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Article

Development of a potent small-molecule degrader against oncogenic BRAFV600E protein that evades paradoxical MAPK activation.

Cancer science - 1 Aug 2022

Ohoka Nobumichi, Suzuki Masanori, Uchida Takuya, Tsukumo Yoshinori, Yoshida Masayuki, Inoue Takao, Ohki Hitoshi, Naito Mikihiko

Abstract excerpt

BRAF mutations are frequently observed in melanoma and hairy-cell leukemia. Currently approved rapidly accelerated fibrosarcoma (RAF) kinase inhibitors targeting oncogenic BRAF V600 mutations have shown remarkable efficacy in the clinic, but their therapeutic benefits are occasionally hampered by acquired resistance due to RAF dimerization-dependent reactivation of the downstream MAPK pathway, which is known as...

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Identifiers

PMID: 35579105
DOI: 10.1111/cas.15401
PMCID: PMC9357609

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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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