Caloxin 1C2 – Other Categories

Plasma membrane calcium pumps (PMCA) play integral roles in calcium homeostasis and calcium signalling. There are four PMCA isoforms (1-4), their expression and localisation are varied amongst cell types and diseased tissue. Therefore, identification of specific inhibitors of each PMCA is underway to aid understanding of the individual roles the PMCAs play. Use of phage libraries and mutagenesis has allowed rapid screening of possible peptides. A PMCA inhibitor of importance found by screening and mutagenesis is caloxin 1C2. Caloxin 1C2 has been shown to have a 10 found higher affinity for PMCA4 than any other isoforms suggesting it is a suitable selective inhibitor for PMCA4 activity. The allosteric inhibitor is already being used in research to help understand the specific function of PMCA4 in tissues. Since changes in the levels of activity and expression of the PMCA isoforms have been linked to several conditions, such as hypertension and diabetes, clarifying the function of PMCA4 with the use of caloxin1C2 inhibitor could provide new treatments in the future.