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TitleCryo-EM structures of the human P2X1 receptor reveal subtype-specific architecture and antagonism by supramolecular ligand-binding.
Journal, issue, pagesNat Commun, Vol. 15, Issue 1, Page 8490, Year 2024
Publish dateOct 1, 2024
AuthorsAdam C Oken / Nicolas E Lisi / Ismayn A Ditter / Haoyuan Shi / Nadia A Nechiporuk / Steven E Mansoor /
PubMed AbstractP2X receptors are a family of seven trimeric non-selective cation channels that are activated by extracellular ATP to play roles in the cardiovascular, neuronal, and immune systems. Although it is ...P2X receptors are a family of seven trimeric non-selective cation channels that are activated by extracellular ATP to play roles in the cardiovascular, neuronal, and immune systems. Although it is known that the P2X1 receptor subtype has increased sensitivity to ATP and fast desensitization kinetics, an underlying molecular explanation for these subtype-selective features is lacking. Here we report high-resolution cryo-EM structures of the human P2X1 receptor in the apo closed, ATP-bound desensitized, and the high-affinity antagonist NF449-bound inhibited states. The apo closed and ATP-bound desensitized state structures of human P2X1 define subtype-specific properties such as distinct pore architecture and ATP-interacting residues. The NF449-bound inhibited state structure of human P2X1 reveals that NF449 has a unique dual-ligand supramolecular binding mode at the interface of neighboring protomers, inhibiting channel activation by overlapping with the canonical P2X receptor ATP-binding site. Altogether, these data define the molecular pharmacology of the human P2X1 receptor laying the foundation for structure-based drug design.
External linksNat Commun / PubMed:39353889 / PubMed Central
MethodsEM (single particle)
Resolution2.42 - 2.9 Å
Structure data

45152

9c2a

EMDB-45152, PDB-9c2a:
Cryo-EM structure of the human P2X1 receptor in the apo closed state
Method: EM (single particle) / Resolution: 2.74 Å

45153

9c2b

EMDB-45153, PDB-9c2b:
Cryo-EM structure of the human P2X1 receptor in the ATP-bound desensitized state
Method: EM (single particle) / Resolution: 2.42 Å

45154

9c2c

EMDB-45154, PDB-9c2c:
Cryo-EM structure of the human P2X1 receptor in the NF449-bound inhibited state
Method: EM (single particle) / Resolution: 2.9 Å

Chemicals

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

ChemComp-Y01:
CHOLESTEROL HEMISUCCINATE

ChemComp-HOH:
WATER

ChemComp-MG:
Unknown entry

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

PDB-1ali:
ALKALINE PHOSPHATASE MUTANT (H412N)

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

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