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Discovery of Potent and Brain-Penetrant Tau Tubulin Kinase 1 (TTBK1) Inhibitors that Lower Tau Phosphorylation In Vivo.
Halkina T, Henderson JL, Lin EY, Himmelbauer MK, Jones JH, Nevalainen M, Feng J, King K, Rooney M, Johnson JL, Marcotte DJ, Chodaparambil JV, Kumar PR, Patterson TA, Murugan P, Schuman E, Wong L, Hesson T, Lamore S, Bao C, Calhoun M, Certo H, Amaral B, Dillon GM, Gilfillan R, de Turiso FG. Halkina T, et al. Among authors: henderson jl. 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
Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor.
Henderson JL, Kormos BL, Hayward MM, Coffman KJ, Jasti J, Kurumbail RG, Wager TT, Verhoest PR, Noell GS, Chen Y, Needle E, Berger Z, Steyn SJ, Houle C, Hirst WD, Galatsis P. Henderson JL, et al. J Med Chem. 2015 Jan 8;58(1):419-32. doi: 10.1021/jm5014055. Epub 2014 Nov 17. J Med Chem. 2015. PMID: 25353650
SLC6A19 inhibition facilitates urinary neutral amino acid excretion and lowers plasma phenylalanine.
Wobst HJ, Viader A, Muncipinto G, Hollibaugh R, van Kalken D, Burkhart CT, Cantin SM, Bates RM, Regimbald-Dumas Y, Gross L, Antalek MT, Zweig JE, Wu F, Rettenmaier TJ, Labenski MT, Pullen N, Blanchette HS, Henderson JL, Weng HH, Vaughn TA, Brown DG, Throup JP, Barrish JC. Wobst HJ, et al. Among authors: henderson jl. JCI Insight. 2024 Nov 8;9(21):e182876. doi: 10.1172/jci.insight.182876. JCI Insight. 2024. PMID: 39513367 Free article. Clinical Trial.
139 results