G Protein-Coupled Receptor (GPCR) Expression in Native Cells: "Novel" endoGPCRs as Physiologic Regulators and Therapeutic Targets.

摘要: G protein–coupled receptors (GPCRs), the largest family of signaling in human genome, are also class targets approved drugs. Are optimal GPCRs (in terms efficacy and safety) currently targeted therapeutically? Especially given large number (∼120) orphan (which lack known physiologic agonists), it is likely that previously unrecognized GPCRs, especially receptors, regulate cell function can be therapeutic targets. Knowledge limited regarding diversity identity activated by endogenous ligands native cells express. Here, we review approaches to define GPCR expression tissues results from studies using these approaches. We identify problems with available data suggest future ways validate roles GPCRs. propose a particularly useful approach functionally important potential will focus on show selective increases diseased patients experimental animals.