Characterization of IP3 Receptors

Creative Bioarray is committed to providing high-quality inositol 1,4,5-trisphosphate receptors (IP3Rs) characterization services to accelerate the understanding of IP3 receptor properties from structure to function. Our recognized professional level and accumulated successful experience ensure that we can provide you with reliable and rigorous scientific results.

Introduction

IP3R is a major intracellular calcium release channel located mainly in the endoplasmic reticulum (ER) membrane. There are three main subtypes of IP3Rs, which are distributed in different tissues and have different physiological functions. These tetrameric calcium channels, consisting of six transmembrane segments, function in a number of important physiological processes by influencing intracellular calcium signaling, including excitatory contractile coupling, cell cycle regulation, intercellular communication, gene expression, and learning and memory.

IP3Rs have been implicated in the development of tumors, cardiovascular disease, and neurodegenerative disorders. Furthermore, because IP3Rs have multiple direct and allosteric regulatory site regulation, it is an excellent target for therapeutic agent development as well as pharmacology specific to various cellular pathways. Despite recent advances in the structural characterization of IP3Rs, the molecular mechanisms involved in regulating IP3R activity remain incomplete. Therefore, further studies on the molecular structure and function of IP3Rs are important not only for basic life research but also for the prevention, treatment, and diagnosis of clinical diseases.

Fig. 1 IP3 receptors are stimulated by IP3 and Ca²⁺. (Prole, 2019)

Our Services

We help our clients characterize the structure and function of IP3Rs through multiple technologies. Our services include but not limited to:

• Structure characterization of IP3Rs.

We focus on the optimization of cryoelectron microscopy, crystallography, and other technologies to provide clients with higher resolution structural information on IP3R gating conformations.

• Analysis of conformational changes in the pre-active states.
• Analysis of conformational changes in pore opening mediated by Ca²⁺ binding.
• Analysis of ATP binding sites.
• Structural analysis of the transmembrane domain (TMD) in the open conformation.
• Biophysical characterization of IP3Rs.

We help our clients analyze the biophysical properties of IP3Rs through electrophysiological technology, such as analyzing the activity and functional changes of channels under different Ca²⁺ concentrations.

• Analysis of interaction between IP3R and many accessory proteins, such as calmodulin (CaM), carbonic anhydrase-related protein (CARP), cyclin-B1 (CYB), end-binding protein 3 (EB3), and stromal interaction molecule 1 (STIM1).
• Identification of IP3R inhibitors.

Applications

• Modeling of the regulatory loop of IP3Rs
• Study on the molecular mechanism of IP3R channel gating
• Study on the pharmacological significance of IP3Rs

Equipped with state-of-the-art laboratory facilities and a dedicated research team, Creative Bioarray is well placed to provide comprehensive IP3 receptors characterization services to our clients. We help you to gain information about the structure and function of the IP3 receptors, contributing to a deeper understanding of the structural basis of IP3 receptor gating and the physiopathological significance of IP3 receptors. If you are interested in our services, please contact us for more details.

Reference

1. Prole, D. L.; Taylor, C. W. Structure and function of IP3 receptors. Cold Spring Harbor Perspectives in Biology, 2019, 11(4): a035063.