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Page 1
Discovery and characterization of a selective IKZF2 glue degrader for cancer immunotherapy.
Bonazzi S, d'Hennezel E, Beckwith REJ, Xu L, Fazal A, Magracheva A, Ramesh R, Cernijenko A, Antonakos B, Bhang HC, Caro RG, Cobb JS, Ornelas E, Ma X, Wartchow CA, Clifton MC, Forseth RR, Fortnam BH, Lu H, Csibi A, Tullai J, Carbonneau S, Thomsen NM, Larrow J, Chie-Leon B, Hainzl D, Gu Y, Lu D, Meyer MJ, Alexander D, Kinyamu-Akunda J, Sabatos-Peyton CA, Dales NA, Zécri FJ, Jain RK, Shulok J, Wang YK, Briner K, Porter JA, Tallarico JA, Engelman JA, Dranoff G, Bradner JE, Visser M, Solomon JM. Bonazzi S, et al. Among authors: dales na. Cell Chem Biol. 2023 Mar 16;30(3):235-247.e12. doi: 10.1016/j.chembiol.2023.02.005. Epub 2023 Mar 1. Cell Chem Biol. 2023. PMID: 36863346 Free article.
SMN2 splice modulators enhance U1-pre-mRNA association and rescue SMA mice.
Palacino J, Swalley SE, Song C, Cheung AK, Shu L, Zhang X, Van Hoosear M, Shin Y, Chin DN, Keller CG, Beibel M, Renaud NA, Smith TM, Salcius M, Shi X, Hild M, Servais R, Jain M, Deng L, Bullock C, McLellan M, Schuierer S, Murphy L, Blommers MJ, Blaustein C, Berenshteyn F, Lacoste A, Thomas JR, Roma G, Michaud GA, Tseng BS, Porter JA, Myer VE, Tallarico JA, Hamann LG, Curtis D, Fishman MC, Dietrich WF, Dales NA, Sivasankaran R. Palacino J, et al. Among authors: dales na. Nat Chem Biol. 2015 Jul;11(7):511-7. doi: 10.1038/nchembio.1837. Epub 2015 Jun 1. Nat Chem Biol. 2015. PMID: 26030728
Discovery of Small Molecule Splicing Modulators of Survival Motor Neuron-2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA).
Cheung AK, Hurley B, Kerrigan R, Shu L, Chin DN, Shen Y, O'Brien G, Sung MJ, Hou Y, Axford J, Cody E, Sun R, Fazal A, Fridrich C, Sanchez CC, Tomlinson RC, Jain M, Deng L, Hoffmaster K, Song C, Van Hoosear M, Shin Y, Servais R, Towler C, Hild M, Curtis D, Dietrich WF, Hamann LG, Briner K, Chen KS, Kobayashi D, Sivasankaran R, Dales NA. Cheung AK, et al. Among authors: dales na. J Med Chem. 2018 Dec 27;61(24):11021-11036. doi: 10.1021/acs.jmedchem.8b01291. Epub 2018 Dec 13. J Med Chem. 2018. PMID: 30407821
Use of Intramolecular 1,5-Sulfur-Oxygen and 1,5-Sulfur-Halogen Interactions in the Design of N-Methyl-5-aryl-N-(2,2,6,6-tetramethylpiperidin-4-yl)-1,3,4-thiadiazol-2-amine SMN2 Splicing Modulators.
Axford J, Sung MJ, Manchester J, Chin D, Jain M, Shin Y, Dix I, Hamann LG, Cheung AK, Sivasankaran R, Briner K, Dales NA, Hurley B. Axford J, et al. Among authors: dales na. J Med Chem. 2021 Apr 22;64(8):4744-4761. doi: 10.1021/acs.jmedchem.0c02173. Epub 2021 Apr 6. J Med Chem. 2021. PMID: 33822618
Corrigendum: SMN2 splice modulators enhance U1-pre-mRNA association and rescue SMA mice.
Palacino J, Swalley SE, Song C, Cheung AK, Shu L, Zhang X, Van Hoosear M, Shin Y, Chin DN, Keller CG, Beibel M, Renaud NA, Smith TM, Salcius M, Shi X, Hild M, Servais R, Jain M, Deng L, Bullock C, McLellan M, Schuierer S, Murphy L, Blommers MJ, Blaustein C, Berenshteyn F, Lacoste A, Thomas JR, Roma G, Michaud GA, Tseng BS, Porter JA, Myer VE, Tallarico JA, Hamann LG, Curtis D, Fishman MC, Dietrich WF, Dales NA, Sivasankaran R. Palacino J, et al. Among authors: dales na. Nat Chem Biol. 2015 Sep;11(9):741. doi: 10.1038/nchembio0915-741a. Nat Chem Biol. 2015. PMID: 26284678 No abstract available.
Corrigendum: SMN2 splice modulators enhance U1-pre-mRNA association and rescue SMA mice.
Palacino J, Swalley SE, Song C, Cheung AK, Shu L, Zhang X, Van Hoosear M, Shin Y, Chin DN, Keller CG, Beibel M, Renaud NA, Smith TM, Salcius M, Shi X, Hild M, Servais R, Jain M, Deng L, Bullock C, McLellan M, Schuierer S, Murphy L, Blommers MJ, Blaustein C, Berenshteyn F, Lacoste A, Thomas JR, Roma G, Michaud GA, Tseng BS, Porter JA, Myer VE, Tallarico JA, Hamann LG, Curtis D, Fishman MC, Dietrich WF, Dales NA, Sivasankaran R. Palacino J, et al. Among authors: dales na. Nat Chem Biol. 2016 Apr;12(4):304. doi: 10.1038/nchembio0416-304c. Nat Chem Biol. 2016. PMID: 26991088 No abstract available.
BET bromodomain inhibitors regulate keratinocyte plasticity.
Schutzius G, Kolter C, Bergling S, Tortelli F, Fuchs F, Renner S, Guagnano V, Cotesta S, Rueeger H, Faller M, Bouchez L, Salathe A, Nigsch F, Richards SM, Louis M, Gruber V, Aebi A, Turner J, Grandjean F, Li J, Dimitri C, Thomas JR, Schirle M, Blank J, Drueckes P, Vaupel A, Tiedt R, Manley PW, Klopp J, Hemmig R, Zink F, Leroy N, Carbone W, Roma G, Keller CG, Dales N, Beyerbach A, Zimmerlin A, Bonenfant D, Terranova R, Berwick A, Sahambi S, Reynolds A, Jennings LL, Ruffner H, Tarsa P, Bouwmeester T, Driver V, Frederiksen M, Lohmann F, Kirkland S. Schutzius G, et al. Nat Chem Biol. 2021 Mar;17(3):280-290. doi: 10.1038/s41589-020-00716-z. Epub 2021 Jan 18. Nat Chem Biol. 2021. PMID: 33462494
An orally available, brain penetrant, small molecule lowers huntingtin levels by enhancing pseudoexon inclusion.
Keller CG, Shin Y, Monteys AM, Renaud N, Beibel M, Teider N, Peters T, Faller T, St-Cyr S, Knehr J, Roma G, Reyes A, Hild M, Lukashev D, Theil D, Dales N, Cha JH, Borowsky B, Dolmetsch R, Davidson BL, Sivasankaran R. Keller CG, et al. Nat Commun. 2022 Mar 3;13(1):1150. doi: 10.1038/s41467-022-28653-6. Nat Commun. 2022. PMID: 35241644 Free PMC article.
17 results