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Article Abstract
Extracellular signal-regulated kinase 5 (ERK5) is recognized as a key member of the mitogen-activated protein kinase family and is involved in tumor growth, migration, and angiogenesis. However, the results of ERK5 inhibition in multiple studies are controversial, and a highly specific ERK5-targeting agent is required to confirm physiological functions. Using proteolysis-targeting chimera technology, we designed the selective ERK5 degrader and examined its biological effect on cancer cells. Interestingly, the selective degradation of ERK5 with did not influence tumor cell growth directly. Based on proteomics analysis, the ERK5 deletion may be associated with tumor immunity. influences tumor development by affecting the differentiation of macrophages. Therefore, is an effective small-molecule tool for studying ERK5 and a promising immunotherapy drug candidate.
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| http://dx.doi.org/10.1021/acs.jmedchem.3c00864 | DOI Listing |
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