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- W3010049907 endingPage "183265" @default.
- W3010049907 startingPage "183265" @default.
- W3010049907 abstract "G protein-coupled receptors (GPCRs) constitute the largest superfamily of membrane proteins in higher eukaryotes, and facilitate information transfer from the extracellular environment to the cellular interior upon activation by ligands. Their role in diverse signaling processes makes them an attractive choice as drug targets. GPCRs are coupled to heterotrimeric G-proteins which represent an important interface through which signal transduction occurs across the plasma membrane upon activation by ligands. To obtain further insight into the molecular details of interaction of G-proteins with GPCRs, in this work, we explored the selectivity of binding of specific agonists and antagonists to the serotonin1A receptor under conditions of progressive G-protein inactivation. The serotonin1A receptor is an important neurotransmitter receptor belonging to the GPCR family and is a popular drug target. By use of a number of agents to inactivate G-proteins, we show here that the serotonin1A receptor displays differential discrimination between agonist and antagonist binding. Our results show a reduction in binding sites of the receptor upon treatment with G-protein inactivating agents. In addition, G-protein coupling efficiency was enhanced when G-proteins were inactivated using urea and alkaline pH. We envision that our results could be useful in achieving multiple signaling states of the receptor by fine tuning the conditions of G-protein inactivation and in structural biology of GPCRs bound to specific ligands." @default.
- W3010049907 created "2020-03-13" @default.
- W3010049907 creator A5063835467 @default.
- W3010049907 creator A5064761749 @default.
- W3010049907 creator A5083143380 @default.
- W3010049907 date "2020-06-01" @default.
- W3010049907 modified "2023-09-24" @default.
- W3010049907 title "Selectivity in agonist and antagonist binding to Serotonin1A receptors via G-protein coupling" @default.
- W3010049907 cites W1135792216 @default.
- W3010049907 cites W1170028849 @default.
- W3010049907 cites W1499695147 @default.
- W3010049907 cites W1515847803 @default.
- W3010049907 cites W1518637829 @default.
- W3010049907 cites W1524415596 @default.
- W3010049907 cites W1568667145 @default.
- W3010049907 cites W1570378576 @default.
- W3010049907 cites W1603274157 @default.
- W3010049907 cites W1604388739 @default.
- W3010049907 cites W1615152444 @default.
- W3010049907 cites W1934687632 @default.
- W3010049907 cites W1965835906 @default.
- W3010049907 cites W1971469548 @default.
- W3010049907 cites W1974738889 @default.
- W3010049907 cites W1976548894 @default.
- W3010049907 cites W1978310995 @default.
- W3010049907 cites W1980596504 @default.
- W3010049907 cites W1981194125 @default.
- W3010049907 cites W1981818755 @default.
- W3010049907 cites W1987970138 @default.
- W3010049907 cites W1988097700 @default.
- W3010049907 cites W1991276907 @default.
- W3010049907 cites W1992963529 @default.
- W3010049907 cites W1998317438 @default.
- W3010049907 cites W2003440473 @default.
- W3010049907 cites W2010122297 @default.
- W3010049907 cites W2011325946 @default.
- W3010049907 cites W2011504421 @default.
- W3010049907 cites W2014826286 @default.
- W3010049907 cites W2015414687 @default.
- W3010049907 cites W2024790914 @default.
- W3010049907 cites W2025513890 @default.
- W3010049907 cites W2047567287 @default.
- W3010049907 cites W2056458954 @default.
- W3010049907 cites W2060553492 @default.
- W3010049907 cites W2064232716 @default.
- W3010049907 cites W2064993556 @default.
- W3010049907 cites W2065073659 @default.
- W3010049907 cites W2065095084 @default.
- W3010049907 cites W2065648777 @default.
- W3010049907 cites W2065765661 @default.
- W3010049907 cites W2066495105 @default.
- W3010049907 cites W2073438769 @default.
- W3010049907 cites W2077116772 @default.
- W3010049907 cites W2080231167 @default.
- W3010049907 cites W2088667287 @default.
- W3010049907 cites W2089880141 @default.
- W3010049907 cites W2091111816 @default.
- W3010049907 cites W2094622306 @default.
- W3010049907 cites W2094770888 @default.
- W3010049907 cites W2103912693 @default.
- W3010049907 cites W2104477830 @default.
- W3010049907 cites W2107345283 @default.
- W3010049907 cites W2114565306 @default.
- W3010049907 cites W2139945041 @default.
- W3010049907 cites W2140820106 @default.
- W3010049907 cites W2141036148 @default.
- W3010049907 cites W2144904732 @default.
- W3010049907 cites W2150601291 @default.
- W3010049907 cites W2151232434 @default.
- W3010049907 cites W2154550811 @default.
- W3010049907 cites W2154756937 @default.
- W3010049907 cites W2160574926 @default.
- W3010049907 cites W2167857702 @default.
- W3010049907 cites W2171912603 @default.
- W3010049907 cites W2175262146 @default.
- W3010049907 cites W2188537475 @default.
- W3010049907 cites W2253476058 @default.
- W3010049907 cites W2499343687 @default.
- W3010049907 cites W2505532605 @default.
- W3010049907 cites W2509928882 @default.
- W3010049907 cites W253029884 @default.
- W3010049907 cites W259764148 @default.
- W3010049907 cites W2607506319 @default.
- W3010049907 cites W2623292471 @default.
- W3010049907 cites W2741191097 @default.
- W3010049907 cites W2765153686 @default.
- W3010049907 cites W2809303314 @default.
- W3010049907 cites W2809662941 @default.
- W3010049907 cites W2907496293 @default.
- W3010049907 cites W2908941063 @default.
- W3010049907 cites W2946259785 @default.
- W3010049907 cites W2971093965 @default.
- W3010049907 cites W2996977664 @default.
- W3010049907 cites W3100271906 @default.
- W3010049907 cites W4211248987 @default.
- W3010049907 cites W4245806881 @default.
- W3010049907 doi "https://doi.org/10.1016/j.bbamem.2020.183265" @default.
- W3010049907 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32156647" @default.