Localization of ATP-gated P2X Channels

Creative Bioarray aims to provide clients with high-quality localization services for ATP-gated P2X channels and help them explore the ATP binding sites of P2X receptors. Our expert technical support will help accelerate our clients' understanding of the broad tissue distribution of P2X receptors and the mechanisms of P2X receptor activation, providing background information for future studies of these receptors in animal disease models.

Background

The P2X receptor family of ATP ligand-gated channels is non-selective cation channels consisting of homo- or heterodimeric trimers. Their permeability to Ca²⁺ is greater than that of Na⁺ and K⁺. P2X channels exist in many organisms and are the third largest family of mammalian transmitter-gated ion channels. The P2X receptor family consists of seven isoforms, P2X1-7, which are highly relevant to the pharmacology of a given P2X receptor. The different subunits show different sensitivities to purinergic agonists and antagonists.

There has been considerable progress in the study of P2 receptors, including their classification, distribution, biochemical properties, signal transduction mechanisms, and biological functions. The development of potential therapeutic agents targeting P2 receptors has rapidly expanded to a wide range of diseases, including cystic fibrosis, asthma, inflammation, incontinence, cancer, and pain. In addition to drug selectivity, the tissue distribution of the targeted receptor is an important factor to consider in order to reduce the side effects of potential drugs. Therefore, the localization of ATP-gated P2X channels is important for the drug development of P2X channel-related diseases.

Fig. 1 The subcellular distribution of P2X receptors. (Robinson, 2013)

Our Services

We offer our clients a variety of strategies to explore the broad distribution of P2X receptors in a variety of tissues such as the central nervous system, smooth muscle cells, immune cells, and more.

• Providing information on the distribution of the P2X receptors by autoradiography with [³H]α,β-MeATP.
• Providing subcellular distribution of P2X receptors by immunocytochemical procedures. We combine immunocytochemistry with signal enhancement techniques to help our clients reveal the existence of P2X receptors in fine structures such as sensory nerve fibers in the skin.

In addition, we have established a variety of experimental methods to help our clients explore the ATP binding sites in P2X receptors.

• Analysis of ATP binding sites based on systematic site-directed mutagenesis and electrophysiological characterization.
• Precise localization of the ATP-binding sites by the strategy of site-directed affinity labeling.
• Identification of ATP-binding sites by voltage-clamp fluorometry and site-directed fluorescence labeling.
• Providing important information on the ATP binding mechanisms by photoaffinity labeling experiments.

Applications

• Study on physiological functions of P2X subtypes
• Study on the pharmacology of P2X receptors
• Development of new competitive antagonists with therapeutic properties

With our extensive expertise and advanced technology platform, Creative Bioarray is well-positioned to provide our clients with services for the localization of ATP-gated P2X channels and their ATP-binding sites. We look forward to becoming your reliable scientific assistant and developing efficient and cost-effective experimental schemes for you. If you are interested in our services, please contact us for more details.

Reference

1. Robinson, L. E.; Murrell-Lagnado, R. D. The trafficking and targeting of P2X receptors. Frontiers in cellular neuroscience, 2013, 7: 233.