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Page 1
Discovery of Potent and Brain-Penetrant Tau Tubulin Kinase 1 (TTBK1) Inhibitors that Lower Tau Phosphorylation In Vivo.
J Med Chem. 2021 May 13;64(9):6358-6380. doi: 10.1021/acs.jmedchem.1c00382. Epub 2021 May 4.
J Med Chem. 2021.
PMID: 33944571
Acute inhibition of the CNS-specific kinase TTBK1 significantly lowers tau phosphorylation at several disease relevant sites.
Dillon GM, Henderson JL, Bao C, Joyce JA, Calhoun M, Amaral B, King KW, Bajrami B, Rabah D.
Dillon GM, et al. Among authors: amaral b.
PLoS One. 2020 Apr 7;15(4):e0228771. doi: 10.1371/journal.pone.0228771. eCollection 2020.
PLoS One. 2020.
PMID: 32255788
Free PMC article.
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Structural Basis for Achieving GSK-3β Inhibition with High Potency, Selectivity, and Brain Exposure for Positron Emission Tomography Imaging and Drug Discovery.
Bernard-Gauthier V, Mossine AV, Knight A, Patnaik D, Zhao WN, Cheng C, Krishnan HS, Xuan LL, Chindavong PS, Reis SA, Chen JM, Shao X, Stauff J, Arteaga J, Sherman P, Salem N, Bonsall D, Amaral B, Varlow C, Wells L, Martarello L, Patel S, Liang SH, Kurumbail RG, Haggarty SJ, Scott PJH, Vasdev N.
Bernard-Gauthier V, et al. Among authors: amaral b.
J Med Chem. 2019 Nov 14;62(21):9600-9617. doi: 10.1021/acs.jmedchem.9b01030. Epub 2019 Oct 21.
J Med Chem. 2019.
PMID: 31535859
Free PMC article.
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Elucidation of the GSK3α Structure Informs the Design of Novel, Paralog-Selective Inhibitors.
Amaral B, Capacci A, Anderson T, Tezer C, Bajrami B, Lulla M, Lucas B, Chodaparambil JV, Marcotte D, Kumar PR, Murugan P, Spilker K, Cullivan M, Wang T, Peterson AC, Enyedy I, Ma B, Chen T, Yousaf Z, Calhoun M, Golonzhka O, Dillon GM, Koirala S.
Amaral B, et al.
ACS Chem Neurosci. 2023 Mar 15;14(6):1080-1094. doi: 10.1021/acschemneuro.2c00476. Epub 2023 Feb 22.
ACS Chem Neurosci. 2023.
PMID: 36812145
Free PMC article.
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