The role of GPR133 in glioblastoma biology

We recently described that GPR133, an orphan member of the adhesion family of G protein-coupled receptors (GPCR), is necessary for glioblastoma growth. GPR133 is expressed in all glioblastomas, regardless of molecular subtype, but is absent from normal brain tissue. This expression profile, along with the fact GPR133 is expected to be “druggable” by virtue of being a GPCR, suggest a favorable therapeutic profile. We are currently elucidating basic mechanisms of action of GPR133, but also developing it translationally as a novel therapeutic target, using high-through screening for inhibitor discovery.