IP3 Receptor Inhibitors

Inositol 1,4,5-trisphosphate (IP₃) receptors are a form of ligand-gated ion channels that are activated by cytosolic Ca²⁺ and IP₃. They are localized to intracellular membranes, such as the endoplasmic reticulum, and mediate the mobilization of intracellular Ca²⁺ stores.

IP₃ receptors play an important role in intracellular Ca²⁺ signaling in a variety of cell types. There are three IP₃ receptor subtypes; IP₃R1, IP₃R2 and IP₃R3, which exist as homo- and heterotetramers. All subtypes are closely associated with calmodulin and FK506-binding protein and are modulated through phosphorylation by PKA, PKC, PKG and CaMKII.