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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: briner k. 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: briner k. 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
Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor.
Richardson TI, Ornstein PL, Briner K, Fisher MJ, Backer RT, Biggers CK, Clay MP, Emmerson PJ, Hertel LW, Hsiung HM, Husain S, Kahl SD, Lee JA, Lindstrom TD, Martinelli MJ, Mayer JP, Mullaney JT, O'Brien TP, Pawlak JM, Revell KD, Shah J, Zgombick JM, Herr RJ, Melekhov A, Sampson PB, King CH. Richardson TI, et al. Among authors: briner k. J Med Chem. 2004 Jan 29;47(3):744-55. doi: 10.1021/jm0304109. J Med Chem. 2004. PMID: 14736255
Privileged structure based ligands for melanocortin receptors--substituted benzylic piperazine derivatives.
Fisher MJ, Backer RT, Collado I, de Frutos O, Husain S, Hsiung HM, Kuklish SL, Mateo AI, Mullaney JT, Ornstein PL, Paredes CG, O'Brian TP, Richardson TI, Shah J, Zgombick JM, Briner K. Fisher MJ, et al. Among authors: briner k. Bioorg Med Chem Lett. 2005 Nov 15;15(22):4973-8. doi: 10.1016/j.bmcl.2005.08.018. Bioorg Med Chem Lett. 2005. PMID: 16169215
Synthesis and structure-activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor.
Shi Q, Ornstein PL, Briner K, Richardson TI, Arnold MB, Backer RT, Buckmaster JL, Canada EJ, Doecke CW, Hertel LW, Honigschmidt N, Hsiung HM, Husain S, Kuklish SL, Martinelli MJ, Mullaney JT, O'Brien TP, Reinhard MR, Rothhaar R, Shah J, Wu Z, Xie C, Zgombick JM, Fisher MJ. Shi Q, et al. Among authors: briner k. Bioorg Med Chem Lett. 2006 May 1;16(9):2341-6. doi: 10.1016/j.bmcl.2005.10.103. Epub 2005 Nov 15. Bioorg Med Chem Lett. 2006. PMID: 16297618
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