ArticleEuropean journal of nuclear medicine and molecular imaging2025
Development of lisinopril radioconjugates for nuclear imaging of the angiotensin converting enzyme.
Article in European journal of nuclear medicine and molecular imaging, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
purposeThe angiotensin converting enzyme (ACE) is essential in maintaining cardiovascular homeostasis and its dysfunction is associated with various pathological conditions. This study aimed to investigate lisinopril-based radioconjugates for nuclear imaging of ACE.
methodsLisinopril conjugates were prepared using solid-phase peptide synthesis and labeled with gallium-67. The resulting radioconjugates were assessed for their in vitro stability in saline and in mouse and human blood plasma. ACE-mediated uptake was evaluated in HEK cells transfected with human ACE, and the findings were interpreted using molecular dynamic studies. Tissue distribution profiles of the radioconjugates were evaluated in mice bearing HEK-ACE xenografts by means of nuclear imaging and classic biodistribution studies. The feasibility to detect physiologic ACE was further assessed by ex vivo autoradiography of the lungs and the kidneys collected from mice injected with [
resultsDOTA-LIS-01, DOTA-LIS-02 and NODAGA-LIS-02 were prepared with > 98% chemical purity. Radiolabeling of the conjugates with gallium-67 was achieved at 80 MBq/nmol with > 99% radiochemical purity. [
conclusion[
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