
pmid: 15808509
The melastatin-related transient receptor potential channel TRPM2 is a plasma membrane Ca2+-permeable cation channel that is activated by intracellular adenosine diphosphoribose (ADPR) binding to the channel's enzymatic Nudix domain. Channel activity is also seen with nicotinamide dinucleotide (NAD+) and hydrogen peroxide (H2O2), but their mechanisms of action remain unknown. Here, we identify cyclic adenosine diphosphoribose (cADPR) as an agonist of TRPM2 with dual activity: at concentrations above 100 microM, cADPR can gate the channel by itself, whereas lower concentrations of 10 microM have a potentiating effect that enables ADPR to gate the channel at nanomolar concentrations. ADPR's breakdown product adenosine monophosphate (AMP) specifically inhibits ADPR, but not cADPR-mediated gating of TRPM2, whereas the cADPR antagonist 8-Br-cADPR exhibits the reverse block specificity. Our results establish TRPM2 as a coincidence detector for ADPR and cADPR signaling and provide a functional context for cADPR as a second messenger for Ca2+ influx.
Cyclic ADP-Ribose, Patch-Clamp Techniques, Membrane Proteins, TRPM Cation Channels, Cell Biology, Hydrogen Peroxide, Kidney, Adenosine Monophosphate, Ion Channels, Cell Line, Membrane Potentials, Humans, Calcium, Calcium Signaling, Molecular Biology, Ion Channel Gating
Cyclic ADP-Ribose, Patch-Clamp Techniques, Membrane Proteins, TRPM Cation Channels, Cell Biology, Hydrogen Peroxide, Kidney, Adenosine Monophosphate, Ion Channels, Cell Line, Membrane Potentials, Humans, Calcium, Calcium Signaling, Molecular Biology, Ion Channel Gating
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