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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: mader p. 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.
Identification of RP-6685, an Orally Bioavailable Compound that Inhibits the DNA Polymerase Activity of Polθ.
Bubenik M, Mader P, Mochirian P, Vallée F, Clark J, Truchon JF, Perryman AL, Pau V, Kurinov I, Zahn KE, Leclaire ME, Papp R, Mathieu MC, Hamel M, Duffy NM, Godbout C, Casas-Selves M, Falgueyret JP, Baruah PS, Nicolas O, Stocco R, Poirier H, Martino G, Fortin AB, Roulston A, Chefson A, Dorich S, St-Onge M, Patel P, Pellerin C, Ciblat S, Pinter T, Barabé F, El Bakkouri M, Parikh P, Gervais C, Sfeir A, Mamane Y, Morris SJ, Black WC, Sicheri F, Gallant M. Bubenik M, et al. Among authors: mader p. J Med Chem. 2022 Oct 13;65(19):13198-13215. doi: 10.1021/acs.jmedchem.2c00998. Epub 2022 Sep 20. J Med Chem. 2022. PMID: 36126059 Free PMC article.
Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4.
Chana CK, Maisonneuve P, Posternak G, Grinberg NGA, Poirson J, Ona SM, Ceccarelli DF, Mader P, St-Cyr DJ, Pau V, Kurinov I, Tang X, Deng D, Cui W, Su W, Kuai L, Soll R, Tyers M, Röst HL, Batey RA, Taipale M, Gingras AC, Sicheri F. Chana CK, et al. Among authors: mader p. J Med Chem. 2022 Oct 13;65(19):12725-12746. doi: 10.1021/acs.jmedchem.2c00509. Epub 2022 Sep 18. J Med Chem. 2022. PMID: 36117290 Free PMC article.
Functional characterization of a PROTAC directed against BRAF mutant V600E.
Posternak G, Tang X, Maisonneuve P, Jin T, Lavoie H, Daou S, Orlicky S, Goullet de Rugy T, Caldwell L, Chan K, Aman A, Prakesch M, Poda G, Mader P, Wong C, Maier S, Kitaygorodsky J, Larsen B, Colwill K, Yin Z, Ceccarelli DF, Batey RA, Taipale M, Kurinov I, Uehling D, Wrana J, Durocher D, Gingras AC, Al-Awar R, Therrien M, Sicheri F. Posternak G, et al. Among authors: mader p. Nat Chem Biol. 2020 Nov;16(11):1170-1178. doi: 10.1038/s41589-020-0609-7. Epub 2020 Aug 10. Nat Chem Biol. 2020. PMID: 32778845 Free PMC article.
Bora phosphorylation substitutes in trans for T-loop phosphorylation in Aurora A to promote mitotic entry.
Tavernier N, Thomas Y, Vigneron S, Maisonneuve P, Orlicky S, Mader P, Regmi SG, Van Hove L, Levinson NM, Gasmi-Seabrook G, Joly N, Poteau M, Velez-Aguilera G, Gavet O, Castro A, Dasso M, Lorca T, Sicheri F, Pintard L. Tavernier N, et al. Among authors: mader p. Nat Commun. 2021 Mar 26;12(1):1899. doi: 10.1038/s41467-021-21922-w. Nat Commun. 2021. PMID: 33771996 Free PMC article.
Identification and characterization of the first fragment hits for SETDB1 Tudor domain.
Mader P, Mendoza-Sanchez R, Iqbal A, Dong A, Dobrovetsky E, Corless VB, Liew SK, Houliston SR, De Freitas RF, Smil D, Sena CCD, Kennedy S, Diaz DB, Wu H, Dombrovski L, Allali-Hassani A, Min J, Schapira M, Vedadi M, Brown PJ, Santhakumar V, Yudin AK, Arrowsmith CH. Mader P, et al. Bioorg Med Chem. 2019 Sep 1;27(17):3866-3878. doi: 10.1016/j.bmc.2019.07.020. Epub 2019 Jul 12. Bioorg Med Chem. 2019. PMID: 31327677
136 results