PKC regulation of the human equilibrative nucleoside transporter, hENT1

FEBS Letters

Coe, Imogen¹  Zhang, Ying¹  Naydenova, Zlatina¹  McKenzie, Tamara¹ 

[1] Department of Biology, York University, 4700 Keele St., Toronto, Canada M3J 1P3

关键词: Nucleoside transporter;    Human equilibrative nucleoside transporter 1;    Regulation;    Protein kinase C;    PKC;    protein kinase C;    NBTI;    S-(4-nitrobenzyl)-6-thioinosine;    hENT1;    human equilibrative nucleoside transporter 1;   

DOI  :  10.1016/S0014-5793(02)02622-4

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Regulation of nucleoside transporters is poorly understood. We show that acute stimulation of protein kinase C (PKC) causes a rapid increase in S-(4-nitrobenzyl)-6-thioinosine-sensitive (human equilibrative nucleoside transporter 1, hENT1) nucleoside uptake, in human cultured cells, which is not due to increased metabolism and which can be blocked by PKC inhibitors. Use of isoform-specific inhibitors indicates that PKC δ and/or ϵ (but not α, β or γ) are responsible for the acute effects. Down-regulation of PKC decreases hENT1-dependent uridine uptake. These are the first data to show rapid PKC δ/ϵ-dependent stimulation of hENT1 transport by a mechanism that may involve activation of transporters at the membrane possibly by post-translational modification of the protein.

【 授权许可】

Unknown