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In Vivo Visualizati...
In Vivo Visualization of beta-Cells by Targeting of GPR44
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- Eriksson, Olof (author)
- Uppsala universitet,Theranostics
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- Johnstrom, P. (author)
- Karolinska Institutet, Karolinska University Hospital, Stockholm, Sweden
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- Cselenyi, Z. (author)
- Karolinska Institutet
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- Jahan, M. (author)
- Karolinska Institutet and Stockholm County Council, Stockholm, Sweden
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- Selvaraju, Ram kumar (author)
- Uppsala universitet,Plattformen för Preklinisk PET-MRI
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- Jensen Waern, Marianne (author)
- Swedish University of Agricultural Sciences,Sveriges lantbruksuniversitet,Institutionen för kliniska vetenskaper (KV),Department of Clinical Sciences,Swedish University of Agricultural Sciences, Uppsala, Sweden
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- Takano, A. (author)
- Karolinska Institutet and Stockholm County Council, Stockholm, Sweden
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- Skrtic, Stanko, 1970 (author)
- Gothenburg University,Göteborgs universitet,Institutionen för medicin, avdelningen för invärtesmedicin och klinisk nutrition,Institute of Medicine, Department of Internal Medicine and Clinical Nutrition,Sahlgrenska Academy, University of Gothenburg, Gothenburg, Sweden
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- Halldin, C. (author)
- Karolinska Institutet
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- Skrtic, Stanko, 1970 (author)
- Gothenburg University,Göteborgs universitet,Institutionen för medicin, avdelningen för invärtesmedicin och klinisk nutrition,Institute of Medicine, Department of Internal Medicine and Clinical Nutrition
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- Korsgren, Olle (author)
- Uppsala universitet,Klinisk immunologi
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- Sörhede Winzell, Maria (author)
- AstraZeneca R&D, Mölndal, Sweden
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(creator_code:org_t)
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- 2017-12-05
- 2018
- English.
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In: Diabetes. - : American Diabetes Association. - 0012-1797 .- 1939-327X. ; 67:2, s. 182-192
- Related links:
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https://diabetes.dia...
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https://gup.ub.gu.se...
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https://doi.org/10.2...
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Abstract
Subject headings
Close
- GPR44 expression has recently been described as highly beta-cell selective in the human pancreas and constitutes a tentative surrogate imaging biomarker in diabetes. A radiolabeled small-molecule GPR44 antagonist, [C-11]AZ12204657, was evaluated for visualization of beta-cells in pigs and non-human primates by positron emission tomography as well as in immunodeficient mice transplanted with human islets under the kidney capsule. In vitro autoradiography of human and animal pancreatic sections from subjects without and with diabetes, in combination with insulin staining, was performed to assess beta-cell selectivity of the radiotracer. Proof of principle of in vivo targeting of human islets by [C-11]AZ12204657 was shown in the immunodeficient mouse transplantation model. Furthermore, [C-11]AZ12204657 bound by a GPR44-mediated mechanism in pancreatic sections from humans and pigs without diabetes, but not those with diabetes. In vivo [C-11]AZ12204657 bound specifically to GPR44 in pancreas and spleen and could be competed away dose-dependently in nondiabetic pigs and nonhuman primates. [C-11]AZ12204657 is a first-in-class surrogate imaging biomarker for pancreatic beta-cells by targeting the protein GPR44.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Endokrinologi och diabetes (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Endocrinology and Diabetes (hsv//eng)
Keyword
- receptor
Publication and Content Type
- ref (subject category)
- art (subject category)
Find in a library
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Diabetes
(Search for host publication in LIBRIS)
To the university's database
- By the author/editor
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Eriksson, Olof
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Johnstrom, P.
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Cselenyi, Z.
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Jahan, M.
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Selvaraju, Ram k ...
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Jensen Waern, Ma ...
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show more...
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Takano, A.
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Skrtic, Stanko, ...
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Halldin, C.
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Korsgren, Olle
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Sörhede Winzell, ...
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- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Clinical Medicin ...
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and Endocrinology an ...
- Articles in the publication
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Diabetes
- By the university
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University of Gothenburg
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Swedish University of Agricultural Sciences
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Uppsala University
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Karolinska Institutet