Characterization of ATP-Gated P2X Receptor Ion Channels

Creative Bioarray is committed to integrating various techniques to help clients analyze the structure, function, and therapeutic potential of ATP-gated P2X receptor ion channels. We are confident to offer our clients professional scientific services and technical support, providing molecular insights into the functional roles of these channels.

Introduction

P2X receptors (P2XRs), or P2X purinoceptors, are a family of cation-permeable ligand-gated ion channels that are expressed throughout the body and mediate a variety of functions, including muscle contraction, neuronal excitability, and bone formation. When the P2X receptor binds to extracellular ATP, the P2X channel opens, allowing cations (Na⁺, Ca²⁺, etc.) to pass through. At present, seven P2X receptor subtypes (P2X1-7) have been identified, which have two transmembrane (TM) domains, intracellular N- and C-termini, and a large extracellular loop.

Biochemical analysis suggests that P2XR subunits assemble as homo- or hetero-trimers with a range of phenotypes and functions. They generally have different properties in terms of agonist sensitivity and/or the time course of response. These receptors offer new therapeutic targets for a variety of diseases, including arterial thrombosis, pain, and irritable bowel syndrome. Therefore, it is necessary to determine the molecular mechanisms of P2XR related to ATP binding, ion conduction, channel gating, and regulation, as well as characterize the role of receptor subunits in native systems by various methods including mutagenesis, biochemical studies, electrophysiology, etc.

Fig. 1 P2X receptor (P2XR) structures. (Schmid, 2019)

Our Services

We provide our clients with P2XRs characterization services, mainly focusing on structural analysis, functional analysis, and the nature of interactions with other proteins. Our services include but not limited to:

• Localization and expression pattern analysis of ATP-gated P2XRs in different tissues, such as in dorsal root ganglion (DRG) neurons.
• Analysis of P2XR structure and ligand action. We use X-ray crystallography technology to help clients characterize the overall structure and subunit structure of P2XRs, and analyze the conformational changes around ATP binding sites after ATP binding. In addition, we provide the analysis of agonist and antagonist binding sites of P2XRs.
• Analysis of P2X receptor subunit assembly and characterization. We provide clients with the identification of recombinant P2XRs and analysis of their properties, including time course and ATP sensitivity.
• Analysis of the interaction between P2XRs and other ligand-gated ion channels, such as GABA_A, GABA_C, and 5HT₃ receptors.
• Functional characterization of P2XRs in native cells. We provide the characterization of the P2XR subtype for native receptors based on a combination of expression/localization, functional, pharmacological, and knockout/knockdown approaches.
• Analysis of the therapeutic potential of P2XRs. We focus on helping our clients analyze the physiological and pathophysiological effects of ATP acting on the identified P2XR subtypes.

Applications

• Study on the molecular basis of agonist action and antagonist action of P2XRs
• Study on the competitive inhibition of the ATP-gated P2XR channels
• Study on the P2XRs function and pathophysiological roles

Creative Bioarray has advanced experimental instruments and a professional research team to ensure high-quality P2XRs characterization services for our clients, accelerating the development of novel drugs for the treatment of P2XRs-related diseases. If you are interested in our services, please contact us for more details.

Reference

1. Schmid, R.; Evans, R. J. ATP-gated P2X receptor channels: molecular insights into functional roles. Annual Review of Physiology, 2019, 81: 43-62.