The subcellular signaling landscape of receptors
G protein-coupled receptors (GPCRs) form the largest receptor family in humans. GPCRs mediate the effects of diverse natural ligands, such as hormones and neurotransmitters, and many therapeutic drugs, including pain killers and beta blockers. While GPCRs were classically described as cell surface receptors, it is clear today that GPCR signaling also occurs in specific cellular compartments inside cells, the organelles, which can lead to distinct physiological outcomes.
In two recent reviews the Stoeber team together with international colleagues discuss the current knowledge about how the subcellular localization of GPCRs is established, and how signaling at distinct organelles can be measured with state-of-the-art techniques.
A deeper mechanistic understanding of subcellular GPCR function holds significant promise for advancing drug discovery. Such insights can lead to the development of more precise drugs with improved action and fewer side effects, ultimately opening new avenues for treating a wide range of diseases.