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Structure paper

TitleHigh-affinity agonism at the P2X receptor is mediated by three residues outside the orthosteric pocket.
Journal, issue, pagesNat Commun, Vol. 15, Issue 1, Page 6662, Year 2024
Publish dateAug 6, 2024
AuthorsAdam C Oken / Nicolas E Lisi / Ipsita Krishnamurthy / Alanna E McCarthy / Michael H Godsey / Arthur Glasfeld / Steven E Mansoor /
PubMed AbstractP2X receptors are trimeric ATP-gated ion channels that activate diverse signaling cascades. Due to its role in apoptotic pathways, selective activation of P2X is a potential experimental tool and ...P2X receptors are trimeric ATP-gated ion channels that activate diverse signaling cascades. Due to its role in apoptotic pathways, selective activation of P2X is a potential experimental tool and therapeutic approach in cancer biology. However, mechanisms of high-affinity P2X activation have not been defined. We report high-resolution cryo-EM structures of wild-type rat P2X bound to the high-affinity agonist BzATP as well as significantly improved apo receptor structures in the presence and absence of sodium. Apo structures define molecular details of pore architecture and reveal how a partially hydrated Na ion interacts with the conductance pathway in the closed state. Structural, electrophysiological, and direct binding data of BzATP reveal that three residues just outside the orthosteric ATP-binding site are responsible for its high-affinity agonism. This work provides insights into high-affinity agonism for any P2X receptor and lays the groundwork for development of subtype-specific agonists applicable to cancer therapeutics.
External linksNat Commun / PubMed:39107314 / PubMed Central
MethodsEM (single particle)
Resolution2.49 - 2.78 Å
Structure data

41570

8tr5

EMDB-41570, PDB-8tr5:
Cryo-EM structure of the rat P2X7 receptor in the apo closed state
Method: EM (single particle) / Resolution: 2.53 Å

41581

8trj

EMDB-41581, PDB-8trj:
Cryo-EM structure of the rat P2X7 receptor in complex with the high-affinity agonist BzATP
Method: EM (single particle) / Resolution: 2.78 Å

42976

8v4s

EMDB-42976, PDB-8v4s:
Cryo-EM structure of the rat P2X7 receptor in the apo closed state purified in the absence of sodium
Method: EM (single particle) / Resolution: 2.49 Å

Chemicals

ChemComp-GDP:
GUANOSINE-5'-DIPHOSPHATE / GDP, energy-carrying molecule*YM

ChemComp-ZN:
Unknown entry

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

ChemComp-PLM:
PALMITIC ACID

ChemComp-NA:
Unknown entry

ChemComp-HOH:
WATER


ChemComp, No image

ChemComp-KD9:
Unknown entry

Source
  • rattus (rat)
KeywordsMEMBRANE PROTEIN / Ion Channel / Ligand-gate Ion Channel / P2X Receptor / Allosteric Antagonist / High-Affinity Agonist

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