使用含18F的残留标记正电子发射断层扫描对脂蛋白代谢进行定量评估。

Quantitative assessment of lipoprotein metabolism by positron emission tomography with an 18F-containing residualizing label.

作者信息

Daugherty A, Kilbourn M R, Dence C S, Sobel B E, Thorpe S R

机构信息

Cardiovascular Division, Washington University, School of Medicine, St. Louis, MO 63110.

出版信息

Int J Rad Appl Instrum B. 1992 Apr;19(3):411-6. doi: 10.1016/0883-2897(92)90127-k.

DOI:10.1016/0883-2897(92)90127-k

PMID:1629030

Abstract

Residualizing labels for proteins are designed to remain entrapped within cells following uptake and degradation of the carrier protein. In the present work we report the synthesis of a novel residualizing label, N-lactitol-S-([18F]fluorophenacyl)-cysteamine ([18F]LCSH, and its use for quantifying the accumulation of low density lipoprotein in tissues in vivo by positron emission tomography (PET). The retention of degradation products in tissues from lipoprotein or from other rapidly catabolized protein pharmaceuticals tagged with [18F]LCSH reduces leakage of tracer into the plasma compartment. Thus, residualizing labels provide a valuable tool for enhancing signal-to-noise ratios, even during the relatively short interval of PET studies.

摘要

蛋白质的残留标记物设计为在载体蛋白被摄取和降解后仍滞留在细胞内。在本研究中，我们报道了一种新型残留标记物N-乳糖醇-S-([18F]氟苯甲酰)-半胱胺（[18F]LCSH）的合成，及其用于通过正电子发射断层扫描（PET）在体内定量组织中低密度脂蛋白的积累。用[18F]LCSH标记的脂蛋白或其他快速分解代谢的蛋白质药物在组织中的降解产物保留减少了示踪剂泄漏到血浆区室。因此，即使在PET研究相对较短的时间间隔内，残留标记物也是提高信噪比的有价值工具。