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The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition.

Journal of medicinal chemistry - 8 Feb 2024

Chen Young K, Kanouni Toufike, Arnold Lee D, Cox Jason M, Gardiner Elisabeth, Grandinetti Kathryn, Jiang Ping, Kaldor Stephen W, Lee Catherine, Li Chun, Martin Eric S, Miller Nichol, Murphy Eric A, Timple Noel, Tyhonas John S, Vassar Angie, Wang Tim S, Williams Richard, Yuan Ding, Kania Robert S

Abstract excerpt

RAF, a core signaling component of the MAPK kinase cascade, is often mutated in various cancers, including melanoma, lung, and colorectal cancers. The approved inhibitors were focused on targeting the BRAFV600E mutation that results in constitutive activation of kinase signaling through the monomeric protein (Class I). However, these inhibitors also paradoxically activate kinase signaling of RAF dimers, resulting...

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Identifiers

PMID: 38230963
DOI: 10.1021/acs.jmedchem.3c01830

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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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