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MEN1 mutations mediate clinical resistance to menin inhibition.
Perner F, Stein EM, Wenge DV, Singh S, Kim J, Apazidis A, Rahnamoun H, Anand D, Marinaccio C, Hatton C, Wen Y, Stone RM, Schaller D, Mowla S, Xiao W, Gamlen HA, Stonestrom AJ, Persaud S, Ener E, Cutler JA, Doench JG, McGeehan GM, Volkamer A, Chodera JD, Nowak RP, Fischer ES, Levine RL, Armstrong SA, Cai SF. Perner F, et al. Nature. 2023 Mar;615(7954):913-919. doi: 10.1038/s41586-023-05755-9. Epub 2023 Mar 15. Nature. 2023. PMID: 36922589 Free PMC article. Clinical Trial.
IKAROS and MENIN coordinate therapeutically actionable leukemogenic gene expression in MLL-r acute myeloid leukemia.
Aubrey BJ, Cutler JA, Bourgeois W, Donovan KA, Gu S, Hatton C, Perlee S, Perner F, Rahnamoun H, Theall ACP, Henrich JA, Zhu Q, Nowak RP, Kim YJ, Parvin S, Cremer A, Olsen SN, Eleuteri NA, Pikman Y, McGeehan GM, Stegmaier K, Letai A, Fischer ES, Liu XS, Armstrong SA. Aubrey BJ, et al. Nat Cancer. 2022 May;3(5):595-613. doi: 10.1038/s43018-022-00366-1. Epub 2022 May 9. Nat Cancer. 2022. PMID: 35534777 Free PMC article.
Mezigdomide is effective alone and in combination with menin inhibition in preclinical models of KMT2A-r and NPM1c AML.
Bourgeois W, Cutler JA, Aubrey BJ, Wenge DV, Perner F, Martucci C, Henrich JA, Klega K, Nowak RP, Donovan KA, Boileau M, Wen Y, Hatton C, Apazidis AA, Olsen SN, Kirmani N, Pikman Y, Pollard JA, Perry JA, Sperling AS, Ebert BL, McGeehan GM, Crompton BD, Fischer ES, Armstrong SA. Bourgeois W, et al. Blood. 2024 Apr 11;143(15):1513-1527. doi: 10.1182/blood.2023021105. Blood. 2024. PMID: 38096371