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Structure paper

TitleHuman P2X4 receptor gating is modulated by a stable cytoplasmic cap and a unique allosteric pocket.
Journal, issue, pagesSci Adv, Vol. 11, Issue 3, Page eadr3315, Year 2025
Publish dateJan 17, 2025
AuthorsHaoyuan Shi / Ismayn A Ditter / Adam C Oken / Steven E Mansoor /
PubMed AbstractP2X receptors (P2XRs) are adenosine 5'-triphosphate (ATP)-gated ion channels comprising homomeric and heteromeric trimers of seven subtypes (P2X1-P2X7) that confer different rates of desensitization. ...P2X receptors (P2XRs) are adenosine 5'-triphosphate (ATP)-gated ion channels comprising homomeric and heteromeric trimers of seven subtypes (P2X1-P2X7) that confer different rates of desensitization. The helical recoil model of P2XR desensitization proposes stability of the cytoplasmic cap sets the rate of desensitization, but timing of its formation is unclear for slow-desensitizing P2XRs. We report cryo-electron microscopy structures of full-length wild-type human P2X4 receptor in apo closed, antagonist-bound inhibited, and ATP-bound desensitized states. Because the apo closed and antagonist-bound inhibited state structures of this slow-desensitizing P2XR include an intact cytoplasmic cap while the ATP-bound desensitized state structure does not, the cytoplasmic cap is formed before agonist binding. Furthermore, structural and functional data suggest the cytoplasmic cap is stabilized by lipids to modulate desensitization, and P2X4 is modified by glycosylation and palmitoylation. Last, our antagonist-bound inhibited state structure reveals features specific to the allosteric ligand-binding pocket in human receptors that facilitates development of small-molecule modulators.
External linksSci Adv / PubMed:39823330 / PubMed Central
MethodsEM (single particle)
Resolution2.27 - 2.55 Å
Structure data

44799

9bqh

EMDB-44799, PDB-9bqh:
Cryo-EM structure of the full-length human P2X4 receptor in the apo closed state
Method: EM (single particle) / Resolution: 2.27 Å

44800

9bqi

EMDB-44800, PDB-9bqi:
Cryo-EM structure of BAY-1797 bound to the full-length human P2X4 receptor in the closed state
Method: EM (single particle) / Resolution: 2.55 Å

45177

9c48

EMDB-45177, PDB-9c48:
Cryo-EM structure of the full-length human P2X4 receptor in the ATP-bound desensitized state
Method: EM (single particle) / Resolution: 2.4 Å

Chemicals

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

ChemComp-LMT:
DODECYL-BETA-D-MALTOSIDE / detergent*YM

ChemComp-HOH:
WATER

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

ChemComp-ATP:
ADENOSINE-5'-TRIPHOSPHATE / ATP, energy-carrying molecule*YM

ChemComp-MG:
Unknown entry

Source
  • homo sapiens (human)
KeywordsMEMBRANE PROTEIN / Ion Channel / Ligand-gated Ion Channel / P2X Receptor / Allosteric Antagonist

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