• TRPM2

    Mean concentration-response data for rosiglitazone inhibition of TRPM3 activated by 5 μM PregS or TRPM2 activated by 1 mM H2O2

    Majeed et al. (2011)

TRPM2 | Transient Receptor Potential Cation Channel Subfamily M Member 2

Family:
Transient  receptor potential channels

Subgroups:
TRPC (TRPC1–TRPC7), TRPV (TRPV1-TRPV6), TRPA1, TRPM (TRPM1–TRPM8), TRPP (TRPP1–TRPP3, PKD1, PKDREJ, PKDL1–PKDL3), TRPML (TRPML1–TRPML3), TRPN

Topology:
Most TRP channels are composed of 6 transmembrane domains (helices) with intracellular N- and C-termini, non-selectively permeable to various cations

TRPM2: Background information

TRPM2 is a tetrameric cation channel that is permeable to calcium, sodium, and potassium. It is regulated by and is also activated by intracellular endogenous ligands and reactive oxygen species.

Gene:
TRPM2

Human Protein:
UniProt O94759

Tissue:
Brain, pancreas, spleen, kidney and a wide range of immunocytes, including lymphocytes, neutrophils, and monocytes/macrophages

Function/ Application:
TRPM2 is a thermosensitive channel which functions as ligand-gated ion channel. It mediates Sodium and Calcium influx into the cell, leading to increased cytoplasmic Calcium levels. TRPM2 contributes to Ca2+ release from intracellular stores in response to ADP-ribose. The ion channel plays a role in numerous processes that involve signaling via intracellular Ca2+ levels e.g. for the dendritic cell differentiation and maturation, and in dendritic cell chemotaxis or in the regulation of the reorganization of the actin cytoskeleton, or for the filopodia formation in response to reactive oxygen species via its role in increasing cytoplasmic Ca2+ and Zn2+ levels. It participates in immunity and inflammation processes, insulin secretion and body temperature regulation.

Pathology:
Alzheimer's disease, auto inflammatory and metabolic diseases, such as gout, obesity and diabetes

Endogenous agonists/ antagonists:
ADPR and cyclic ADPR (cADPR) activate TRPM2. Furthermore pyridine dinucleotides bind to TRPM2 (which might be not involved in TRPM2 activation) including β-nicotinamide adenine dinucleotide (NAD), nicotinic acid adenine dinucleotide (NAAD) and NAAD-2’-phosphate (NAADP). TRPM2 is also activated by redox signals and its activation is involved in cell death induced by oxidative stress. Inactivated by intracellular ATP.

Interaction:
Calmodulin, EFHC1, PKCơ, PTPL1, Ras-related C3 botulinum toxin substrate 1 (Rac1), Polyubiquitin-C

Modulator:
Flufenamic Acid, Clotrimazole, Econazole

Assays:
Patch Clamp: whole cell, temperature control, intracellular solution exchange

Recommended Reviews:
International Union of Pharmacology. XLIII. Compendium of voltage-gated ion channels: transient receptor potential channels., Pharmacol Rev 55(4):591-6 Clapham, et al. 2003

Publications

2011 - Rapid and Contrasting Effects of Rosiglitazone on Transient Receptor Potential TRPM3 and TRPC5 Channels

icon pl  Patchliner publication in Molecular Pharmacology (2011)

Authors: 
Majeed Y., Bahnasi Y., Seymour V.A.L., Wilson L.A., Milligan C.J., Agarwal A.K., Sukumar P., Naylor J., Beech D.J.

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