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- Title
Cryo-EM advances in GPCR structure determination.
- Authors
Shihoya, Wataru; Iwama, Aika; Sano, Fumiya K; Nureki, Osamu
- Abstract
G-protein-coupled receptors (GPCRs) constitute a prominent superfamily in humans and are categorized into six classes (A–F) that play indispensable roles in cellular communication and therapeutics. Nonetheless, their structural comprehension has been limited by challenges in high-resolution data acquisition. This review highlights the transformative impact of cryogenic electron microscopy (cryo-EM) on the structural determinations of GPCR–G-protein complexes. Specific technologies, such as nanobodies and mini-G-proteins, stabilize complexes and facilitate structural determination. We discuss the structural alterations upon receptor activation in different GPCR classes, revealing their diverse mechanisms. This review highlights the robust foundation for comprehending GPCR function and pave the way for future breakthroughs in drug discovery and therapeutic targeting.
- Subjects
DRUG discovery; IMMUNOGLOBULINS; ACQUISITION of data; ELECTRON microscopy; THERAPEUTICS
- Publication
Journal of Biochemistry, 2024, Vol 176, Issue 1, p1
- ISSN
0021-924X
- Publication type
Article
- DOI
10.1093/jb/mvae029