Receptor Activated Solely By A Synthetic Ligand - Uses

Uses

A recent study using the M1 muscarinic receptor which has rational mutations in the third and fifth intracellular tail has shown it no longer responds to its endogenous ligand acetylcholine but rather responds to the previously inert clozapine-N-oxide (CNO). The study has shown that upon ligand binding, the receptor is differentially phosphorylated when expressed in chinese hamster ovary (CHO) cells (http://www.pa2online.org/abstract/abstract.jsp?abid=30048).

GPCRs are the target for some of the most widely used pharmaceuticals to treat diseases that involve virtually all tissues of the body. New GPCR signaling systems will provide insights into GPCR-induced physiological responses and will allow for new forms of controlling engineered tissues in vivo.