Sentence examples for binding of the agonist from inspiring English sources
Moreover, binding of the agonist PET ligand [11C]AF150(S) appears to be sensitive to changes in extracellular ACh levels.
Some allosteric antagonists are known to disrupt agonist signaling without necessarily disrupting the binding of the agonist to the receptor.
In a similar vein, binding of the agonist [I]melatonin to the MT1 receptor was eliminated when the orphan GPCR GPR50 was co-expressed along with the melatonin MT1 receptor [ 27].
The binding of the agonist to the receptor in the cytoplasm and its migration to the nucleus could explain the increase of the MC4R protein in the nuclear fraction during APR.
The activation of GABAAR (as of any other ligand-gated channel) consists of at least two kinetically distinct steps including binding of the agonist to the receptor and the conformational transitions of bound receptor.
Binding of the agonist to all three receptors was sensitive to sodium ions, with a loss of 50% of specific binding seen at approximately 25 mM NaCl.
In most of the studied GPCRs, binding of the sensed ligand molecule (agonist) causes a conformational change in the helical bundle that promotes an interaction with a GTP/GDP binding protein, which then triggers the intracellular signal cascade [ 4, 5].
Once established, binding of Rh-ET-1 persisted after washout of free Rh-ET-1 and was not reversed by BQ123 (1 µM; Fig. 6F) indicating quasi-irreversible receptor-binding of the agonist.
As illustrated in Figure 7 B, the binding mode of the agonist C4-HSL is similar to that of the natural ligand as it retains most of the binding interactions of the homoserine lactone and amide moieties of C12-HSL, including four intermolecular hydrogen bonds involving Tyr-56, Trp-60, Asp-73 and Ser-129, CH−Π interactions with Trp-88 and a lipophilic contact with Ala-105.
These results lead to two conclusions: (1) occupation at each primary face of an α subunit is needed to activate the channel and (2) the complementary face of the adjacent subunit dictates the binding ability of the agonist.
Thus, the binding of the pure agonist Dex induces a GR conformation in which the position of H12 allows the interaction with coactivators such as the transcriptional intermediary factor 2 (TIF2) [19], [19].
