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TitleStructural insights into the allosteric inhibition of P2X4 receptors.
Journal, issue, pagesNat Commun, Vol. 14, Issue 1, Page 6437, Year 2023
Publish dateOct 13, 2023
AuthorsCheng Shen / Yuqing Zhang / Wenwen Cui / Yimeng Zhao / Danqi Sheng / Xinyu Teng / Miaoqing Shao / Muneyoshi Ichikawa / Jin Wang / Motoyuki Hattori /
PubMed AbstractP2X receptors are ATP-activated cation channels, and the P2X4 subtype plays important roles in the immune system and the central nervous system, particularly in neuropathic pain. Therefore, P2X4 ...P2X receptors are ATP-activated cation channels, and the P2X4 subtype plays important roles in the immune system and the central nervous system, particularly in neuropathic pain. Therefore, P2X4 receptors are of increasing interest as potential drug targets. Here, we report the cryo-EM structures of the zebrafish P2X4 receptor in complex with two P2X4 subtype-specific antagonists, BX430 and BAY-1797. Both antagonists bind to the same allosteric site located at the subunit interface at the top of the extracellular domain. Structure-based mutational analysis by electrophysiology identified the important residues for the allosteric inhibition of both zebrafish and human P2X4 receptors. Structural comparison revealed the ligand-dependent structural rearrangement of the binding pocket to stabilize the binding of allosteric modulators, which in turn would prevent the structural changes of the extracellular domain associated with channel activation. Furthermore, comparison with the previously reported P2X structures of other subtypes provided mechanistic insights into subtype-specific allosteric inhibition.
External linksNat Commun / PubMed:37833294 / PubMed Central
MethodsEM (single particle)
Resolution3.23 - 3.43 Å
Structure data

36668

8jv5

EMDB-36668, PDB-8jv5:
Cryo-EM structure of the zebrafish P2X4 receptor in complex with BX430
Method: EM (single particle) / Resolution: 3.23 Å

36669

8jv6

EMDB-36669, PDB-8jv6:
Cryo-EM structure of the zebrafish P2X4 receptor in complex with BAY-1797
Method: EM (single particle) / Resolution: 3.43 Å

Chemicals

ChemComp-P73:
1-[2,6-bis(bromanyl)-4-propan-2-yl-phenyl]-3-pyridin-3-yl-urea

ChemComp-NAG:
2-acetamido-2-deoxy-beta-D-glucopyranose

ChemComp-P6E:
N-[4-(3-chloranylphenoxy)-3-sulfamoyl-phenyl]-2-phenyl-ethanamide

Source
  • danio rerio (zebrafish)
KeywordsTRANSPORT PROTEIN / ATP / allosteric modulator / channel

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