Modulating Ca2+ release by the IP3R/Ca2+ channel as a potential therapeutic treatment for neurological diseases.
Recent research into neurodegenerative disorders found that their pathogeneses have a link to the inositol 1,4,5-trisphosphate receptors (IP3R). This is encouraging, because despite extensive efforts, researchers have not fully understood the pathophysiologies of those disorders, and have yet to find the cure. The IP3R provides a possible point of convergence that new therapeutic drugs can target. This review highlights patents that manipulate activities of the IP3R. They generally involve the use of peptides designed from the amino acid sequences of IP3R-binding proteins, and of buffers that limit the availability of its ligand, IP3. Additionally, one of them details the use of a chromophore-conjugated small synthetic molecule to directly inhibit the IP3R in a highly spatiotemporally specific manner. Although many of them have only been tested in vitro or are in the early stages of in vivo application, more research-effective therapies for neurodegenerative diseases can hopefully be developed.
Laboratory for Neuronal Growth Mechanisms, RIKEN Brain Science Institute, Wako, Saitama, Japan. chanccm@gmail.com.
Carmen C M
CC
Chan
D000818:Animals; D002118:Calcium / Q000378:metabolism*; D015220:Calcium Channels / Q000187:drug effects*; D020013:Calcium Signaling / Q000187:drug effects; D006801:Humans; D053496:Inositol 1,4,5-Trisphosphate Receptors / Q000037:antagonists & inhibitors / Q000096:biosynthesis / Q000187:drug effects* / Q000235:genetics / Q000502:physiology; D009422:Nervous System Diseases / Q000188:drug therapy*; D011485:Protein Binding; D013347:Subcellular Fractions / Q000378:metabolism
D015220:Calcium Channels; D053496:Inositol 1,4,5-Trisphosphate Receptors; D002118:Calcium