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Upon binding to an agonist, the PPAR-GAL4 fusion protein activates a luciferase reporter [20].
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The nature of the ligand-hPPARγ-LBD interaction can also be inferred: an agonist ligand enhances binding to a coactivator and decreases binding to a corepressor; an inverse agonist causes the opposite effect; and a neutral antagonist decreases binding for both coactivators and corepressors.
The classic paradigm of G protein-coupled receptor (GPCR) activation was based on the understanding that agonist binding to a receptor induces or stabilizes a conformational change to an 'active' conformation.
These two classes of compounds act through the binding to a NR and the activation (agonist ligands) or the inhibition (antagonist ligands) of its activity.
Given the known effects of agonist binding to a PPAR one could speculate whether the dominant negative effect of the PPARδ LBD is due to RXR or transcriptional co-activator squelching.
Cyclic AMP production is reduced during agonist binding to a low affinity state.
It is also notable that the pIC50 values obtained for XAC from inhibition of the number of τD3 particles and the pEC50 for XAC-induced increase in the number of τD2 particles (both ∼6.0) are consistent with the value obtained previously for the IC50 for XAC binding to a fluorescent agonist occupied A3AR (30).
After binding to its agonists, a conformational change in AhR releases itself from the complex and thus enables its translocation to the nucleus.
Although these interesting findings do not provide definitive evidence for a causal association between VDR gene and migraine, the VDR has a broad expression in the central nervous system, where the binding to its agonists produces an important (pleiotropic) anti-inflammatory effect [ 28].
First, EGCG could potentially bind to RIG-I and prevent its binding to the RNA agonist.
The binding of an agonist to a GPCR leads to structural changes within the TM regions allowing activation of a G-protein, receptor internalization and desensitization.
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