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Variable Dependence of Signaling Output on Agonist Occupancy of Ste2p, a G Protein-coupled Receptor in Yeast
| Content Provider | Scilit |
|---|---|
| Author | Sridharan, Rajashri Connelly, Sara M. Naider, Fred Dumont, Mark E. |
| Copyright Year | 2016 |
| Description | Journal: Journal of Biological Chemistry We report here on the relationship between ligand binding and signaling responses in the yeast pheromone response pathway, a well characterized G protein-coupled receptor system. Responses to agonist (α-factor) by cells expressing widely varying numbers of receptors depend primarily on fractional occupancy, not the absolute number of agonist-bound receptors. Furthermore, the concentration of competitive antagonist required to inhibit α-factor-dependent signaling is more than 10-fold higher than predicted based on the known ligand affinities. Thus, responses to a particular number of agonist-bound receptors can vary greatly, depending on whether there are unoccupied or antagonist-bound receptors present on the same cell surface. This behavior does not appear to be due to pre-coupling of receptors to G protein or to the Sst2p regulator of G protein signaling. The results are consistent with a signaling response that is determined by the integration of positive signals from agonist-occupied receptors and inhibitory signals from unoccupied receptors, where the inhibitory signals can be diminished by antagonist binding. |
| Related Links | http://www.jbc.org/content/291/46/24261.full.pdf https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5104947/pdf http://www.jbc.org/article/S0021925820346913/pdf |
| Ending Page | 24279 |
| Page Count | 19 |
| Starting Page | 24261 |
| ISSN | 00219258 |
| e-ISSN | 1083351X |
| DOI | 10.1074/jbc.m116.733006 |
| Journal | Journal of Biological Chemistry |
| Issue Number | 46 |
| Volume Number | 291 |
| Language | English |
| Publisher | Elsevier BV |
| Publisher Date | 2016-11-01 |
| Access Restriction | Open |
| Subject Keyword | Journal: Journal of Biological Chemistry G Protein G Protein-coupled Receptor (gpcr) Regulator of G Protein Signaling (rgs) Signal Transduction |
| Content Type | Text |
| Resource Type | Article |
| Subject | Cell Biology Biochemistry Molecular Biology |
