PEF Activators

PEF Activators encompass a range of chemicals that can influence the activity of PEF, also known as PEF1, a protein intricately linked with calcium-binding functions. Given its association with calcium, a significant fraction of chemicals classified as PEF Activators focuses on modulating intracellular calcium levels, subsequently influencing the activity and function of PEF1.

Calcium ions, central to a myriad of cellular processes, play a pivotal role in the context of PEF activators. Agents like thapsigargin elevate cytosolic calcium levels by inhibiting the sarco/endoplasmic reticulum Ca^2+-ATPase (SERCA), indirectly influencing PEF1's activity. Similarly, ionomycin, a calcium ionophore, increases intracellular calcium concentrations, thereby affecting PEF1. Ryanodine, by modulating calcium release from the sarcoplasmic reticulum, and BAPTA-AM, a cell-permeable calcium chelator, are other notable agents that can alter the cellular calcium landscape, subsequently impacting PEF1's function. Furthermore, chemicals like caffeine, which modify calcium release from internal stores, and 2-Aminoethoxydiphenyl borate (2-APB), which alters intracellular calcium levels, can also influence PEF1. On the other hand, calcium channel blockers like nifedipine and verapamil modulate calcium entry into cells, indirectly affecting PEF1's calcium-binding function. EGTA, a potent calcium chelator, and cyclopiazonic acid, a SERCA inhibitor, represent other agents that through their actions on calcium homeostasis can indirectly modulate PEF1.