G protein–coupled receptor deorphanizations
O Civelli, RK Reinscheid, Y Zhang… - Annual review of …, 2013 - annualreviews.org
Annual review of pharmacology and toxicology, 2013•annualreviews.org
G protein–coupled receptors (GPCRs) are major regulators of intercellular interactions. They
initiate these actions by being activated by a wide variety of natural ligands. Historically,
ligands were discovered first, but the advent of molecular biology reversed this trend. Most
GPCRs are identified on the basis of their DNA sequences and thus are initially unmatched
to known natural ligands. They are termed orphan GPCRs. Discovering their ligands—
ie,“deorphanizing” the GPCRs—gave birth to the field of reverse pharmacology. This review …
initiate these actions by being activated by a wide variety of natural ligands. Historically,
ligands were discovered first, but the advent of molecular biology reversed this trend. Most
GPCRs are identified on the basis of their DNA sequences and thus are initially unmatched
to known natural ligands. They are termed orphan GPCRs. Discovering their ligands—
ie,“deorphanizing” the GPCRs—gave birth to the field of reverse pharmacology. This review …
G protein–coupled receptors (GPCRs) are major regulators of intercellular interactions. They initiate these actions by being activated by a wide variety of natural ligands. Historically, ligands were discovered first, but the advent of molecular biology reversed this trend. Most GPCRs are identified on the basis of their DNA sequences and thus are initially unmatched to known natural ligands. They are termed orphan GPCRs. Discovering their ligands—i.e., “deorphanizing” the GPCRs—gave birth to the field of reverse pharmacology. This review discusses the present status of GPCR deorphanization, presents a few examples of successes and surprises, and highlights difficulties encountered in these efforts.
Annual Reviews