Click here to close Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly. We suggest using a current version of Chrome, FireFox, or Safari.
XB-ART-52179
Drug Metab Pharmacokinet 2016 Jun 01;313:218-23. doi: 10.1242/dev.138057.
Show Gene links Show Anatomy links

Effect of diclofenac on SLC16A3/MCT4 by the Caco-2 cell line.

Sasaki S , Futagi Y , Ideno M , Kobayashi M , Narumi K , Furugen A , Iseki K .


???displayArticle.abstract???
In the present study, we demonstrated that monocarboxylate transporter 4 (MCT4) is functionally expressed in Caco-2 cells. We studied the effects of 4 nonsteroidal anti-inflammatory drugs on the uptake of l-lactate as a good substrate of MCT4 by the cells. The monocarboxylate drugs inhibited the uptake of l-lactate into the cells. Diclofenac, as a member of the aryl-acetic acid group of nonsteroidal anti-inflammatory drugs, was the most potent inhibitor, with an inhibition constant of 20 μM. In the next study, we determined the type of inhibition for diclofenac. An l-lactate carrier is non-competitively inhibitable by the drug. We also demonstrated, in Xenopus oocyte expression system, potential of diclofenac for MCT4 inhibitor. The present results could provide a useful tool to discover MCT4-specific inhibitors.

???displayArticle.pubmedLink??? 27236641
???displayArticle.link??? Drug Metab Pharmacokinet


Species referenced: Xenopus laevis
Genes referenced: slc16a3