期刊
TRENDS IN PHARMACOLOGICAL SCIENCES
卷 39, 期 6, 页码 547-559出版社
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tips.2018.03.002
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资金
- NIAID NIH HHS [R01 AI118985, R21 AI122211] Funding Source: Medline
- NIGMS NIH HHS [R01 GM117424] Funding Source: Medline
Recent crystal structures of multiple G protein-coupled receptors (GPCRs) have revealed a highly conserved intracellular pocket that can be used to modulate these receptors from the inside. This novel intracellular site partially overlaps with the G protein and beta-arrestin binding site, providing a new manner of pharmacological intervention. Here we provide an update of the architecture and function of the intracellular region of GPCRs, until now portrayed as the signaling domain. We review the available evidence on the presence of intracellular binding sites among chemokine receptors and other class A GPCRs, as well as different strategies to target it, including small molecules, pepducins, and nanobodies. Finally, the potential advantages of intracellular (allosteric) ligands over orthosteric ligands are also discussed.
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