Preparation and Evaluation of Fluorine-18-Labeled Insulin as a Molecular Imaging Probe for Studying Insulin Receptor Expression in Tumors
Publication type: Journal Article
Publication date: 2014-04-22
scimago Q1
wos Q1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
24712894
Drug Discovery
Molecular Medicine
Abstract
A convenient emulsion-based labeling method was used to synthesize fluorine-18-labeled insulin specifically B(1)-(4-[(18)F]fluorobenzoyl)insulin ((18)F-4b) in 6% overall radiochemical yield in 240 min. In vitro screening in MCF7 breast cancer cells demonstrated that the nonradioactive analogue (19)F-4a effectively competed with (125)I-insulin for the insulin receptor (IC50 = 10.6 nM) comparable to that for insulin (IC50 = 7.4 nM). (18)F-4b was also more stable than (125)I-insulin in mouse plasma with 50% remaining intact after 30 min. A biodistribution study in normal mice showed initial uptake of the tracer in the kidneys, liver, and gall bladder but rapid clearance via the urine/bladder which was also observed in murine models bearing insulin receptor positive tumors.
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Kim D., Blacker M., Valliant J. Preparation and Evaluation of Fluorine-18-Labeled Insulin as a Molecular Imaging Probe for Studying Insulin Receptor Expression in Tumors // Journal of Medicinal Chemistry. 2014. Vol. 57. No. 9. pp. 3678-3686.
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Kim D., Blacker M., Valliant J. Preparation and Evaluation of Fluorine-18-Labeled Insulin as a Molecular Imaging Probe for Studying Insulin Receptor Expression in Tumors // Journal of Medicinal Chemistry. 2014. Vol. 57. No. 9. pp. 3678-3686.
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TY - JOUR
DO - 10.1021/jm401020c
UR - https://doi.org/10.1021/jm401020c
TI - Preparation and Evaluation of Fluorine-18-Labeled Insulin as a Molecular Imaging Probe for Studying Insulin Receptor Expression in Tumors
T2 - Journal of Medicinal Chemistry
AU - Kim, Donghyun
AU - Blacker, Megan
AU - Valliant, John
PY - 2014
DA - 2014/04/22
PB - American Chemical Society (ACS)
SP - 3678-3686
IS - 9
VL - 57
PMID - 24712894
SN - 0022-2623
SN - 1520-4804
ER -
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@article{2014_Kim,
author = {Donghyun Kim and Megan Blacker and John Valliant},
title = {Preparation and Evaluation of Fluorine-18-Labeled Insulin as a Molecular Imaging Probe for Studying Insulin Receptor Expression in Tumors},
journal = {Journal of Medicinal Chemistry},
year = {2014},
volume = {57},
publisher = {American Chemical Society (ACS)},
month = {apr},
url = {https://doi.org/10.1021/jm401020c},
number = {9},
pages = {3678--3686},
doi = {10.1021/jm401020c}
}
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MLA
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Kim, Donghyun, et al. “Preparation and Evaluation of Fluorine-18-Labeled Insulin as a Molecular Imaging Probe for Studying Insulin Receptor Expression in Tumors.” Journal of Medicinal Chemistry, vol. 57, no. 9, Apr. 2014, pp. 3678-3686. https://doi.org/10.1021/jm401020c.