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Proposed TRPV4 potentiation mechanism.

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posted on 11.05.2010, 00:23 by Rainer Strotmann, Marcus Semtner, Frauke Kepura, Tim D. Plant, Torsten Schöneberg

(A) In the resting state, an N-terminal site (filled box) binds to a C-terminal domain (open box) thus permitting only weak channel activation. The hatched lines in the fourth transmembrane region are meant to indicate that the interaction can occur between channel subunits or possibly within a channel subunit. (B) Increase of the intracellular calcium concentration to micromolar concentrations leads to Ca2+/CaM binding to the C-terminal site and displacement of the N-terminal interaction site. The corresponding conformational change induces further increase in channel activity. In the potentiated state, the N-terminal binding site may form a homologous interaction with a second channel subunit.

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