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Custom Vector Construction> | The chicken P2X7 crystallization construct (ckP2X7cryst) was prepared by using the synthesized ckP2X7 WT (NCBI Accession Number: XP_001235163) sequence (GenScript) and subcloned into the pEG BacMam vector, with an N-terminal GFP-His8 tag, a tobacco etch virus (TEV) cleavage site and following the GSGS linker (Supplementary Table 1), and was expressed in HEK293S GnTI− (N-acetylglucosaminyl-transferase I− negative) cells (ATCC, cat. | Get A Quote |
P2X receptors are non-selective cation channels gated by extracellular ATP, and the P2X7 receptor subtype plays a crucial role in the immune and nervous systems. Altered expression and dysfunctions of P2X7 receptors caused by genetic deletions, mutations, and polymorphic variations have been linked to various diseases, such as rheumatoid arthritis and hypertension. Despite the availability of crystal structures of P2X receptors, the mechanism of competitive antagonist action for P2X receptors remains controversial. Here, we determine the crystal structure of the chicken P2X7 receptor in complex with the competitive P2X antagonist, TNP-ATP. The structure reveals an expanded, incompletely activated conformation o... More