Hydrophobic regions of calmodulin and calmodulin antagonists

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Structure-activity Relationship of Calmodulin Antagonists

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Calmodulin antagonists inhibit secretion in Paramecium

Secretion in Paramecium is Ca2+-dependent and involves exocytic release of the content of the secretory organelle, known as the trichocyst. The content, called the trichocyst matrix, undergoes a Ca2+-induced reordering of its paracrystalline structure during release, and we have defined three stages in this expansion process. The stage I, or fully condensed trichocyst, is the 4 microns-long mem...

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Potentiation of DNA damage and cytotoxicity by calmodulin antagonists.

Many physical and chemical agents used in anti-neoplastic therapy are known to act by effecting DNA damage. The possibility that calmodulin may be an important modulator of the response to DNA damage in eukaryotic cells has been explored in a number of studies which use calmodulin antagonists in combination with agents known to damage DNA. We review these studies and discuss the therapeutic pot...

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Comparison of the calmodulin antagonists compound 48/80 and calmidazolium.

The two presumed calmodulin antagonists calmidazolium and compound 48/80 were compared for their effects on several calmodulin-dependent and calmodulin-independent enzyme systems. Compound 48/80 and calmidazolium were found to be about equipotent in antagonizing the calmodulin-dependent fraction of brain phosphodiesterase and erythrocyte Ca2+-transporting ATPase. Compound 48/80 combines high po...

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Local anesthetics, mepacrine, and propranolol are antagonists of calmodulin.

Local anesthetics such as dibucaine, QX572, tetracaine, and phenacaine, as well as other drugs with local anesthetic-like properties (e.g., mepacrine, propranolol, and SKF 525A) inhibit the specific calmodulin-dependent stimulation of erythrocyte Ca2+-ATPase (ATP phosphohydrolase, EC 3.6.1.3) and cyclic nucleotide phosphodiesterases (3',5'-cyclic-nucleotide 5'-nucleotidohydrolase, EC 3.1.4.17) ...

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ژورنال

عنوان ژورنال: Japanese Journal of Pharmacology

سال: 1981

ISSN: 0021-5198

DOI: 10.1016/s0021-5198(19)54625-x