The members of the organic anion transporter (OAT) family are mainly expressed in kidney, liver, placenta, intestine, and brain. These transporters play important roles in the disposition of clinical drugs, pesticides, signaling molecules, heavy metal conjugates, components of phytomedicines, and toxins, and therefore critical for maintaining systemic homeostasis. Alterations in the expression and function of OATs contribute to the intra- and inter-individual variability of the therapeutic efficacy and the toxicity of many drugs, and to many pathophysiological conditions. Consequently, the activity of these transporters must be highly regulated to carry out their normal functions. This review will present an update on the recent advance in understanding the cellular and molecular mechanisms underlying the regulation of renal OATs, emphasizing on the post-translational modification (PTM), the crosstalk among these PTMs, and the remote sensing and signaling network of OATs. Such knowledge will provide significant insights into the roles of these transporters in health and disease.

有机阴离子转运蛋白（OAT）家族的成员主要在肾脏、肝脏、胎盘、肠和脑中表达。这些转运蛋白在临床药物、杀虫剂、信号分子、重金属结合物、植物药物成分和毒素的处置中发挥重要作用，因此对于维持系统稳态至关重要。OAT 表达和功能的改变导致治疗功效和许多药物毒性的个体内部和个体间差异，以及许多病理生理条件。因此，必须高度调节这些转运蛋白的活动以执行其正常功能。这篇综述将介绍最近在理解肾 OATs 调控的细胞和分子机制方面的最新进展，强调翻译后修饰 (PTM)、这些 PTM 之间的串扰以及 OAT 的遥感和信令网络。这些知识将为了解这些转运蛋白在健康和疾病中的作用提供重要的见解。