Mutations in G proteins and G protein-coupled receptors in endocrine disease.

Mutations in G proteins and G protein-coupled receptors in endocrine disease.

G Proteins couple receptors for diverse extracellular signals to effecters such as enzymes and ion channels. The majority of polypeptide hormones, all monoamine neurotransmitters, PGs, and even extracellular Ca’+ signal their target cells through G protein-coupled receptors (GPCR). In the past few years, mutations in G proteins and GPCR have been identified as the causes of several endocrine di...

G Protein-coupled receptors

G protein-coupled receptors and heterotrimeric G proteins can diffuse laterally in the plasma membrane such that one receptor can catalyze the activation (GDP/GTP exchange) of multiple G proteins. In some cases, these processes are fast enough to support molecular signal amplification, where a single receptor maintains the activation of multiple G proteins at steady-state. Amplification in cell...

G-protein-coupled receptors.

G-Protein-coupled receptors mediate many of the hypnotic and analgesic actions of the drugs employed in anesthesia. Notably, opioid agonists represent the most successful and efficacious class of analgesic agents employed over the last century. Also, major clinical advances have been made by the study of alpha(2) adrenoceptor agonists, which possess both hypnotic and analgesic qualities that ar...

G-protein Coupled Receptor Dimerization

A growing body of evidence suggests that GPCRs exist and function as dimers or higher oligomers. The evidence for GPCR dimerization comes from biochemical, biophysical and functional studies. In addition, researchers have shown the occurrence of heterodimerization between different members of the GPCR family. Two receptors can interact with each other to make a dimer through their extracellular...

Modelling G protein-coupled receptors