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Membrane Protein Stable Cell Lines
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Unique sensory proteins that are expressed in practically all tissues and cell types and that are crucial for a variety of homeostatic processes make up the superfamily of Transient Receptor Potential (TRP) cation channels. One member of the TRP family, the ankyrin-repeat channel TRPA1 is of special interest for its functional diversity as a sensor of irritating and cell damaging signals, and its important role in many different diseases. Later investigations suggest that TRPA1 is involved in the detection of cold hypersensitivity rather than physiological cold pain. TRPA1 was once thought to detect noxious cold (cold pain). Additionally, a number of irritant chemicals and endogenous tissue injury byproducts activate TRPA1.

Creative Biolabs organized a professional bioinformatics team to provide our customers with TRPA drug discovery assays and related products:

Overview of TRPA

Similar to other TRP proteins, TRPA1 has six putative transmembrane segments (S1-6). The first extracellular loop between S1 and S2 comprises two putative Asn-glycosylation sites, and between S5 and S6 is the proposed ion permeable site (pore, pore helix, and selectivity filter). Up to 18 ankyrin repeat domains (ARDs), each of which is made of 33 amino acids, may be found in the lengthy N-terminal moiety. These ARDs may have a role in protein-protein interactions as well as channel trafficking to the plasma membrane. In fact, it has been demonstrated that TRPA1 ARD deletions impair the channel's ability to enter the plasma membrane.

Initially, TRPA1 was identified as a putative transduction channel present in the inner ear (the organ of Corti) and involved in hearing as well as a nociceptive channel expressed in sensory neurons of the dorsal root ganglia (DRG), trigeminal ganglia (TG), and nodose ganglia and responding to noxious cold and pungent compounds. TRPA1 is a widely expressed channel, nevertheless, that has been found in a variety of organs and tissues, including the brain, heart, small intestine, lung, skeletal muscle, and pancreas.

TRPA Drug Discovery

TRPA1 is a chemosensory channel that serves as a model channel for research into its structural and biophysical characteristics as well as an appealing therapeutic target. The bimodal effect of several TRPA1 modulators is a significant species dependency that frequently exists. It is important to understand the binding locations for these nonelectrophilic activators and their potential function as open pore blockers because TRPA1 can also be activated through a more traditional lock-and-key activation. It goes without saying that a deeper comprehension of these mechanisms is essential for the screening of new TRPA1 modulators that could be employed as potential therapeutic agents.


Note: All of our products are for Research Use Only (RUO). NOT intended for diagnostic, therapeutic or clinical use. We DO NOT offer patients any direct products or services. No products from Creative Biolabs may be resold, modified for resale or used to manufacture commercial products without prior written approval from Creative Biolabs.
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