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CAPP‐calmodulin: A potent competitive inhibitor of calmodulin actions

1984; Wiley; Volume: 165; Issue: 2 Linguagem: Inglês

10.1016/0014-5793(84)80183-0

1873-3468

Dianne L. Newton, Claude B. Klee,

Synthesis and biological activity

A covalent adduct of norchlorpromazine (CAPP) and calmodulin is a very potent antagonist of calmodulin activation of several enzymes. The phenothiazine‐calmodulin complex (CAPP‐calmodulin) acts as a pure antagonist with phosphodiesterase and myosin kinase or a partial agonist with the phosphoprotein phosphatase, calcineurin. Because of its potency and the selectivity inherent to its calmodulin moiety, CAPP‐calmodulin should be a uniquely useful probe of calmodulin actions.