School of Life Sciences, The University of Nottingham, Nottingham NG7 2UH, UK.
Laboratory of Molecular Cancer Biology, Molecular Physiology Research Unit (URPHYM), Namur Research Institute for Life Sciences, Faculty of Medicine, Department of Biomedical Sciences, The University of Namur, Namur, Belgium.
Biochim Biophys Acta Mol Cell Biol Lipids. 2021 Mar;1866(3):158860. doi: 10.1016/j.bbalip.2020.158860. Epub 2020 Dec 11.
Members of the ATP binding cassette (ABC) transporter family perform a critical function in maintaining lipid homeostasis in cells as well as the transport of drugs. In this review, we provide an update on the ABCG-transporter subfamily member proteins, which include the homodimers ABCG1, ABCG2 and ABCG4 as well as the heterodimeric complex formed between ABCG5 and ABCG8. This review focusses on progress made in this field of research with respect to their function in health and disease and the recognised transporter substrates. We also provide an update on post-translational regulation, including by transporter substrates, and well as the involvement of microRNA as regulators of transporter expression and activity. In addition, we describe progress made in identifying structural elements that have been recognised as important for transport activity. We furthermore discuss the role of lipids such as cholesterol on the transport function of ABCG2, traditionally thought of as a drug transporter, and provide a model of potential cholesterol binding sites for ABCG2.
三磷酸腺苷结合盒（ABC）转运蛋白家族的成员在维持细胞内脂质平衡以及药物转运方面发挥着关键作用。在这篇综述中，我们更新了 ABCG-转运蛋白亚家族成员蛋白的信息，包括同源二聚体 ABCG1、ABCG2 和 ABCG4 以及 ABCG5 和 ABCG8 形成的异二聚体复合物。这篇综述重点介绍了在健康和疾病方面其功能以及公认的转运体底物方面的研究进展。我们还提供了关于翻译后调节的最新信息，包括转运体底物的调节，以及 microRNA 作为转运体表达和活性调节剂的参与情况。此外，我们描述了在确定被认为对转运活性很重要的结构元件方面所取得的进展。我们还讨论了胆固醇等脂质在传统上被认为是药物转运体的 ABCG2 转运功能中的作用，并为 ABCG2 的潜在胆固醇结合位点提供了一个模型。
