Rhodopsin-like G protein-coupled receptor

The **Rhodopsin-like G protein-coupled receptor** family, also known as Class A GPCRs, represents the largest and most diverse group of membrane receptors in humans, encompassing over 700 distinct proteins. These receptors share a seven-transmembrane helix architecture and mediate the cellular response to a vast array of endogenous ligands—including neurotransmitters, hormones, peptides, lipids, nucleotides, and sensory stimuli (such as light and odorants). Class A GPCRs play crucial roles in normal physiology and are involved in the regulation of cardiovascular, neurological, immune, endocrine, and sensory functions. They are highly "druggable," with hundreds of approved drugs and drug candidates targeting one or more receptors within this family for diverse conditions ranging from psychiatric disorders and pain to glaucoma and cancer[1][3][4][5][8][9]. The classification "Family A GPCRs" is generic and encompasses subgroups such as aminergic, peptide, and lipid receptors. Individual members like dopamine, serotonin, histamine, and opioid receptors are major clinical drug targets. Note: "Family A GPCRs" is not the correct name for a single target; rather, it names a large family. For structured information, each specific receptor (e.g., "Dopamine receptor D2") should be referenced individually[1][3][4][7][9].

Other names

Family A GPCRsClass A GPCRsRhodopsin-like family7TM receptors (refers to the seven-transmembrane architecture)

Agonism (stimulates receptor activity); Antagonism (blocks receptor activity); Inverse agonism (reduces basal activity); Allosteric modulation (influences receptor regulation at non-primary binding sites)