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Palmitoylation of the human β2-adrenergic receptor
Open accessAbstract
We report that a cysteine residue in the human beta 2-adrenergic receptor (beta 2AR) is covalently modified by thioesterification with palmitic acid. By site-directed mutagenesis of the receptor, we have identified Cys341 in the carboxyl tail of the protein as the most likely site of palmitoylation. Mutation of Cys341 to glycine results in a nonpalmitoylated form of the receptor that exhibits a drastically reduced ability to mediate isoproterenol stimulation of adenylyl cyclase. The functional impairment of this mutated beta 2AR is also reflected in a markedly reduced ability to form a guanyl nucleotide-sensitive high affinity state for agonists, characteristic of wild-type receptor. These results indicate that post-translational modification by palmitate of beta 2AR may play a crucial role in the normal coupling of the receptor to the adenylyl cyclase signal transduction system.
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Bradford, M. M. (1976) · Analytical Biochemistry · doi:10.1016/0003-2697(76)90527-3 · Cited by 255,302
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LAEMMLI, U. K. (1970) · Nature · doi:10.1038/227680a0 · Cited by 249,961
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MISSALE, C., NASH, S. R., ROBINSON, S. W., JABER, M., & CARON, M. G. (1998) · Physiological Reviews · doi:10.1152/physrev.1998.78.1.189 · Cited by 3,633
Self-citationHow receptors talk to trimeric G proteins
Bourne, H. R. (1997) · Current Opinion in Cell Biology · doi:10.1016/s0955-0674(97)80054-3 · Cited by 567
Cloning of the cDNA and gene for a human D2 dopamine receptor.
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Sunahara, R. K., Niznik, H. B., Weiner, D. M., Stormann, T. M., Brann, M. R., Kennedy, J. L., Gelernter, J. E., Rozmahel, R., Yang, Y., Israel, Y., et al. (1990) · Nature · doi:10.1038/347080a0 · Cited by 462
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Metadata
- Authors
- O'Dowd, B. F., Hnatowich, M., Caron, M. G., Lefkowitz, R. J., & Bouvier, M.
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 1989-05
- Volume
- 264
- Issue
- 13
- Pages
- 7564-7569
- ISSN
- 0021-9258 (ISSN-L)
- OpenAlex
- W1925289812
- Cited by
- 598
- References
- 2
- FWCI
- 15.62
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- O'Dowd, B. F., Hnatowich, M., Caron, M. G., Lefkowitz, R. J., & Bouvier, M. (1989). Palmitoylation of the human β2-adrenergic receptor. Journal of Biological Chemistry. https://doi.org/10.1016/s0021-9258(18)83271-9
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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