Functional characterization of a PROTAC directed against BRAF mutant V600E.

doi:10.1038/s41589-020-0609-7

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Article

Functional characterization of a PROTAC directed against BRAF mutant V600E.

Nature chemical biology - 1 Nov 2020

Posternak Ganna, Tang Xiaojing, Maisonneuve Pierre, Jin Ting, Lavoie Hugo, Daou Salima, Orlicky Stephen, Goullet de Rugy Theo, Caldwell Lauren, Chan Kin, Aman Ahmed, Prakesch Michael, Poda Gennady, Mader Pavel, Wong Cassandra, Maier Stefan, Kitaygorodsky Julia, Larsen Brett, Colwill Karen, Yin Zhe, Ceccarelli Derek F, Batey Robert A, Taipale Mikko, Kurinov Igor, Uehling David, Wrana Jeff, Durocher Daniel, Gingras Anne-Claude, Al-Awar Rima, Therrien Marc, Sicheri Frank

Abstract excerpt

The RAF family kinases function in the RAS-ERK pathway to transmit signals from activated RAS to the downstream kinases MEK and ERK. This pathway regulates cell proliferation, differentiation and survival, enabling mutations in RAS and RAF to act as potent drivers of human cancers. Drugs targeting the prevalent oncogenic mutant BRAF(V600E) have shown great efficacy in the clinic, but long-term effectiveness is...

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PMID: 32778845
DOI: 10.1038/s41589-020-0609-7
PMCID: PMC7862923

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

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