PAR-2 Activators

PAR-2 Activators are a chemical class that can either directly or indirectly act on the PAR-2 protein. Direct activators, such as trypsin and thrombin, cleave the N-terminus of PAR-2, producing a tethered ligand that activates the protein. This class of chemicals can activate PAR-2 without the need for external factors, making them primary activators of the protein. Serine proteases, which include trypsin and thrombin, feature prominently in this category. Indirect activators, on the other hand, influence the cellular processes or signaling pathways that PAR-2 is involved in. These chemicals do not interact with the protein directly, but their action can lead to the protein's activation. Chlorogenic acid and forskolin, for example, increase cAMP levels, which can activate PAR-2. Similarly, histamine, bradykinin, and prostaglandin E2 act by increasing intracellular calcium, a secondary messenger in the PAR-2 pathway. Dithiothreitol can alter the protein conformation of PAR-2 and indirectly activate its pathway. PIP2 acts as a substrate for producing secondary messengers in the PAR-2 pathway, and calcium ions serve as a secondary messenger themselves.