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Article

Inhibition of a lower potency target drives the anticancer activity of a clinical p38 inhibitor.

Cell chemical biology - 19 Oct 2023

Bhattacharjee Debanjan, Bakar Jaweria, Chitnis Surbhi P, Sausville Erin L, Ashtekar Kumar Dilip, Mendelson Brianna E, Long Kaitlin, Smith Joan C, Heppner David E, Sheltzer Jason M

Abstract excerpt

The small-molecule drug ralimetinib was developed as an inhibitor of the p38α mitogen-activated protein kinase, and it has advanced to phase 2 clinical trials in oncology. Here, we demonstrate that ralimetinib resembles EGFR-targeting drugs in pharmacogenomic profiling experiments and that ralimetinib inhibits EGFR kinase activity in vitro and in cellulo. While ralimetinib sensitivity is unaffected by deletion of...

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Identifiers

PMID: 37827156
DOI: 10.1016/j.chembiol.2023.09.013
PMCID: PMC10715717

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