Calmodulin

Calmodulin antagonists and inhibitors bind calmodulin, the main calcium sensor inside eukaryotic cells. Calmodulin is a small protein with four helix-loop-helix calcium-binding motifs that binds calcium ions and then regulates kinases, phosphatases, ion channels and phosphodiesterases. Its 1985 crystal structure showed two globular lobes joined by a long central helix. Naphthalenesulfonamides were among the first synthetic antagonists, and a 1981 study reported that W-7 inhibits cell proliferation. W-5 hydrochloride, an analog without the chlorine atom, binds calmodulin more weakly and often serves as a control. Fluphenazine-N-2-chloroethane hydrochloride is a phenothiazine-derived antagonist, and DY-9760e is a further calmodulin inhibitor. Calcium/calmodulin-dependent protein kinases are listed in the neighboring CaMK category.

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