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The rat type 1a (AT
Volume 270,
Number 17,
Issue of April 28, pp. 9702-9705, 1995
©1995 by The American Society for Biochemistry and Molecular Biology, Inc.
) angiotensin II (Ang II)
receptor contains a highly conserved tyrosine residue in the fifth
transmembrane region that is present in most G protein-coupled
receptors. The role of this amino acid in AT
receptor
activation was analyzed in a mutant receptor (Y215F) created by
replacing Tyrwith phenylalanine. The mutant receptor was
highly expressed in transfected COS-7 cells, and its binding affinity
for the peptide antagonist
[Sar
,Ile
]Ang II was similar to that
of the wild type receptor. Although the structural integrity of the
peptide ligand binding domain was preserved in the Y215F mutant
receptor, its affinity for the native agonist, Ang II, was
significantly reduced. Also, whereas guanosine
5`-3- O-(thio)triphosphate markedly reduced Ang II binding to
the wild type receptor, it had little effect on agonist binding to the
mutant receptor. Agonist-induced internalization of the mutant receptor
was also impaired, and its ability to mediate inositol phosphate
responses to Ang II stimulation was abolished. The concomitant
decreases in receptor internalization and G protein-mediated signaling
of the Y215F mutant receptor indicate that Tyrhas a
critical role in AT
receptor activation. In view of its
conservation among members of the seven transmembrane domain receptor
superfamily, this residue is likely to be of general importance in
signal transduction from G protein-coupled receptors.
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