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Article

Design, synthesis and characterisation of a novel type II B-RAF paradox breaker inhibitor.

European journal of medicinal chemistry - 15 Mar 2023

Arora Rohit, Linders Joannes T M, Aci-Sèche Samia, Verheyen Thomas, Van Heerde Erika, Brehmer Dirk, Chaikuad Apirat, Knapp Stefan, Bonnet Pascal

Abstract excerpt

The mutation V600E in B-Raf leads to mitogen activated protein kinase (MAPK) pathway activation, uncontrolled cell proliferation, and tumorigenesis. ATP competitive type I B-Raf inhibitors, such as vemurafenib (1) and PLX4720 (4) efficiently block the MAPK pathways in B-Raf mutant cells, however these inhibitors induce conformational changes in the wild type B-Raf (wtB-Raf) kinase domain leading to...

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Methodology Data sources Editorial policy Privacy Delete account & data About Contact Helena Bioinformatics

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Source

Identifiers

PMID: 36878151
DOI: 10.1016/j.ejmech.2023.115231

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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