4NFN

Human tau tubulin kinase 1 (TTBK1) complexed with 3-({5-[(4-amino-4-methylpiperidin-1-yl)methyl]pyrrolo[2,1-f][1,2,4]triazin-4-yl}amino)-5-bromophenol

Summary for 4NFN

• Entry DOI: 10.2210/pdb4nfn/pdb
• Related: 4NFM
• Descriptor: Tau-tubulin kinase 1, 3-({5-[(4-amino-4-methylpiperidin-1-yl)methyl]pyrrolo[2,1-f][1,2,4]triazin-4-yl}amino)-5-bromophenol, SULFATE ION, ... (4 entities in total)
• Functional Keywords: protein kinase, phosphotransferase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Cytoplasm: Q5TCY1
• Total number of polymer chains: 1
• Total formula weight: 36184.45

Authors

Sheriff, S. (deposition date: 2013-10-31, release date: 2014-02-05, Last modification date: 2023-09-20)

Primary citation

Kiefer, S.E.,Chang, C.J.,Kimura, S.R.,Gao, M.,Xie, D.,Zhang, Y.,Zhang, G.,Gill, M.B.,Mastalerz, H.,Thompson, L.A.,Cacace, A.M.,Sheriff, S.
The structure of human tau-tubulin kinase 1 both in the apo form and in complex with an inhibitor.
Acta Crystallogr F Struct Biol Commun, 70:173-181, 2014

PubMed 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.

PubMed: 24637750
DOI: 10.1107/S2053230X14000144

Experimental method

X-RAY DIFFRACTION (1.42 Å)