Article

A drug’s most potent target is not necessarily the source of its anti-cancer activity

2022-10-16

Abstract excerpt

<h4>ABSTRACT</h4> The small-molecule drug ralimetinib was developed as an inhibitor of the kinase p38α, and it has advanced to phase 2 clinical trials in oncology. Here, we apply a multi-modal approach to demonstrate that ralimetinib’s anti-cancer activity occurs due to its ability to inhibit EGFR, rather than p38α. We find that cancer cell lines driven by EGFR mutations exhibit the greatest sensitivity to ralime...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: ecad24b2-dd29-5d24-ad57-d8ef1f8b1762
DOI: 10.1101/2022.10.16.512438

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

A drug’s most potent target is not necessarily the source of its anti-cancer activityDOI 10.1101/2022.10.16.512438Read

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

Durability of Kinase-Directed Therapies—A Network Perspective on Response and ResistanceSemantic proximity Read

Tyrosine kinase inhibitors - small molecular weight compounds inhibiting EGFR.Semantic proximity Read

Targeted Therapies in Cancer: To Be or Not to Be, SelectiveSemantic proximity Read

Combined Cellular and Biochemical Profiling to Identify Predictive Drug Response Biomarkers for Kinase Inhibitors Approved for Clinical Use between 2013 and 2017Semantic proximity Read

Polypharmacology is an enduring and nearly universal property of kinase inhibitorsSemantic proximity Read

Tyrosine phosphoproteome profiling identifies cell-intrinsic signals limiting the efficacy of tyrosine kinase inhibitor therapiesSemantic proximity Read

Dissecting sources of variability in patient response to targeted therapy: anti-HER2 therapies as a case studySemantic proximity Read

ERK Inhibition: A New Front in the War against MAPK Pathway-Driven Cancers?Semantic proximity Read

Rational Discovery of Dual-Action Multi-Target Kinase Inhibitor for Precision Anti-Cancer Therapy Using Structural Systems PharmacologySemantic proximity Read

First-in-class ultralong-target-residence-time p38α inhibitors as a mitosis-targeted therapy for colorectal cancerSemantic proximity Read

The molecular basis of targeting protein kinases in cancer therapeutics.Semantic proximity Read