+Search query
-Structure paper
| Title | Structural basis of oligomerization-modulated activation and autoinhibition of orphan receptor GPR3. |
|---|---|
| Journal, issue, pages | Cell Rep, Vol. 44, Issue 4, Page 115478, Year 2025 |
| Publish date | Mar 28, 2025 |
Authors | Hao Chang / Xiaoting Li / Hongqing Tu / Lijie Wu / Yanan Yu / Junlin Liu / Na Chen / Wei L Shen / Tian Hua / ![]() |
| PubMed Abstract | G protein-coupled receptor 3 (GPR3) is a class A orphan receptor characterized by high constitutive activity in the G signaling pathway. GPR3 has been implicated in Alzheimer's disease and the ...G protein-coupled receptor 3 (GPR3) is a class A orphan receptor characterized by high constitutive activity in the G signaling pathway. GPR3 has been implicated in Alzheimer's disease and the regulation of thermogenesis in human adipocytes, yet the molecular mechanisms underlying its self-activation and potential endogenous modulators remain unclear. In this study, we present cryo-electron microscopy (cryo-EM) structures of GPR3 in different oligomerization states, both in the absence and presence of G protein. Notably, in addition to the monomeric form of GPR3, our findings reveal a functional GPR3 dimer with an extensive dimer interface-a feature rarely observed in class A GPCRs. Moreover, oligomerization appears to be linked to a unique autoinhibition mechanism involving intracellular loops, which may regulate GPR3 signaling. Collectively, these results provide new insights into the oligomerization-modulated activation of orphan GPCRs, advancing our understanding of their signaling properties. |
External links | Cell Rep / PubMed:40158220 |
| Methods | EM (single particle) |
| Resolution | 3.06 - 3.66 Å |
| Structure data | EMDB-63522, PDB-9lyd: EMDB-63523, PDB-9lyc: EMDB-63525, PDB-9lyb: |
| Source |
|
Keywords | STRUCTURAL PROTEIN / GPCR / G protein / cryo-EM / membrane protein |
Movie
Controller
Structure viewers
About Yorodumi Papers



Authors
External links





homo sapiens (human)
Keywords