Dataset Information

Synthesis and Evaluation of ¹¹C- and ¹⁸F-Labeled SOAT1 Inhibitors as Macrophage Foam Cell Imaging Agents.

ABSTRACT: PD-132301, an inhibitor of sterol O-acyltransferase 1 (SOAT1; also known as acyl-coenzyme A:cholesterol acyltransferase-1, ACAT1), is under clinical investigation for numerous adrenal disorders. Radiolabeled SOAT1 inhibitors could support drug discovery and help diagnose SOAT1-related disorders, such as atherosclerosis. We synthesized two radiolabeled SOAT1 inhibitors, [¹¹C]PD-132301 and fluorine analogue [¹⁸F]1. Rat biodistribution studies were conducted with both agents and, as the most selective tracer, [¹¹C]PD-132301 was advanced to preclinical positron emission tomography studies in (atherosclerotic) ApoE^-/- mice. The uptake of [¹¹C]PD-132301 in SOAT1-rich tissue warrants further investigation into the compound as an atherosclerosis and adrenal imaging agent.

SUBMITTER: Hill JR

PROVIDER: S-EPMC7294710 | biostudies-literature | 2020 Jun

REPOSITORIES: biostudies-literature

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Synthesis and Evaluation of 11C- and 18F-Labeled SOAT1 Inhibitors as Macrophage Foam Cell Imaging Agents.

Hill James R JR Shao Xia X Wright Jay S JS Stauff Jenelle J Sherman Phillip S PS Arteaga Janna J Wong Ka Kit KK Viglianti Benjamin L BL Scott Peter J H PJH Brooks Allen F AF

ACS medicinal chemistry letters 20200430 6

PD-132301, an inhibitor of sterol O-acyltransferase 1 (SOAT1; also known as acyl-coenzyme A:cholesterol acyltransferase-1, ACAT1), is under clinical investigation for numerous adrenal disorders. Radiolabeled SOAT1 inhibitors could support drug discovery and help diagnose SOAT1-related disorders, such as atherosclerosis. We synthesized two radiolabeled SOAT1 inhibitors, [11C]PD-132301 and fluorine analogue [18F]1. Rat biodistribution studies were conducted with ...[more]

PMID: 32551015

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Dataset Information

Synthesis and Evaluation of ¹¹C- and ¹⁸F-Labeled SOAT1 Inhibitors as Macrophage Foam Cell Imaging Agents.

Publications

Synthesis and Evaluation of <sup>11</sup>C- and <sup>18</sup>F-Labeled SOAT1 Inhibitors as Macrophage Foam Cell Imaging Agents.

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