Regulation of organic anion transporters: Role in physiology, pathophysiology, and drug elimination

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. (C) 2020 Elsevier Inc. All rights reserved.

Automated summary

Members of the OAT family are mainly expressed in kidney, liver, placenta, intestine, and brain, playing crucial roles in maintaining systemic homeostasis. Alterations in OAT expression and function can impact therapeutic efficacy, toxicity, and pathophysiological conditions. Understanding the regulation of OATs at the cellular and molecular levels can provide insights into their roles in health and disease.