CONSTITUTIVELY ACTIVE G-PROTEIN-COUPLED RECEPTORS - POTENTIAL MECHANISMS OF RECEPTOR ACTIVATION

Mutations of G protein-coupled receptors can increase their constituti ve (agonist-independent) activity. Some of these mutations have been a rtificially introduced by site-directed mutagenesis, others occur spon taneously in human diseases. The analysis of the constitutively active G protein-coupled receptors has provided important informations about the molecular mechanisms underlying receptor activation and drug acti on.