ryan K Muir, R. Gonciarz, A. Olshen, I. Yeh, B. Hann, Ning Zhao, Yung-hua Wang, S. Behr, J. Korkola, M. Evans, E. Collisson, A. Renslo

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引用次数: 12

摘要

Jiang等人报道，在KRAS介导的突变体转化过程中，致癌KRAS信号传导诱导亚铁(Fe2+)积累。将fda批准的MEK抑制剂转化为亚铁活化药物偶联物(FeADC)，可在肿瘤细胞中实现有效的MAPK阻断，并具有优越的全身耐受性。

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Ferrous iron–activatable drug conjugate achieves potent MAPK blockade in KRAS-driven tumors

Jiang et al. report that oncogenic KRAS signaling induces ferrous iron (Fe2+) accumulation throughout mutant KRAS-mediated transformation. Converting an FDA-approved MEK inhibitor into a ferrous iron–activatable drug conjugate (FeADC) achieves potent MAPK blockade in tumor cells with superior systemic tolerability.

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The Tokushima journal of experimental medicine

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