A drug discovery platform to identify compounds that inhibit EGFR triple mutants.

doi:10.1038/s41589-020-0484-2

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A drug discovery platform to identify compounds that inhibit EGFR triple mutants.

Nature chemical biology - 1 May 2020

Saraon Punit, Snider Jamie, Kalaidzidis Yannis, Wybenga-Groot Leanne E, Weiss Konstantin, Rai Ankit, Radulovich Nikolina, Drecun Luka, Vučković Nika, Vučetić Adriana, Wong Victoria, Thériault Brigitte, Pham Nhu-An, Park Jin H, Datti Alessandro, Wang Jenny, Pathmanathan Shivanthy, Aboualizadeh Farzaneh, Lyakisheva Anna, Yao Zhong, Wang Yuhui, Joseph Babu, Aman Ahmed, Moran Michael F, Prakesch Michael, Poda Gennady, Marcellus Richard, Uehling David, Samaržija Miroslav, Jakopović Marko, Tsao Ming-Sound, Shepherd Frances A, Sacher Adrian, Leighl Natasha, Akhmanova Anna, Al-Awar Rima, Zerial Marino, Stagljar Igor

Abstract excerpt

Receptor tyrosine kinases (RTKs) are transmembrane receptors of great clinical interest due to their role in disease. Historically, therapeutics targeting RTKs have been identified using in vitro kinase assays. Due to frequent development of drug resistance, however, there is a need to identify more diverse compounds that inhibit mutated but not wild-type RTKs. Here, we describe MaMTH-DS (mammalian membrane...

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PMID: 32094923
DOI: 10.1038/s41589-020-0484-2
PMCID: PMC8123931

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