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The involvement of the endogenous ERbeta system in the mechanism of action of 3beta-Adiol in these cells is supported by the ability of the compound to activate ERE-mediated transcription, an effect that is dose-dependently counteracted by the presence of the pure antiestrogen ICI 182,780.
In contrast, the agonist phenotype clustering of NRs showed good concordance with the sequence clustering results because cytotoxicity interference was minimal in the agonist (gain of signal) mode assays and binding to the LBD is probably necessary for a compound to activate an NR.
The efficacy of a compound to activate LasR was directly correlated with its ability to maintain the binding interactions observed in the LasRLBD/C12-HSL binary complex.
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In order to find serotonin type 4 receptor (5-HT4R) biased ligands, we analyzed the ability of several compounds to activate the Gs and Gq/11 pathways in COS-7 cells that transiently express wild type 5-HT4R, the 5-HT4R-D100A mutalso(known asso as 5-HT4-RASSL, oRs1s1) or the 5-HT4R-T104A modifieswhich modifies agonist-induced 5-HT4R activation.
We then assessed the ability of the compounds to activate the p53 pathway.
This finding points to the possibility of using pharmacological compounds to activate Notch signaling to prevent satellite cell loss and preserve satellite cell functions in DMD patients.
Prior to treatment, the ability of these compounds to activate SXR was confirmed in transient transfection assays (see Additional file 1: supplementary Figure 2A).
The present study provides the framework of using natural compounds to activate the Nrf2-dependent protective pathway to counteract arsenic-induced damage.
Many other ion channels are studied by using small chemical compounds to activate them, but there were none that were known to act on Piezo proteins.
It has been suggested that Candida species play a role in oral carcinogenesis by triggering nitrosamine compounds to activate specified oncogenes, thereby initiating oral neoplasia [ 51, 53, 54].
To elucidate the different behavior between 3beta-Adiol and the other ERbeta selective ligands on Rv1 cell growth, first of all we tested the ability of the compounds to activate transcription through the binding of ERbeta to ERE sequences.
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