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[ 18 F]PRIMATX, a New Positron Emission Tomography Tracer for Imaging of Autotaxin in Lung Tissue and Tumor‐Bearing Mice
Author(s) -
Briard Emmanuelle,
Joshi Aniket D.,
Shanmukhappa Shiva,
Ilovich Ohad,
Auberson Yves P.
Publication year - 2019
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201900297
Subject(s) - autotaxin , positron emission tomography , in vivo , lung , fibrosis , pathology , chemistry , medicine , ex vivo , cancer research , nuclear medicine , biology , biochemistry , in vitro , receptor , lysophosphatidic acid , microbiology and biotechnology
Autotaxin (ATX) is a secreted enzyme with tissue levels associated with tissue injury, which increase during wound healing and chronic fibrotic diseases. We selected [ 18 F]( R , E )‐3‐(4‐chloro‐2‐((5‐methyl‐2 H ‐tetrazol‐2‐yl)methyl)phenyl)‐1‐(4‐((5‐(2‐fluoroethoxy)pyridin‐2‐yl)methyl)‐2‐methylpiperazin‐1‐yl)prop‐2‐en‐1‐one ([ 18 F]PRIMATX, [ 18 F] 2 ), a tracer for positron emission tomography, to image ATX expression in vivo. It successfully differentiates expression levels in lung tissue samples from idiopathic pulmonary fibrosis patients, and allows the detection of ATX‐expressing tumors in living mice, confirming its potential for development as a clinical imaging agent.