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Department of Anesthesiology and Molecular Biology Institute,
University of California, Los Angeles School of Medicine, Los Angeles,
California 90095
Palmitoylation of the V2 vasopressin receptor (V2R) and its
functional role were investigated in transfected cells. Palmitoylation was assessed by incubating transfected cells with
[3H]palmitic acid and immunoprecipitating the receptor
with an antibody raised against a portion of the third intracellular
loop of V2R. Wild-type and nonglycosylated V2R yielded tritium signals
at 45-55 and 40 kDa, respectively, demonstrating that the V2R is
palmitoylated and that receptor palmitoylation is independent of
glycosylation. Substitution of CC341/342 for serines eliminated
receptor palmitoylation, whereas replacement of a single amino acid,
C341S or C342S, restored partial palmitoylation. Saturation binding
assays revealed decreased cell surface expression of the
nonpalmitoylated receptor compared with the wild-type; this effect was
more pronounced when a truncated form of V2R (G345ter) was studied. The
presence of either cysteine residue (C341S or C342S) elevated receptor
expression to normal levels, most likely due to the partial restoration
of palmitoylation. Ligand binding affinity, hormone-induced stimulation
of adenylyl cyclase activity, receptor internalization, and
desensitization were not affected by the absence of palmitoylation. No
increase but rather a slight decrease in the extent of receptor
palmitoylation was detected after exposure to vasopressin. It was
concluded that the V2R is palmitoylated in both cysteines, each
cysteine is palmitoylated independently from the other, and
palmitoylation enhances cell surface expression of the V2R.
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