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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. 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: szychowski 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.
Structure-based design, synthesis and A-site rRNA co-crystal complexes of novel amphiphilic aminoglycoside antibiotics with new binding modes: a synergistic hydrophobic effect against resistant bacteria.
Hanessian S, Pachamuthu K, Szychowski J, Giguère A, Swayze EE, Migawa MT, François B, Kondo J, Westhof E. Hanessian S, et al. Among authors: szychowski j. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7097-101. doi: 10.1016/j.bmcl.2010.09.084. Epub 2010 Sep 19. Bioorg Med Chem Lett. 2010. PMID: 20970332
Structure-based design, synthesis, and A-site rRNA cocrystal complexes of functionally novel aminoglycoside antibiotics: C2" ether analogues of paromomycin.
Hanessian S, Szychowski J, Adhikari SS, Vasquez G, Kandasamy P, Swayze EE, Migawa MT, Ranken R, François B, Wirmer-Bartoschek J, Kondo J, Westhof E. Hanessian S, et al. Among authors: szychowski j. J Med Chem. 2007 May 17;50(10):2352-69. doi: 10.1021/jm061200+. Epub 2007 Apr 26. J Med Chem. 2007. PMID: 17458946
211 results