Comprehensive Target Engagement by the EZH2 Inhibitor Tulmimetostat Allows for Targeting of ARID1A Mutant Cancers.

doi:10.1158/0008-5472.CAN-24-0398

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Comprehensive Target Engagement by the EZH2 Inhibitor Tulmimetostat Allows for Targeting of ARID1A Mutant Cancers.

Cancer research - 1 Aug 2024

Keller Patricia J, Adams Elizabeth J, Wu Rentian, Côté Alexandre, Arora Shilpi, Cantone Nico, Meyer Rosana, Mertz Jennifer A, Gehling Victor, Cui Jike, Stuckey Jacob I, Khanna Avinash, Zhao Feng, Chen Zehua, Yu Ziyang, Cummings Richard T, Taimi Mohammed, Lakhani Nehal J, Rasco Drew, Gutierrez Martin, Duska Linda, Devitt Michael, Rippley Ronda, Levell Julian, Truong Jennifer, Wang Jing, Sun Kaiming, Trojer Patrick

Abstract excerpt

Recurrent somatic mutations in the BRG1/BRM-associated factor (BAF) chromatin remodeling complex subunit ARID1A occur frequently in advanced urothelial, endometrial, and ovarian clear cell carcinomas, creating an alternative chromatin state that may be exploited therapeutically. The histone methyltransferase EZH2 has been previously identified as targetable vulnerability in the context of ARID1A mutations. In...

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PMID: 38833522
DOI: 10.1158/0008-5472.CAN-24-0398
PMCID: PMC11292196

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ARID1A

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