TRPM2 channel
| Channel name | TRPM21,2,3,4,5,6,7 |
| Description | Nucleotide-sensing TRP channel |
| Other names | TRPC7, LTRPC2 |
| Molecular information | Human unigene: Hs0.369759, chr. 21q22.3 |
| Mouse unigene: Mm0.276762, chr. 10 C1 | |
| Associated subunits | Not established |
| Functional assays | Patch-clamp, calcium imaging |
| Current | Weakly voltage-sensitive cation current |
| Conductance | 60pS, 58pS (negative potentials); 76pS at positive potentials |
| H2O2-induced channel (52.3pS), β-NAD+-activated channel (59pS) | |
| Ion selectivity | Nonselective, permeant to Na+, Ca2+, and K+ |
| Activation | Redox sensor, activation by H2O2 and TNF-α; modulated by arachidonic acid |
| Inactivation | Flufenamic acid, clotrimazole, econazole, PARP inhibitors |
| Activators | ADP-ribose, β-NAD+, increased [Ca2+]i potentiates (EC50 = 340 nM) |
| Gating inhibitors | None |
| Blockers | None |
| Radioligands | None |
| Channel distribution | Brain, placenta, lung, spinal cord, spleen, lymphocytes |
| Physiological functions | Not established |
| Mutations and pathophysiology | Not established |
| Pharmacological significance | Not established |
chr., chromosome; NAD, nicotinamide adenine dinucleotide; TNF, tumor necrosis factor; PARP, poly(ADP-ribose) polymerase.
↵1. Nagamine K, Kudoh J, Minoshima S, Kawasaki K, Asakawa S, Ito F, and Shimizu N (1998) Molecular cloning of a novel putative Ca2+ channel protein (TRPC7) highly expressed in brain. Genomics 54:124-131
↵2. Perraud AL, Fleig A, Dunn CA, Bagley LA, Launay P, Schmitz C, Stokes AJ, Zhu Q, Bessman MJ, Penner R, et al. (2001) ADP-ribose gating of the calcium-permeable LTRPC2 channel revealed by Nudix motif homology. Nature (Lond) 411:595-599
↵3. Sano Y, Inamura K, Miyake A, Mochizuki S, Yokoi H, Matsushime H, and Furuichi K (2001) Immunocyte Ca2+ influx system mediated by LTRPC2. Science (Wash DC) 293:1327-1330
↵4. Hara Y, Wakamori M, Ishii M, Maeno E, Nishida M, Yoshida T, Yamada H, Shimizu S, Mori E, Kudoh J, et al. (2002) LTRPC2 Ca2+-permeable channel activated by changes in redox status confers susceptibility to cell death. Mol Cell 9:163-173
↵5. Hill K, McNulty S, and Randall AD (2004) Inhibition of TRPM2 channels by the antifungal agents clotrimazole and econazole. Naunyn Schmiedeberg's Arch Pharmacol 370:227-237
↵6. Fonfria E, Marshall IC, Benham CD, Boyfield I, Brown JD, Hill K, Hughes JP, Skaper SD, and McNulty S (2004) TRPM2 channel opening in response to oxidative stress is dependent on activation of poly(ADP-ribose) polymerase. Br J Pharmacol 143:186-192
↵7. Kraft R, Grimm C, Grosse K, Hoffmann A, Sauerbruch S, Kettenmann H, Schultz G, Harteneck C (2004) Hydrogen peroxide, and ADP-ribose induce TRPM2-mediated calcium influx and cation currents in microglia. Am J Physiol Cell Physiol 286:C129-C137