Liu Wanling, Mossel Pascalle, Schwach Verena, Slart Riemer H J A, Luurtsema Gert
Department of Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, University of Groningen, Hanzeplein 1, 9713 GZ Groningen, The Netherlands.
Department of Applied Stem Cell Technologies, TechMed Centre, University of Twente, 7500 AE Enschede, The Netherlands.
Pharmaceuticals (Basel). 2023 Dec 11;16(12):1715. doi: 10.3390/ph16121715.
Adenosine triphosphate binding cassette (ABC) transporters are a broad family of membrane protein complexes that use energy to transport molecules across cells and/or intracellular organelle lipid membranes. Many drugs used to treat cardiac diseases have an affinity for these transporters. Among others, P-glycoprotein (P-gp) plays an essential role in regulating drug concentrations that reach cardiac tissue and therefore contribute to cardiotoxicity. As a molecular imaging modality, positron emission tomography (PET) has emerged as a viable technique to investigate the function of P-gp in organs and tissues. Using PET imaging to evaluate cardiac P-gp function provides new insights for drug development and improves the precise use of medications. Nevertheless, information in this field is limited. In this review, we aim to examine the current applications of ABC transporter PET imaging and its tracers in the heart, with a specific emphasis on P-gp. Furthermore, the opportunities and challenges in this novel field will be discussed.
三磷酸腺苷结合盒（ABC）转运蛋白是一类广泛的膜蛋白复合物，它们利用能量将分子跨细胞和/或细胞内细胞器脂质膜进行转运。许多用于治疗心脏病的药物对这些转运蛋白具有亲和力。其中，P-糖蛋白（P-gp）在调节到达心脏组织的药物浓度方面起着至关重要的作用，因此会导致心脏毒性。作为一种分子成像方式，正电子发射断层扫描（PET）已成为研究器官和组织中P-gp功能的可行技术。利用PET成像评估心脏P-gp功能为药物开发提供了新的见解，并改善了药物的精准使用。然而，该领域的信息有限。在本综述中，我们旨在研究ABC转运蛋白PET成像及其示踪剂在心脏中的当前应用，特别强调P-gp。此外，还将讨论这一新兴领域的机遇和挑战。
