Contribution of heteromerization to G protein-coupled receptor function.
G protein-coupled receptors (GPCRs) are a remarkably multifaceted family of transmembrane proteins that exert a variety of physiological effects. Although family A GPCRs are able to operate as monomers, there is increasing evidence that heteromerization represents a fundamental aspect of receptor function, trafficking and pharmacology. Most recently, it has been suggested that GPCR heteromers may play a crucial role as new molecular targets of heteromer-selective and bivalent ligands. The current review summarizes key recent developments in these topics.
Department of Physiology and Biophysics, Virginia Commonwealth University School of Medicine, Richmond, VA 23298, United States.
Supriya A
SA
Gaitonde
Department of Physiology and Biophysics, Virginia Commonwealth University School of Medicine, Richmond, VA 23298, United States. Electronic address: jgmaeso@vcu.edu.
Javier
J
González-Maeso
D000818:Animals; D015195:Drug Design; D006801:Humans; D008024:Ligands; D058990:Molecular Targeted Therapy; D055503:Protein Multimerization; D021381:Protein Transport; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*
D008024:Ligands; D043562:Receptors, G-Protein-Coupled