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Rapid Regulation of Human Multidrug and Extrusion Transporters hMATE1 and hMATE2K

Medicine Clinic D, Experimental Nephrology, University Hospital of Münster, 48149 Münster, Germany
Author to whom correspondence should be addressed.
These authors equally contributed to the manuscript.
Int. J. Mol. Sci. 2020, 21(14), 5157;
Received: 4 June 2020 / Revised: 17 July 2020 / Accepted: 20 July 2020 / Published: 21 July 2020
Vectorial transport of organic cations (OCs) in renal proximal tubules is mediated by sequential action of human OC transporter 2 (hOCT2) and human multidrug and toxic extrusion protein 1 and 2K (hMATE1 and hMATE2K), expressed in the basolateral (hOCT2) and luminal (hMATE1 and hMATE2K) plasma membranes, respectively. It is well known that hOCT2 activity is subjected to rapid regulation by several signaling pathways, suggesting that renal OC secretion may be acutely adapted to physiological requirements. Therefore, in this work, the acute regulation of hMATEs stably expressed in human embryonic kidney cells was characterized using the fluorescent substrate 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP+) as a marker. A specific regulation of ASP+ transport by hMATE1 and hMATE2K measured in uptake and efflux configurations was observed. In the example of hMATE1 efflux reduction by inhibition of casein kinase II, it was also shown that this regulation is able to modify transcellular transport of ASP+ in Madin–Darby canine kidney II cells expressing hOCT2 and hMATE1 on the basolateral and apical membrane domains, respectively. The activity of hMATEs can be rapidly regulated by some intracellular pathways, which sometimes are common to those found for hOCTs. Interference with these pathways may be important to regulate renal secretion of OCs. View Full-Text
Keywords: organic cations; transport; kidneys; regulation organic cations; transport; kidneys; regulation
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MDPI and ACS Style

Kantauskaitė, M.; Hucke, A.; Reike, M.; Ahmed Eltayeb, S.; Xiao, C.; Barz, V.; Ciarimboli, G. Rapid Regulation of Human Multidrug and Extrusion Transporters hMATE1 and hMATE2K. Int. J. Mol. Sci. 2020, 21, 5157.

AMA Style

Kantauskaitė M, Hucke A, Reike M, Ahmed Eltayeb S, Xiao C, Barz V, Ciarimboli G. Rapid Regulation of Human Multidrug and Extrusion Transporters hMATE1 and hMATE2K. International Journal of Molecular Sciences. 2020; 21(14):5157.

Chicago/Turabian Style

Kantauskaitė, Marta, Anna Hucke, Moritz Reike, Sara Ahmed Eltayeb, Chuyan Xiao, Vivien Barz, and Giuliano Ciarimboli. 2020. "Rapid Regulation of Human Multidrug and Extrusion Transporters hMATE1 and hMATE2K" International Journal of Molecular Sciences 21, no. 14: 5157.

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