MDM2 E3 ubiquitin ligase mediates UT-A1 urea transporter ubiquitination and degradation.
UT-A1 is the primary urea transporter in the apical plasma membrane responsible for urea reabsorption in the inner medullary collecting duct. Although the physiological function of UT-A1 has been well established, the molecular mechanisms that regulate its activity are less well understood. Analysis of the UT-A1 amino acid sequence revealed ... a potential MDM2 E3 ubiquitin ligase-binding motif in the large intracellular loop of UT-A1, suggesting that UT-A1 urea transporter protein may be regulated by the ubiquitin-proteasome pathway. Here, we report that UT-A1 is ubiquitinated and degraded by the proteasome but not the lysosome proteolytic pathway. Inhibition of proteasome activity causes UT-A1 cell surface accumulation and concomitantly increases urea transport activity. UT-A1 interacts directly with MDM2; the binding site is located in the NH2-terminal p53-binding region of MDM2. MDM2 mediates UT-A1 ubiquitination both in vivo and in vitro. Overexpression of MDM2 promotes UT-A1 degradation. The mechanism is likely to be physiologically important as UT-A1 ubiquitination was identified in kidney inner medullary tissue. The ubiquitin-proteasome degradation pathway provides an important novel mechanism for UT-A1 regulation.
Mesh Terms:
Animals, Binding Sites, Cell Line, Cell Membrane, Cycloheximide, Dogs, Enzyme Inhibitors, Humans, Imidazoles, Kidney Medulla, Leupeptins, Male, Membrane Transport Proteins, Mice, Piperazines, Protease Inhibitors, Proteasome Endopeptidase Complex, Protein Binding, Proto-Oncogene Proteins c-mdm2, Rats, Rats, Sprague-Dawley, Sequence Deletion, Ubiquitin-Protein Ligases, Ubiquitination, Urea
Animals, Binding Sites, Cell Line, Cell Membrane, Cycloheximide, Dogs, Enzyme Inhibitors, Humans, Imidazoles, Kidney Medulla, Leupeptins, Male, Membrane Transport Proteins, Mice, Piperazines, Protease Inhibitors, Proteasome Endopeptidase Complex, Protein Binding, Proto-Oncogene Proteins c-mdm2, Rats, Rats, Sprague-Dawley, Sequence Deletion, Ubiquitin-Protein Ligases, Ubiquitination, Urea
Am. J. Physiol. Renal Physiol.
Date: Nov. 01, 2008
PubMed ID: 18784257
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