Discovery of Potent and Brain-Penetrant Tau Tubulin Kinase 1 (TTBK1) Inhibitors that Lower Tau Phosphorylation In Vivo.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00382
Abstract: Structural analysis of the known NIK inhibitor 3 bound to the kinase domain of TTBK1 led to the design and synthesis of a novel class of azaindazole TTBK1 inhibitors exemplified by 8 (cell IC50: 571… read more here.
Keywords: tau; discovery potent; ttbk1 inhibitors; kinase ... See more keywords
Adult onset pan-neuronal human tau tubulin kinase 1 expression causes severe cerebellar neurodegeneration in mice
Sign Up to like & getrecommendations! Published in 2020 at "Acta Neuropathologica Communications"
DOI: 10.1186/s40478-020-01073-7
Abstract: The kinase TTBK1 is predominantly expressed in the central nervous system and has been implicated in neurodegenerative diseases including Alzheimer’s disease, frontotemporal lobar degeneration, and amyotrophic lateral sclerosis through its ability to phosphorylate the proteins tau… read more here.
Keywords: severe cerebellar; pan neuronal; neurodegeneration; expression ... See more keywords