PPARα and PPARγ regulate the nucleoside transporter hENT1

Biochemical and Biophysical Research Communications
Trinidad D MonteroAndrea V Leisewitz

Abstract

Human equilibrative nucleoside transporter 1 (hENT1) is an important determinant for nucleoside analog based chemotherapy success. Preliminary data suggest hENT1 regulation by PPARs. Using A2780 cells, we investigated the role of PPARs on hENT1 expression and activity. PPARα and PPARγ agonists, Wy14,643 and RGZ, increased hENT1 expression, but only PPARα activation or overexpression resulted in higher hENT1 transport activity. On the other hand, promoter analysis showed two putative PPRE in hENT1 promoter and luciferase-coupled promoter constructs were generated and analyzed. Our results suggest that PPARα-but not PPARγ-mediated expression regulation of hENT1 is PPRE-dependent. In conclusion, PPARα and PPARγ activation modulate hENT1 expression.

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Citations

Aug 28, 2012·Pharmacogenomics·Ashkan Emadi, Judith E Karp
Jul 7, 2016·Pharmacogenomics·Juan Eduardo Megías-VericatSalvador F Aliño
Apr 8, 2014·Neurochemistry International·Alexandre Dos Santos-RodriguesImogen R Coe
May 22, 2016·Molecular Carcinogenesis·Jingjing GongAddanki P Kumar
Jan 23, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Adriano Cleis ArrudaRonaldo Carvalho Araujo
Jan 17, 2021·Molecular Aspects of Medicine·Sara LamorteTracy L McGaha

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