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Discovery of a Novel ATP-Competitive MEK Inhibitor DS03090629 that Overcomes Resistance Conferred by BRAF Overexpression in BRAF-Mutated Melanoma.

Molecular cancer therapeutics - 2 Mar 2023

Takano Kohei, Munehira Yoichi, Hatanaka Mana, Murakami Ryo, Shibata Yoshihiro, Shida Takeshi, Takeuchi Kosuke, Takechi Sho, Tabata Toshiki, Shimada Takashi, Kishikawa Shuhei, Matsui Yumi, Ubukata Osamu, Seki Takahiko, Kaneta Yasuyuki

Abstract excerpt

Patients with melanoma with activating BRAF mutations (BRAF V600E/K) initially respond to combination therapy of BRAF and MEK inhibitors. However, their clinical efficacy is limited by acquired resistance, in some cases driven by amplification of the mutant BRAF gene and subsequent reactivation of the MAPK pathway. DS03090629 is a novel and orally available MEK inhibitor that inhibits MEK in an ATP-competitive...

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Identifiers

PMID: 36622773
DOI: 10.1158/1535-7163.MCT-22-0306

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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