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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. Among authors: ghosh as. 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
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. Among authors: ghosh as. J Med Chem. 2015 Jan 8;58(1):401-18. doi: 10.1021/jm5013984. Epub 2014 Oct 23. J Med Chem. 2015. PMID: 25341110
A Phase 1 study of GDC-0134, a dual leucine zipper kinase inhibitor, in ALS.
Katz JS, Rothstein JD, Cudkowicz ME, Genge A, Oskarsson B, Hains AB, Chen C, Galanter J, Burgess BL, Cho W, Kerchner GA, Yeh FL, Ghosh AS, Cheeti S, Brooks L, Honigberg L, Couch JA, Rothenberg ME, Brunstein F, Sharma KR, van den Berg L, Berry JD, Glass JD. Katz JS, et al. Among authors: ghosh as. Ann Clin Transl Neurol. 2022 Jan;9(1):50-66. doi: 10.1002/acn3.51491. Epub 2022 Jan 10. Ann Clin Transl Neurol. 2022. PMID: 35014217 Free PMC article. Clinical Trial.
TMEM106B reduction does not rescue GRN deficiency in iPSC-derived human microglia and mouse models.
Dominguez SL, Laufer BI, Ghosh AS, Li Q, Ruggeri G, Emani MR, Phu L, Friedman BA, Sandoval W, Rose CM, Ngu H, Foreman O, Reichelt M, Juste Y, Lalehzadeh G, Hansen D, Nymark H, Mellal D, Gylling H, Kiełpiński ŁJ, Chih B, Bingol B, Hoogenraad CC, Meilandt WJ, Easton A. Dominguez SL, et al. Among authors: ghosh as. iScience. 2023 Oct 29;26(11):108362. doi: 10.1016/j.isci.2023.108362. eCollection 2023 Nov 17. iScience. 2023. PMID: 37965143 Free PMC article.
94 results