The CREST Activators are a group of chemicals that enhance the functional activity of CREST primarily through influencing the cAMP-CREB signaling pathway, a biological process directly involving CREST. These activators, which include phosphodiesterase inhibitors such as Forskolin, IBMX, Rolipram, Zaprinast, Vinpocetine, Milrinone, Anagrelide, Dipyridamole, Cilostazol, and Theophylline, increase cAMP levels. Elevated cAMP levels activate the CREB signaling pathway, in which CREST acts as a co-activator. Thus, by initiating the activation of CREB, these compounds indirectly enhance the co-activator function of CREST.
Furthermore, CREST Activators include protein kinase A inhibitors like H-89 and KT5720. Protein kinase A is responsible for phosphorylating and activating CREB. However, when protein kinase A is inhibited by these compounds, it indirectly enhances the demand for CREST's co-activator function. This is because in the absence of phosphorylated (and thus activated) CREB, more CREST is required to achieve the same level of CREB activation. Therefore, through these specific mechanisms, the compounds listed above can enhance the functional activity of CREST.
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