Knowledge of the molecular architecture and the structural and functional diversity of the members of the G protein-coupled receptor superfamily is increasing at an exponential rate. An appreciation of the conservation of key structural components of these receptors, and the corresponding relationships at the DNA sequence level, has greatly facilitated the isolation of new members of this superfamily, including those encoding receptors which recognize as yet unidentified ligands. The molecular cloning of DNA sequences encoding these receptors has also facilitated the biosynthesis of large amounts of purified receptor for structural studies, as well as providing the basic templates for rapid analysis of structural determinants through in vitro mutagenesis and expression in heterologous systems. As approximately 80% of bioactive molecules, especially hormones and neurotransmitters, act through interaction with G protein-coupled receptors, it is not surprising that this rapidly increasing knowledge of the detailed structure and function of this receptor class is providing growing insight into the molecular pathology of a wide range of disorders, as well as providing important new tools for the development of novel receptor subtype specific therapeutic agents.
KeywordsReceptor Subtype Color Blindness Small Molecule Ligand Basic Template Directed Mutagenesis Study
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