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Journal article
Development of 2-Deoxy-2-[F-18]fluororibose for Positron Emission Tomography Imaging Liver Function in Vivo
Journal of medicinal chemistry, v 58(14), pp 5538-5547
23 Jul 2015
PMID: 26102222
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
Life-threatening: acute liver failure can be triggered, by a variety of factors,, including common drugs such as acetaminophen,. Positron emission tomography (BET) is rarely used to monitor liver function, In part because of a lack of specific imaging agents for liver function.. Here we report a new PET probe, 2-deoxy-2[F-18]fluororibose ([F-18]-2-DFR), for use in imaging liver function. [F-18]-2-DFR was synthesized and validated as a competitive substrate for the ribose salvage pathway. [F-18]-2-DFR was prepared through an efficient late Stage radiofluorination. The desired selectivity of fluorination was achieved using an unorthodox protecting group on the precursor, which could withstand harsh S(N)2 reaction conditions with no side reactions.[F-18,]-2-DFR accumulated preferentially in the liver and was metabolized by the same enzymes, as ribose. [F-18]-2-DFR could distinguish between healthy liver and, liver damaged by acetaminophen. [(18)]-2-DFR is expected to-be a useful PET probe for imaging and quantifying liver functions in vivo, with likely significant clinical utility.
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Details
- Title
- Development of 2-Deoxy-2-[F-18]fluororibose for Positron Emission Tomography Imaging Liver Function in Vivo
- Creators
- Nikolai M. Evdokimov - University of California, Los AngelesPeter M. Clark - Supreme Council Of HealthGraciela Flores - Supreme Council Of HealthTimothy Chai - Supreme Council Of HealthKym F. Faull - Supreme Council Of HealthMichael E. Phelps - Supreme Council Of HealthOwen N. Witte - Supreme Council Of HealthMichael E. Jung - University of California, Los Angeles
- Publication Details
- Journal of medicinal chemistry, v 58(14), pp 5538-5547
- Publisher
- American Chemical Society; Washington, DC
- Number of pages
- 10
- Grant note
- TG2-01169 / California Institute of Regenerative Medicine Training Grant University of California Amgen Scholars Program Eli and Edythe Broad Center of Regenerative Medicine and Stem Cell Research R25CA098010 / NATIONAL CANCER INSTITUTE; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA; NIH National Cancer Institute (NCI) P50 CA086306 / UCLA in Vivo Cellular and Molecular Imaging Center Career Development Award CHE-1048804 / National Science Foundation Equipment Grant R25T CA098010 / UCLA Scholars in Oncologic Molecular Imaging Program National Cancer Institute Grant Phelps Family Foundation
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- School of Biomedical Engineering, Science, and Health Systems; Drexel University
- Web of Science ID
- WOS:000358624600013
- Scopus ID
- 2-s2.0-84937675824
- Other Identifier
- 991019356495404721
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- Collaboration types
- Domestic collaboration
- Web of Science research areas
- Chemistry, Medicinal