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| Title | Molecular insights into ligand recognition and activation of chemokine receptors CCR2 and CCR3. |
|---|---|
| Journal, issue, pages | Cell Discov, Vol. 8, Issue 1, Page 44, Year 2022 |
| Publish date | May 15, 2022 |
 Authors | Zhehua Shao / Yangxia Tan / Qingya Shen / Li Hou / Bingpeng Yao / Jiao Qin / Peiyu Xu / Chunyou Mao / Li-Nan Chen / Huibing Zhang / Dan-Dan Shen / Chao Zhang / Weijie Li / Xufei Du / Fei Li / Zhi-Hua Chen / Yi Jiang / H Eric Xu / Songmin Ying / Honglei Ma / Yan Zhang / Huahao Shen /  |
| PubMed Abstract | Chemokine receptors are a family of G-protein-coupled receptors with key roles in leukocyte migration and inflammatory responses. Here, we present cryo-electron microscopy structures of two human CC ...Chemokine receptors are a family of G-protein-coupled receptors with key roles in leukocyte migration and inflammatory responses. Here, we present cryo-electron microscopy structures of two human CC chemokine receptor-G-protein complexes: CCR2 bound to its endogenous ligand CCL2, and CCR3 in the apo state. The structure of the CCL2-CCR2-G-protein complex reveals that CCL2 inserts deeply into the extracellular half of the transmembrane domain, and forms substantial interactions with the receptor through the most N-terminal glutamine. Extensive hydrophobic and polar interactions are present between both two chemokine receptors and the Gα-protein, contributing to the constitutive activity of these receptors. Notably, complemented with functional experiments, the interactions around intracellular loop 2 of the receptors are found to be conserved and play a more critical role in G-protein activation than those around intracellular loop 3. Together, our findings provide structural insights into chemokine recognition and receptor activation, shedding lights on drug design targeting chemokine receptors. |
 External links | Cell Discov / PubMed:35570218 / PubMed Central |
| Methods | EM (single particle) |
| Resolution | 2.9 - 3.1 Å |
| Structure data | EMDB-33085, PDB-7x9y: EMDB-33086, PDB-7xa3: |
| Source |
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 Keywords |  MEMBRANE PROTEIN / GPCR / CCR3 / Chemokine Receptor / MEMBRNE PROTEIN / CCR2 |
