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Structure-Based Design of Potent, Selective, and Orally Bioavailable VPS34 Kinase Inhibitors.
Hu DX, Patel S, Chen H, Wang S, Staben ST, Dimitrova YN, Wallweber HA, Lee JY, Chan GKY, Sneeringer CJ, Prangley MS, Moffat JG, Wu KC, Schutt LK, Salphati L, Pang J, McNamara E, Huang H, Chen Y, Wang Y, Zhao W, Lim J, Murthy A, Siu M. Hu DX, et al. Among authors: patel s. J Med Chem. 2022 Sep 8;65(17):11500-11512. doi: 10.1021/acs.jmedchem.1c01180. Epub 2021 Nov 15. J Med Chem. 2022. PMID: 34779204
Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).
Patel S, Harris SF, Gibbons P, Deshmukh G, Gustafson A, Kellar T, Lin H, Liu X, Liu Y, Liu Y, Ma C, Scearce-Levie K, Ghosh AS, Shin YG, Solanoy H, Wang J, Wang B, Yin J, Siu M, Lewcock JW. Patel S, et al. J Med Chem. 2015 Oct 22;58(20):8182-99. doi: 10.1021/acs.jmedchem.5b01072. Epub 2015 Oct 2. J Med Chem. 2015. PMID: 26431428
Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.
Hamilton GL, Chen H, Deshmukh G, Eigenbrot C, Fong R, Johnson A, Kohli PB, Lupardus PJ, Liederer BM, Ramaswamy S, Wang H, Wang J, Xu Z, Zhu Y, Vucic D, Patel S. Hamilton GL, et al. Among authors: patel s. Bioorg Med Chem Lett. 2019 Jun 15;29(12):1497-1501. doi: 10.1016/j.bmcl.2019.04.014. Epub 2019 Apr 11. Bioorg Med Chem Lett. 2019. PMID: 31000154
Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models.
Patel S, Cohen F, Dean BJ, De La Torre K, Deshmukh G, Estrada AA, Ghosh AS, Gibbons P, Gustafson A, Huestis MP, Le Pichon CE, Lin H, Liu W, Liu X, Liu Y, Ly CQ, Lyssikatos JP, Ma C, Scearce-Levie K, Shin YG, Solanoy H, Stark KL, Wang J, Wang B, Zhao X, Lewcock JW, Siu M. Patel S, et al. J Med Chem. 2015 Jan 8;58(1):401-18. doi: 10.1021/jm5013984. Epub 2014 Oct 23. J Med Chem. 2015. PMID: 25341110
From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.
Liang J, Labadie S, Zhang B, Ortwine DF, Patel S, Vinogradova M, Kiefer JR, Mauer T, Gehling VS, Harmange JC, Cummings R, Lai T, Liao J, Zheng X, Liu Y, Gustafson A, Van der Porten E, Mao W, Liederer BM, Deshmukh G, An L, Ran Y, Classon M, Trojer P, Dragovich PS, Murray L. Liang J, et al. Among authors: patel s. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2974-2981. doi: 10.1016/j.bmcl.2017.05.016. Epub 2017 May 5. Bioorg Med Chem Lett. 2017. PMID: 28512031
Novel benzoxazole inhibitors of mPGES-1.
Kablaoui N, Patel S, Shao J, Demian D, Hoffmaster K, Berlioz F, Vazquez ML, Moore WM, Nugent RA. Kablaoui N, et al. Among authors: patel s. Bioorg Med Chem Lett. 2013 Feb 1;23(3):907-11. doi: 10.1016/j.bmcl.2012.10.040. Epub 2012 Oct 16. Bioorg Med Chem Lett. 2013. PMID: 23266122
Loss of dual leucine zipper kinase signaling is protective in animal models of neurodegenerative disease.
Le Pichon CE, Meilandt WJ, Dominguez S, Solanoy H, Lin H, Ngu H, Gogineni A, Sengupta Ghosh A, Jiang Z, Lee SH, Maloney J, Gandham VD, Pozniak CD, Wang B, Lee S, Siu M, Patel S, Modrusan Z, Liu X, Rudhard Y, Baca M, Gustafson A, Kaminker J, Carano RAD, Huang EJ, Foreman O, Weimer R, Scearce-Levie K, Lewcock JW. Le Pichon CE, et al. Among authors: patel s. Sci Transl Med. 2017 Aug 16;9(403):eaag0394. doi: 10.1126/scitranslmed.aag0394. Sci Transl Med. 2017. PMID: 28814543
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