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Acta Crystallogr F Struct Biol Commun. 2014 Feb;70(Pt 2):173-81. doi: 10.1107/S2053230X14000144. Epub 2014 Jan 21.

The structure of human tau-tubulin kinase 1 both in the apo form and in complex with an inhibitor.

Author information

1
Molecular Discovery Technologies, Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543-4000, USA.
2
Molecular Discovery Technologies, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA.
3
Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA.
4
Neuroscience Biology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA.

Abstract

Tau-tubulin kinase 1 (TTBK1) is a dual-specificity (serine/threonine and tyrosine) kinase belonging to the casein kinase 1 superfamily. TTBK1 is a neuron-specific kinase that regulates tau phosphorylation. Hyperphosphorylation of tau is implicated in the pathogenesis of Alzheimer's disease. Two kinase-domain constructs of TTBK1 were expressed in a baculovirus-infected insect-cell system and purified. The purified TTBK1 kinase-domain proteins were crystallized using the hanging-drop vapor-diffusion method. X-ray diffraction data were collected and the structure of TTBK1 was determined by molecular replacement both as an apo structure and in complex with a kinase inhibitor.

KEYWORDS:

TTBK1; inhibitors; kinase domain

PMID:
24637750
PMCID:
PMC3936456
DOI:
10.1107/S2053230X14000144
[Indexed for MEDLINE]
Free PMC Article
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