The most widely used and safest medicines today are ligands to GPCRs. The first generation of antihypertensives p-blocked the p-adrenergic receptor, the later generations include blockers of the angiotensin receptor, both GPCRs. Antihistamines to fight hay fever and allergy, antipsychotics, and some antidepressant drugs are also ligands to GPCRs. Furthermore, the analgesic actions of morphine and its analogs are exerted at GPCRs and lately antiviral agents blocking HIV entry into cells are also targeting GPCRs. The pharmaceutical industry at every level — biology, chemistry and toxicology — became so familiar with medicines that target GPCRs for chronic drug therapy that this class of proteins is by far the most favored class of new drug targets. There are still orphan GPCRs whose endogenous ligands and function is not known, these GPCRs hold additional promises for drug therapy together with the very large group of GPCRs that bind neuropeptides and peptide hormones. We are going to see rapid exploration of these GPCRs as drug targets in the treatment of diabetes, obesity and major depression. Hence all new knowledge on expression structure and function of GPCRs is of great value for all who work on developing new medicines.

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