CELSR3 Activators

CELSR3 activators include a range of chemical compounds that facilitate the planar cell polarity (PCP) pathway, where CELSR3 is directly involved. Forskolin, Rolipram, Epinephrine, Caffeine, Dopamine, Histamine, Serotonin, Norepinephrine, IBMX, Isoproterenol, Salbutamol, and Terbutaline all enhance the levels of cAMP, a second messenger that activates protein kinase A (PKA). PKA then phosphorylates Dishevelled (Dsh/Dvl) proteins, a key process in the PCP pathway. By enhancing the phosphorylation of Dsh/Dvl proteins, these chemicals indirectly enhance the functional activity of CELSR3, a key player in this pathway.

Most of these compounds, such as Forskolin andRolipram, act by activating adenylyl cyclase or inhibiting phosphodiesterase, enzymes that respectively synthesize and degrade cAMP. This results in a net increase in cAMP levels, which leads to the activation of PKA. Other compounds, like Epinephrine, Dopamine, Histamine, Serotonin, Norepinephrine, Isoproterenol, Salbutamol, and Terbutaline, are neurotransmitters or drugs that bind to specific receptors, leading to the activation of adenylyl cyclase through G-protein coupled receptor signaling. The resultant increase in cAMP levels promotes PKA activity. The activated PKA phosphorylates Dsh/Dvl proteins, a crucial step in the PCP pathway, leading to the enhanced functional activity of CELSR3. These specific biochemical mechanisms underline the indirect activation of CELSR3 by these chemical compounds.