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Review
. 2020 Mar;15(2):181-191.
doi: 10.1016/j.ajps.2019.10.004. Epub 2019 Nov 13.

Stimulatory effect on the transport mediated by organic anion transporting polypeptide 2B1

Jiro Ogura  1 , Hiroaki Yamaguchi  1 , Nariyasu Mano  1
Affiliations
Review

Stimulatory effect on the transport mediated by organic anion transporting polypeptide 2B1

Jiro Ogura et al. Asian J Pharm Sci. 2020 Mar.

Abstract

Drug-drug interaction (DDI) is one of causes of adverse drug events and can result in life-threatening consequences. Organic anion-transporting polypeptide (OATP) 2B1 is a major uptake transporter in the intestine and contributes to transport various clinically used therapeutic agents. The intestine has a high risk of DDI, because it has a special propensity to be exposed to a high concentration of drugs. Thus, understanding drug interaction mediated by OATP2B1 in the absorption process is important for the prevention of adverse drug events, including decrease in the therapeutic effect of co-administered drugs. Acute drug interaction occurs through the direct inhibitory effect on transporters, including OATP2B1. Moreover, some compounds such as clinically used drugs and food components have an acute stimulatory effect on transport of co-administered drugs by OATP2B1. This review summarizes the acute stimulatory effect on the transport mediated by OATP2B1 and discusses the mechanisms of the acute stimulatory effects of compounds. There are two types of acute stimulatory effects, substrate-independent and -dependent interactions on OATP2B1 function. The facilitating translocation of OATP2B1 to the plasma membrane is one of causes for the substrate-independent acute stimulatory effect. On the contrary, the substrate-dependent effect is based on the direct binding to the substrate-binding site or allosteric progesterone-binding site of OATP2B1.

Keywords: Conformational change; Drug interaction; Membrane translocation; OATP2B1; Stimulatory effect.

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Figures

Image, graphical abstract
Graphical abstract
Fig 1
Fig. 1
Schematic diagrams for various types of DDI in the intestinal transporter.
Fig 2
Fig. 2
Chemical structures for Prostaglandins.
Fig 3
Fig. 3
Schematic diagrams for substrate-independent and -dependent effect on OATP2B1 function.
See this image and copyright information in PMC

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