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1.A.7.1.1
ATP-gated cation channel (purinoceptor or ATP-neuroreceptor). Residues Glu52-Gly96 play roles in agonist binding and channel gating (Allsopp et al., 2011).  The rat protein is 89% identical to the human ortholog. Mutations likely to confer ivermectin sensitivity to human P2X1 have been proposed (Pasqualetto et al. 2018).  The P2X1 receptor is a trimeric ligand-gated ion channel that plays an important role in urogenital and immune functions. Bennetts et al. 2024 employed cryogenic electron microscopy (cryo-EM) to elucidate the structures of the P2X1 receptor in an ATP-bound desensitised state and an NF449-bound closed state. NF449, a potent P2X1 receptor antagonist, engages the receptor distinctively, while ATP, the endogenous ligand, binds in a manner consistent with other P2X receptors. To explore the molecular basis of receptor inhibition, activation, and ligand interactions, key residues involved in ligand and metal ion binding were mutated. Radioligand binding assays with [3H]-α,β-methylene ATP and intracellular calcium ion influx assays were used to evaluate the effects of these mutations. These experiments validated key ligand-receptor interactions and identified conserved and non-conserved residues critical for ligand binding or receptor modulation (Bennetts et al. 2024). 

Accession Number:P47824
Protein Name:P2X1 aka P2RX1
Length:399
Molecular Weight:44957.00
Species:Rattus norvegicus (Rat) [10116]
Number of TMSs:2
Location1 / Topology2 / Orientation3: Membrane1 / Multi-pass membrane protein2
Substrate cation

Cross database links:

RefSeq: NP_037129.1   
Entrez Gene ID: 25505   
Pfam: PF00864   

Gene Ontology

GO:0016021 C:integral to membrane
GO:0045121 C:membrane raft
GO:0005886 C:plasma membrane
GO:0043234 C:protein complex
GO:0019717 C:synaptosome
GO:0005524 F:ATP binding
GO:0008144 F:drug binding
GO:0004931 F:extracellular ATP-gated cation channel acti...
GO:0005515 F:protein binding
GO:0008270 F:zinc ion binding
GO:0006811 P:ion transport
GO:0051291 P:protein heterooligomerization
GO:0051260 P:protein homooligomerization
GO:0019228 P:regulation of action potential in neuron
GO:0008217 P:regulation of blood pressure
GO:0035249 P:synaptic transmission, glutamatergic
GO:0042310 P:vasoconstriction

References (3)

[1] “A new class of ligand-gated ion channel defined by P2x receptor for extracellular ATP.”  Valera S.et.al.   7523951
[2] “The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).”  The MGC Project Teamet.al.   15489334
[3] “Identification of mRNAs associated with programmed cell death in immature thymocytes.”  Owens G.P.et.al.   2072913

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Predict TMSs (Predict number of transmembrane segments)
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FASTA formatted sequence
1:	MARRLQDELS AFFFEYDTPR MVLVRNKKVG VIFRLIQLVV LVYVIGWVFV YEKGYQTSSD 
61:	LISSVSVKLK GLAVTQLQGL GPQVWDVADY VFPAHGDSSF VVMTNFIVTP QQTQGHCAEN 
121:	PEGGICQDDS GCTPGKAERK AQGIRTGNCV PFNGTVKTCE IFGWCPVEVD DKIPSPALLR 
181:	EAENFTLFIK NSISFPRFKV NRRNLVEEVN GTYMKKCLYH KIQHPLCPVF NLGYVVRESG 
241:	QDFRSLAEKG GVVGITIDWK CDLDWHVRHC KPIYQFHGLY GEKNLSPGFN FRFARHFVQN 
301:	GTNRRHLFKV FGIHFDILVD GKAGKFDIIP TMTTIGSGIG IFGVATVLCD LLLLHILPKR 
361:	HYYKQKKFKY AEDMGPGEGE HDPVATSSTL GLQENMRTS