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Early Clinical PET Imaging Results with the Novel PHF-Tau Radioligand [F-18]-T807
Abstract
Aggregates of hyperphosphorylated tau (PHF-tau), such as neurofibrillary tangles, are linked to the degree of cognitive impairment in Alzheimer's disease. We have developed a novel PHF-tau targeting positron emission tomography imaging agent, [F-18]-T807, which may be useful for imaging Alzheimer's disease and other tauopathies. Here in, we describe the first human brain images with [F-18]-T807.
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In the citing paper
“However, at least one first-generation ligand has emerged as a reliable biomarker of 3R/4R PHF tau deposits [28].”
From NIA‐AA Research Framework: Toward a biological definition of Alzheimer's disease (2018) · cites this paper as [28]
In the citing paper
“18F-AV-1451 was originally developed to bind to paired helical filament tau in Alzheimer’s disease (Zhang et al., 2012; Chien et al., 2013; Xia et al., 2013), and has been extensively used in Alzheimer’s and non-Alzheimer’s diseases.”
From Neuroinflammation and protein aggregation co-localize across the frontotemporal dementia spectrum (2020) · cites this paper as Chien et al., 2013
In the citing paper
“Imaging biomarkers for cortical tau have become available.19,20”
From Positron Emission Tomography Imaging With [ 18 F]flortaucipir and Postmortem Assessment of Alzheimer Disease Neuropathologic Changes (2020) · cites this paper as [19]
In the citing paper
“Flortaucipir is being developed as a PET tracer for detection of the aggregated tau of AD.19,21,22,23,24”
From Positron Emission Tomography Imaging With [ 18 F]flortaucipir and Postmortem Assessment of Alzheimer Disease Neuropathologic Changes (2020) · cites this paper as [19]
In the citing paper
“As expected, in vitro QC-01–175 and T807 displayed a significantly lower affinity for all recombinant immobilized tau forms than the reported KD of T807 for native, aggregated tau filaments from AD brain sections (KD15 nM)”
From Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models (2019) · cites this paper as Chien et al., 2013
In the citing paper
“However, small-molecule probes against tau oligomeric species, such as 18F-T807, have been developed and are currently in use as clinical tau PET tracers190.”
From PROTAC targeted protein degraders: the past is prologue (2022) · cites this paper as [190]
Citations
Cited by
Sorted by citations
NIA‐AA Research Framework: Toward a biological definition of Alzheimer's disease
Jack, C. R., Bennett, D. A., Blennow, K., Carrillo, M. C., Dunn, B., Haeberlein, S. B., Holtzman, D. M., Jagust, W., Jessen, F., Karlawish, J., et al. (2018) · Alzheimer's & Dementia · doi:10.1016/j.jalz.2018.02.018 · Cited by 10,537
“However, at least one firstgeneration ligand has emerged as a reliable biomarker of 3R/4R PHF tau deposits [28].”
The amyloid hypothesis of Alzheimer's disease at 25 years
Selkoe, D. J., & Hardy, J. (2016) · EMBO Molecular Medicine · doi:10.15252/emmm.201606210 · Cited by 6,164
“The recent development of imaging agents for tangles (Chien et al, 2013; Liang et al, 2014) will help define the time course of accrual of the two major lesions, although tangles are somewhat non-specific in that they occur increasingly with “normal” aging and in several neurodegenerative processes…”
BackgroundPROTAC targeted protein degraders: the past is prologue
Békés, M., Langley, D. R., & Crews, C. M. (2022) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00371-6 · Cited by 3,395
2018 Alzheimer's disease facts and figures
Alzheimer's Association (2018) · Alzheimer's & Dementia · doi:10.1016/j.jalz.2018.02.001 · Cited by 1,912
Preclinical Alzheimer’s Disease: Definition, Natural History, and Diagnostic Criteria
Dubois, B., Hampel, H., Feldman, H. H., Scheltens, P., Aisen, P., Andrieu, S., Bakardjian, H., Benali, H., Bertram, L., Blennow, K., et al. (2016) · Alzheimer's & Dementia · doi:10.1016/j.jalz.2016.02.002 · Cited by 1,925
“Early human studies show (even with small numbers) the expected correlations with cognitive state and brain atrophy [83,85,86].”
Background
Metadata
- Authors
- Chien, D. T., Bahri, S., Szardenings, A. K., Walsh, J. C., Mu, F., Su, M.-Y., Shankle, W. R., Elizarov, A., & Kolb, H. C.
- Affiliations
- Siemens Molecular Imaging, Inc., Culver City, CA, USA
- University of California, Irvine (US)
- Hoag Memorial Hospital Presbyterian (US)
- Venue
- Journal of Alzheimer's Disease
- Publisher
- SAGE Publications
- Published
- 2013-06-20
- Volume
- 34
- Issue
- 2
- Pages
- 457-468
- ISSN
- 1387-2877 (ISSN-L)
- 1875-8908
- OpenAlex
- W4235092975
- Cited by
- 651
- References
- 0
- Citations by year
- 2026: 14 · 2025: 26 · 2024: 19 · 2023: 31 · 2022: 40 · 2021: 51 · 2020: 49 · 2019: 49 · 2018: 57 · 2017: 88 · 2016: 87 · 2015: 62 · 2014: 54 · 2013: 23
- FWCI
- 52.32
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Alzheimer s Disease (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Alzheimer's disease research and treatments
- Health Sciences › Medicine › Psychiatry and Mental health › Dementia and Cognitive Impairment Research
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Medical Imaging Techniques and Applications
- Keywords
- PHF-tau
- MeSH terms
- Aged, Aged, 80 and over, Alzheimer Disease, Carbolines, Female, Fluorine Radioisotopes, Frontal Lobe, Humans, Male, Middle Aged, Phosphorylation, tau Proteins, Early Diagnosis, Positron-Emission Tomography
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