Eglen Richard M, Reisine Terry
Bio-discovery, PerkinElmer Life and Analytical Sciences, Waltham, MA, USA.
Methods Mol Biol. 2009;552:1-13. doi: 10.1007/978-1-60327-317-6_1.
G protein-coupled receptors (GPCRs) are a large family of proteins that represent targets for approximately 40% of all approved drugs. They possess unique structural motifs that allow them to interact with a diverse series of extracellular ligands, as well as intracellular signaling proteins, such as G proteins, RAMPs, arrestins, and indeed other receptors. Extensive efforts are under way to discover new generations of drugs against GPCRs with unique targeted therapeutic uses, including "designer" drugs such as allosteric regulators, inverse agonists, and drugs targeting hetero-oligomeric complexes. This has been facilitated by the development of new screening technologies to identify novel drugs against both known and orphan GPCRs.
G蛋白偶联受体（GPCRs）是一大类蛋白质，约40%的已批准药物都以它们为靶点。它们具有独特的结构基序，使其能够与多种细胞外配体以及细胞内信号蛋白相互作用，如G蛋白、受体活性修饰蛋白（RAMPs）、抑制蛋白，以及其他受体。目前正在进行广泛的研究，以发现针对GPCRs的新一代具有独特靶向治疗用途的药物，包括变构调节剂、反向激动剂等“设计型”药物，以及针对异源寡聚体复合物的药物。新型筛选技术的发展推动了这一进程，这些技术可用于识别针对已知和孤儿GPCRs的新型药物。
