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Page 1
Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.
Papillon JP, Lou C, Singh AK, Adams CM, Ksander GM, Beil ME, Chen W, Leung-Chu J, Fu F, Gan L, Hu CW, Jeng AY, LaSala D, Liang G, Rigel DF, Russell KS, Vest JA, Watson C. Papillon JP, et al. J Med Chem. 2015 Dec 10;58(23):9382-94. doi: 10.1021/acs.jmedchem.5b01545. Epub 2015 Nov 18. J Med Chem. 2015. PMID: 26540564
Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
Meredith EL, Ksander G, Monovich LG, Papillon JP, Liu Q, Miranda K, Morris P, Rao C, Burgis R, Capparelli M, Hu QY, Singh A, Rigel DF, Jeng AY, Beil M, Fu F, Hu CW, LaSala D. Meredith EL, et al. Among authors: papillon jp. ACS Med Chem Lett. 2013 Oct 17;4(12):1203-7. doi: 10.1021/ml400324c. eCollection 2013 Dec 12. ACS Med Chem Lett. 2013. PMID: 24900631 Free PMC article.
Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers.
Papillon JPN, Nakajima K, Adair CD, Hempel J, Jouk AO, Karki RG, Mathieu S, Möbitz H, Ntaganda R, Smith T, Visser M, Hill SE, Hurtado FK, Chenail G, Bhang HC, Bric A, Xiang K, Bushold G, Gilbert T, Vattay A, Dooley J, Costa EA, Park I, Li A, Farley D, Lounkine E, Yue QK, Xie X, Zhu X, Kulathila R, King D, Hu T, Vulic K, Cantwell J, Luu C, Jagani Z. Papillon JPN, et al. J Med Chem. 2018 Nov 21;61(22):10155-10172. doi: 10.1021/acs.jmedchem.8b01318. Epub 2018 Oct 31. J Med Chem. 2018. PMID: 30339381
Discovery of a novel indole pharmacophore for the irreversible inhibition of myeloperoxidase (MPO).
Patnaik A, Axford L, Deng L, Cohick E, Ren X, Loi S, Kecman S, Hollis-Symynkywicz M, Harrison TJ, Papillon JPN, Dales N, Hamann LG, Lee L, Regard JB, Marcinkeviciene J, Marro ML, Patterson AW. Patnaik A, et al. Among authors: papillon jpn. Bioorg Med Chem. 2020 Jun 15;28(12):115548. doi: 10.1016/j.bmc.2020.115548. Epub 2020 May 12. Bioorg Med Chem. 2020. PMID: 32503688
Discovery of Darovasertib (NVP-LXS196), a Pan-PKC Inhibitor for the Treatment of Metastatic Uveal Melanoma.
Visser M, Papillon JPN, Luzzio M, LaMarche MJ, Fan J, Michael W, Wang D, Zhang A, Straub C, Mathieu S, Kato M, Palermo M, Chen C, Ramsey T, Joud C, Barrett R, Vattay A, Guo R, Bric A, Chung F, Liang G, Romanowski MJ, Lam J, Thohan S, Atassi F, Wylie A, Cooke VG. Visser M, et al. Among authors: papillon jpn. J Med Chem. 2024 Jan 25;67(2):1447-1459. doi: 10.1021/acs.jmedchem.3c02002. Epub 2024 Jan 10. J Med Chem. 2024. PMID: 38198520
Discovery of 1-((6-Aminopyridin-3-yl)Methyl)-3-(4-Bromophenyl)Urea as a Potent, Irreversible Myeloperoxidase Inhibitor.
Marro ML, Patterson AW, Lee L, Deng L, Reynolds A, Ren X, Axford L, Patnaik A, Hollis-Symynkywicz M, Casson N, Custeau D, Ames L, Loi S, Zhang L, Honda T, Blank J, Harrison TJ, Papillon JPN, Hamann LG, Marcinkeviciene J, Regard JB. Marro ML, et al. Among authors: papillon jpn. J Pharmacol Exp Ther. 2018 Oct;367(1):147-154. doi: 10.1124/jpet.118.248435. Epub 2018 Aug 3. J Pharmacol Exp Ther. 2018. PMID: 30076263
The Discovery of SWI/SNF Chromatin Remodeling Activity as a Novel and Targetable Dependency in Uveal Melanoma.
Rago F, Elliott G, Li A, Sprouffske K, Kerr G, Desplat A, Abramowski D, Chen JT, Farsidjani A, Xiang KX, Bushold G, Feng Y, Shirley MD, Bric A, Vattay A, Möbitz H, Nakajima K, Adair CD, Mathieu S, Ntaganda R, Smith T, Papillon JPN, Kauffmann A, Ruddy DA, Bhang HC, Castelletti D, Jagani Z. Rago F, et al. Among authors: papillon jpn. Mol Cancer Ther. 2020 Oct;19(10):2186-2195. doi: 10.1158/1535-7163.MCT-19-1013. Epub 2020 Aug 3. Mol Cancer Ther. 2020. PMID: 32747420
15 results