Overview
"G protein-coupled receptors constitute the largest family of transmembrane proteins on the cell membrane, characterized by a core structure of seven transmembrane α-helices that couple with heterotrimeric G proteins through their intracellular C-terminus. The human genome contains nearly 800 genes encoding GPCRs, making them one of the largest protein classes in mammals. When extracellular signaling molecules (such as hormones, neurotransmitters, and photons) bind to GPCRs, the receptors undergo conformational changes that activate associated G proteins, thereby initiating downstream signaling cascades and regulating the production of second messengers including cAMP, IP3, and Ca2+. GPCRs participate in nearly all physiological processes, including sensory perception, neurotransmission, immune responses, cell growth, and differentiation.
Dysfunction of GPCRs is closely associated with various human diseases, including cancer, inflammatory disorders, cardiovascular diseases, metabolic diseases, and neuropsychiatric disorders. Due to their broad pathological associations, GPCRs are among the most important drug target families. Currently, approximately 30%-40% of marketed drugs exert their therapeutic effects by modulating GPCR activity. Recent studies have also revealed that GPCRs are not only localized on the plasma membrane but also on organelle membranes such as mitochondria, where they participate in regulating energy metabolism and cell survival. Recombinant GPCR proteins serve as indispensable tools in drug screening, antibody development, structure-function studies, and target validation."
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