The DOI matches its Crossref record; 15 of the 15 references it cites were found in a registry or an index.
18F-THK523: a novel in vivo tau imaging ligand for Alzheimer's disease
Abstract
While considerable effort has focused on developing positron emission tomography β-amyloid imaging radiotracers for the early diagnosis of Alzheimer's disease, no radiotracer is available for the non-invasive quantification of tau. In this study, we detail the characterization of (18)F-THK523 as a novel tau imaging radiotracer. In vitro binding studies demonstrated that (18)F-THK523 binds with higher affinity to a greater number of binding sites on recombinant tau (K18Δ280K) compared with β-amyloid(1-42) fibrils. Autoradiographic and histofluorescence analysis of human hippocampal serial sections with Alzheimer's disease exhibited positive THK523 binding that co-localized with immunoreactive tau pathology, but failed to highlight β-amyloid plaques. Micro-positron emission tomography analysis demonstrated significantly higher retention of (18)F-THK523 (48%; P < 0.007) in tau transgenic mice brains compared with their wild-type littermates or APP/PS1 mice. The preclinical examination of THK523 has demonstrated its high affinity and selectivity for tau pathology both in vitro and in vivo, indicating that (18)F-THK523 fulfils ligand criteria for human imaging trials.
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Citations
Cites
Hypothetical model of dynamic biomarkers of the Alzheimer's pathological cascade
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Cited by
Jack, C. R., Knopman, D. S., Jagust, W. J., Petersen, R. C., Weiner, M. W., Aisen, P. S., Shaw, L. M., Vemuri, P., Wiste, H. J., Weigand, S. D., et al. (2013) · The Lancet Neurology · doi:10.1016/s1474-4422(12)70291-0 · Cited by 4,396
Biomarker Modeling of Alzheimer’s Disease
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Tau and neurodegenerative disease: the story so far
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Spreading of pathology in neurodegenerative diseases: a focus on human studies
Brettschneider, J., Tredici, K. D., Lee, V. M.-Y., & Trojanowski, J. Q. (2015) · Nature Reviews Neuroscience · doi:10.1038/nrn3887 · Cited by 790
Maruyama, M., Shimada, H., Suhara, T., Shinotoh, H., Ji, B., Maeda, J., Zhang, M.-R., Trojanowski, J. Q., Lee, V. M.-Y., Ono, M., et al. (2013) · Neuron · doi:10.1016/j.neuron.2013.07.037 · Cited by 760
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Metadata
- Authors
- Fodero-Tavoletti, M. T., Okamura, N., Furumoto, S., Mulligan, R. S., Connor, A. R., McLean, C. A., Cao, D., Rigopoulos, A., Cartwright, G. A., O'Keefe, G., Gong, S., Adlard, P. A., Barnham, K. J., Rowe, C. C., Masters, C. L., Kudo, Y., Cappai, R., Yanai, K., & Villemagne, V. L.
- Venue
- Brain
- Publisher
- Oxford University Press (OUP)
- Published
- 2011-03-24
- Volume
- 134
- Issue
- 4
- Pages
- 1089-1100
- ISSN
- 0006-8950 (ISSN-L)
- 1460-2156
- OpenAlex
- W2100442068
- Cited by
- 328
- References
- 15
- FWCI
- 24.08
- Type
- journal article
- Language
- en
- Open access
- closed
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- Fodero-Tavoletti, M. T., Okamura, N., Furumoto, S., Mulligan, R. S., Connor, A. R., McLean, C. A., Cao, D., Rigopoulos, A., Cartwright, G. A., O'Keefe, G., Gong, S., Adlard, P. A., Barnham, K. J., Rowe, C. C., Masters, C. L., Kudo, Y., Cappai, R., Yanai, K., & Villemagne, V. L. (2011). 18F-THK523: a novel in vivo tau imaging ligand for Alzheimer's disease. Brain. https://doi.org/10.1093/brain/awr038
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