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Page 1
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: roulston a. 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.
RP-3500: A Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors.
Roulston A, Zimmermann M, Papp R, Skeldon A, Pellerin C, Dumas-Bérube É, Dumais V, Dorich S, Fader LD, Fournier S, Li L, Leclaire ME, Yin SY, Chefson A, Alam H, Yang W, Fugère-Desjardins C, Vignini-Hammond S, Skorey K, Mulani A, Rimkunas V, Veloso A, Hamel M, Stocco R, Mamane Y, Li Z, Young JTF, Zinda M, Black WC. Roulston A, et al. Mol Cancer Ther. 2022 Feb;21(2):245-256. doi: 10.1158/1535-7163.MCT-21-0615. Epub 2021 Dec 15. Mol Cancer Ther. 2022. PMID: 34911817 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: roulston a. 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.
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: roulston a. 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.
Guiding ATR and PARP inhibitor combinationswith chemogenomic screens.
Zimmermann M, Bernier C, Kaiser B, Fournier S, Li L, Desjardins J, Skeldon A, Rimkunas V, Veloso A, Young JTF, Roulston A, Zinda M. Zimmermann M, et al. Among authors: roulston a. Cell Rep. 2022 Jul 12;40(2):111081. doi: 10.1016/j.celrep.2022.111081. Cell Rep. 2022. PMID: 35830811 Free article.
Genotype-Directed Synthetic Cytotoxicity of ATR Inhibition with Radiotherapy.
Ng V, Sinha S, Novaj A, Ma J, McDermott N, Pei X, Longhini ALF, Grimsley H, Gardner R, Rosen E, Powell SN, Pareja F, Mandelker D, Khan A, Setton J, Roulston A, Morris S, Koehler M, Lee N, Reis-Filho J, Riaz N. Ng V, et al. Among authors: roulston a. Clin Cancer Res. 2024 Aug 7:OF1-OF14. doi: 10.1158/1078-0432.CCR-24-0154. Online ahead of print. Clin Cancer Res. 2024. PMID: 39109923
The synthetic diazonamide DZ-2384 has distinct effects on microtubule curvature and dynamics without neurotoxicity.
Wieczorek M, Tcherkezian J, Bernier C, Prota AE, Chaaban S, Rolland Y, Godbout C, Hancock MA, Arezzo JC, Ocal O, Rocha C, Olieric N, Hall A, Ding H, Bramoullé A, Annis MG, Zogopoulos G, Harran PG, Wilkie TM, Brekken RA, Siegel PM, Steinmetz MO, Shore GC, Brouhard GJ, Roulston A. Wieczorek M, et al. Among authors: roulston a. Sci Transl Med. 2016 Nov 16;8(365):365ra159. doi: 10.1126/scitranslmed.aag1093. Sci Transl Med. 2016. PMID: 27856798 Free PMC article.
Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis.
Nguyen M, Marcellus RC, Roulston A, Watson M, Serfass L, Murthy Madiraju SR, Goulet D, Viallet J, Bélec L, Billot X, Acoca S, Purisima E, Wiegmans A, Cluse L, Johnstone RW, Beauparlant P, Shore GC. Nguyen M, et al. Among authors: roulston a. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19512-7. doi: 10.1073/pnas.0709443104. Epub 2007 Nov 26. Proc Natl Acad Sci U S A. 2007. PMID: 18040043 Free PMC article.
The small molecule GMX1778 is a potent inhibitor of NAD+ biosynthesis: strategy for enhanced therapy in nicotinic acid phosphoribosyltransferase 1-deficient tumors.
Watson M, Roulston A, Bélec L, Billot X, Marcellus R, Bédard D, Bernier C, Branchaud S, Chan H, Dairi K, Gilbert K, Goulet D, Gratton MO, Isakau H, Jang A, Khadir A, Koch E, Lavoie M, Lawless M, Nguyen M, Paquette D, Turcotte E, Berger A, Mitchell M, Shore GC, Beauparlant P. Watson M, et al. Among authors: roulston a. Mol Cell Biol. 2009 Nov;29(21):5872-88. doi: 10.1128/MCB.00112-09. Epub 2009 Aug 24. Mol Cell Biol. 2009. PMID: 19703994 Free PMC article.
55 results