Ion Channel Modulation

Aside from the binding of a ligand or other stimuli that activate the ion channel, the gating of the ion channel can be affected by other factors that affect the ease of opening the ion channel. This process is loosely referred to as modulation and can occur through the binding of a second messenger or a covalent modification of the ion channel such as phosphorylation. The role of modulation is to tweak or fine-tune the gating of an ion channel, although in some instances the line between modulation and gating can be blurred. For example, the phosphorylation of CFTR is necessary for channel openings to occur.

In general, modulation events originate at receptors that are at a distance from the ion channel. The response is usually slower in onset because a second messenger needs to be generated and then diffuse to the ion channel. The signal transduction cascade also branches off to influence other effectors that produce major changes in a cell's functioning. The modulation of ion channels can be part of long-lasting changes in the cell.

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