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Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306.
Szychowski J, Papp R, Dietrich E, Liu B, Vallée F, Leclaire ME, Fourtounis J, Martino G, Perryman AL, Pau V, Yin SY, Mader P, Roulston A, Truchon JF, Marshall CG, Diallo M, Duffy NM, Stocco R, Godbout C, Bonneau-Fortin A, Kryczka R, Bhaskaran V, Mao D, Orlicky S, Beaulieu P, Turcotte P, Kurinov I, Sicheri F, Mamane Y, Gallant M, Black WC. Szychowski J, et al. Among authors: fourtounis j. J Med Chem. 2022 Aug 11;65(15):10251-10284. doi: 10.1021/acs.jmedchem.2c00552. Epub 2022 Jul 26. J Med Chem. 2022. PMID: 35880755 Free PMC article.
CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition.
Gallo D, Young JTF, Fourtounis J, Martino G, Álvarez-Quilón A, Bernier C, Duffy NM, Papp R, Roulston A, Stocco R, Szychowski J, Veloso A, Alam H, Baruah PS, Fortin AB, Bowlan J, Chaudhary N, Desjardins J, Dietrich E, Fournier S, Fugère-Desjardins C, Goullet de Rugy T, Leclaire ME, Liu B, Bhaskaran V, Mamane Y, Melo H, Nicolas O, Singhania A, Szilard RK, Tkáč J, Yin SY, Morris SJ, Zinda M, Marshall CG, Durocher D. Gallo D, et al. Among authors: fourtounis j. Nature. 2022 Apr;604(7907):749-756. doi: 10.1038/s41586-022-04638-9. Epub 2022 Apr 20. Nature. 2022. PMID: 35444283 Free PMC article.
Targeting CCNE1 amplified ovarian and endometrial cancers by combined inhibition of PKMYT1 and ATR.
Xu H, George E, Gallo D, Medvedev S, Wang X, Kryczka R, Hyer ML, Fourtounis J, Stocco R, Aguado-Fraile E, Petrone A, Yin SY, Shiwram A, Anderson M, Kim H, Liu F, Marshall CG, Simpkins F. Xu H, et al. Among authors: fourtounis j. Res Sq [Preprint]. 2024 Feb 16:rs.3.rs-3854682. doi: 10.21203/rs.3.rs-3854682/v1. Res Sq. 2024. PMID: 38410486 Free PMC article. Preprint.