ABSTRACT

This chapter provides a range of pharmacological agents that target store-operated calcium entry (SOCE) channel inhibitors and are commercially available. Phospholipase C (PLC)-coupled receptors initiate this process through the production of inositol 1,4,5-trisphosphate (IP3). However, this process represents an uncontrolled approach for manipulating SOCE since the magnitude and kinetics of PLC activation may vary and PLC may activate pathways that are unrelated or interfere with SOCE. The external application of sarcoplasmic/endoplasmic reticulum calcium ATPase pump inhibitors to activate SOCE channels, the intracellular Ca2+ store depletion can be achieved by addition of metabolizable or nonmetabolizable analogs of IP3. Ca2+ ionophores have proven useful in transporting Ca2+ ions across a variety of membranes and manipulating intracellular Ca2+ pools in intact cells. ML-9, an inhibitor of myosin light chain kinase, was discovered to inhibit SOCE and thus suggested a possible role for MLCK in the mechanism of SOCE activation.