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Page 1
Small-molecule WNK inhibition regulates cardiovascular and renal function.
Yamada K, Park HM, Rigel DF, DiPetrillo K, Whalen EJ, Anisowicz A, Beil M, Berstler J, Brocklehurst CE, Burdick DA, Caplan SL, Capparelli MP, Chen G, Chen W, Dale B, Deng L, Fu F, Hamamatsu N, Harasaki K, Herr T, Hoffmann P, Hu QY, Huang WJ, Idamakanti N, Imase H, Iwaki Y, Jain M, Jeyaseelan J, Kato M, Kaushik VK, Kohls D, Kunjathoor V, LaSala D, Lee J, Liu J, Luo Y, Ma F, Mo R, Mowbray S, Mogi M, Ossola F, Pandey P, Patel SJ, Raghavan S, Salem B, Shanado YH, Trakshel GM, Turner G, Wakai H, Wang C, Weldon S, Wielicki JB, Xie X, Xu L, Yagi YI, Yasoshima K, Yin J, Yowe D, Zhang JH, Zheng G, Monovich L. Yamada K, et al. Among authors: jain m. Nat Chem Biol. 2016 Nov;12(11):896-898. doi: 10.1038/nchembio.2168. Epub 2016 Sep 5. Nat Chem Biol. 2016. PMID: 27595330
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: jain m. Nat Chem Biol. 2015 Jul;11(7):511-7. doi: 10.1038/nchembio.1837. Epub 2015 Jun 1. Nat Chem Biol. 2015. PMID: 26030728
Optimization of Allosteric With-No-Lysine (WNK) Kinase Inhibitors and Efficacy in Rodent Hypertension Models.
Yamada K, Levell J, Yoon T, Kohls D, Yowe D, Rigel DF, Imase H, Yuan J, Yasoshima K, DiPetrillo K, Monovich L, Xu L, Zhu M, Kato M, Jain M, Idamakanti N, Taslimi P, Kawanami T, Argikar UA, Kunjathoor V, Xie X, Yagi YI, Iwaki Y, Robinson Z, Park HM. Yamada K, et al. Among authors: jain m. J Med Chem. 2017 Aug 24;60(16):7099-7107. doi: 10.1021/acs.jmedchem.7b00708. Epub 2017 Aug 3. J Med Chem. 2017. PMID: 28771350
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: jain m. 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
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: jain m. Nat Chem Biol. 2015 Sep;11(9):741. doi: 10.1038/nchembio0915-741a. Nat Chem Biol. 2015. PMID: 26284678 No abstract available.
Discovery of diamide compounds as diacylglycerol acyltransferase 1 (DGAT1) inhibitors.
Nakajima K, April M, Brewer JT, Daniels T, Forster CJ, Gilmore TA, Jain M, Kanter A, Kwak Y, Li J, McQuire L, Serrano-Wu MH, Streeper R, Szklennik P, Thompson J, Wang B. Nakajima K, et al. Among authors: jain m. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1245-8. doi: 10.1016/j.bmcl.2016.01.025. Epub 2016 Jan 11. Bioorg Med Chem Lett. 2016. PMID: 26804232
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: jain m. Nat Chem Biol. 2016 Apr;12(4):304. doi: 10.1038/nchembio0416-304c. Nat Chem Biol. 2016. PMID: 26991088 No abstract available.
Discovery of an Orally Bioavailable Benzimidazole Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitor That Suppresses Body Weight Gain in Diet-Induced Obese Dogs and Postprandial Triglycerides in Humans.
Nakajima K, Chatelain R, Clairmont KB, Commerford R, Coppola GM, Daniels T, Forster CJ, Gilmore TA, Gong Y, Jain M, Kanter A, Kwak Y, Li J, Meyers CD, Neubert AD, Szklennik P, Tedesco V, Thompson J, Truong D, Yang Q, Hubbard BK, Serrano-Wu MH. Nakajima K, et al. Among authors: jain m. J Med Chem. 2017 Jun 8;60(11):4657-4664. doi: 10.1021/acs.jmedchem.7b00173. Epub 2017 May 24. J Med Chem. 2017. PMID: 28498655 Clinical Trial.
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: jain m. 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
Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial Triglycerides.
Serrano-Wu MH, Coppola GM, Gong Y, Neubert AD, Chatelain R, Clairmont KB, Commerford R, Cosker T, Daniels T, Hou Y, Jain M, Juedes M, Li L, Mullarkey T, Rocheford E, Sung MJ, Tyler A, Yang Q, Yoon T, Hubbard BK. Serrano-Wu MH, et al. Among authors: jain m. ACS Med Chem Lett. 2012 Apr 4;3(5):411-5. doi: 10.1021/ml3000512. eCollection 2012 May 10. ACS Med Chem Lett. 2012. PMID: 24900485 Free PMC article.
4,227 results