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Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
Estrada AA, Liu X, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Chan BK, Chen H, Ding X, DiPasquale AG, Dominguez SL, Dotson J, Drummond J, Flagella M, Flynn S, Fuji R, Gill A, Gunzner-Toste J, Harris SF, Heffron TP, Kleinheinz T, Lee DW, Le Pichon CE, Lyssikatos JP, Medhurst AD, Moffat JG, Mukund S, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Tran T, Trivedi N, Wang S, Zhang S, Zhang X, Zhao G, Zhu H, Sweeney ZK. Estrada AA, et al. Among authors: ding x. J Med Chem. 2012 Nov 26;55(22):9416-33. doi: 10.1021/jm301020q. Epub 2012 Oct 15. J Med Chem. 2012. PMID: 22985112
Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.
Koehler MF, Bergeron P, Blackwood E, Bowman KK, Chen YH, Deshmukh G, Ding X, Epler J, Lau K, Lee L, Liu L, Ly C, Malek S, Nonomiya J, Oeh J, Ortwine DF, Sampath D, Sideris S, Trinh L, Truong T, Wu J, Pei Z, Lyssikatos JP. Koehler MF, et al. Among authors: ding x. J Med Chem. 2012 Dec 27;55(24):10958-71. doi: 10.1021/jm301389h. Epub 2012 Dec 12. J Med Chem. 2012. PMID: 23199076
Ser1292 autophosphorylation is an indicator of LRRK2 kinase activity and contributes to the cellular effects of PD mutations.
Sheng Z, Zhang S, Bustos D, Kleinheinz T, Le Pichon CE, Dominguez SL, Solanoy HO, Drummond J, Zhang X, Ding X, Cai F, Song Q, Li X, Yue Z, van der Brug MP, Burdick DJ, Gunzner-Toste J, Chen H, Liu X, Estrada AA, Sweeney ZK, Scearce-Levie K, Moffat JG, Kirkpatrick DS, Zhu H. Sheng Z, et al. Among authors: ding x. Sci Transl Med. 2012 Dec 12;4(164):164ra161. doi: 10.1126/scitranslmed.3004485. Sci Transl Med. 2012. PMID: 23241745
Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).
Estrada AA, Shore DG, Blackwood E, Chen YH, Deshmukh G, Ding X, Dipasquale AG, Epler JA, Friedman LS, Koehler MF, Liu L, Malek S, Nonomiya J, Ortwine DF, Pei Z, Sideris S, St-Jean F, Trinh L, Truong T, Lyssikatos JP. Estrada AA, et al. Among authors: ding x. J Med Chem. 2013 Apr 11;56(7):3090-101. doi: 10.1021/jm400194n. Epub 2013 Mar 29. J Med Chem. 2013. PMID: 23473235
Structure-based design and synthesis of potent benzothiazole inhibitors of interleukin-2 inducible T cell kinase (ITK).
MacKinnon CH, Lau K, Burch JD, Chen Y, Dines J, Ding X, Eigenbrot C, Heifetz A, Jaochico A, Johnson A, Kraemer J, Kruger S, Krülle TM, Liimatta M, Ly J, Maghames R, Montalbetti CA, Ortwine DF, Pérez-Fuertes Y, Shia S, Stein DB, Trani G, Vaidya DG, Wang X, Bromidge SM, Wu LC, Pei Z. MacKinnon CH, et al. Among authors: ding x. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6331-5. doi: 10.1016/j.bmcl.2013.09.069. Epub 2013 Oct 1. Bioorg Med Chem Lett. 2013. PMID: 24138940
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