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We hypothesize that differential phosphorylation of AL residues of PSKR1 can modulate receptor activity.
Since the acidic JM-C region lies c-terminal to the JM-B region of Ron, we hypothesized that the JM-B region might modulate receptor activity indirectly by affecting localization of the JM-C region.
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Several of the co-activators contain histone acetyltransferase activity, while co-repressor complexes contain histone deacetylase activity, suggesting that localized chromatin remodeling modulates receptor activity [ 14].
Thus, even if Agrp were to be interacting with central melanocortin receptors to modulate energy intake, the disparity of time of onset of effect may be indicative of AgRP-modulating receptor activity in a quite different manner from that of agonist ligands.
For instance, it has been reported that the analogue [ d-Ala]GIP(1 42) possesses greater resistance to enzymatic degradation with no loss of potency at the receptor and greater antidiabetic efficacy, suggesting that the GIP tail region can play a role in modulating receptor activity.
This was done by demonstrating double-labeling of CRH and phosphorylated NR1, an essential subunit of the N-methyl-D-aspartic acid (NMDA) receptor, the phosphorylation of which is known to modulate NMDA receptor activity and can be used as an indicator of NMDA receptor activation.
The broad range of ligands known to modulate ryanodine receptor activity includes a class of heteroaromatic compounds displaying relatively poor efficacy.
A large number of evidences suggest that group-I metabotropic glutamate receptors (mGluR1a, 1b, 1c, 5a, 5b) can modulate NMDA receptor activity.
Additional tropeines, including atropine, modulate glycine receptor activity.
It is becoming clear, having established that signals from cell surface receptors can modulate steroid receptor activity, that nuclear receptors can reciprocate.
It thus appears that any number of cell signalling pathways can modulate nuclear receptor activity either directly or indirectly by altering the activity of co-regulators.
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