Inhibition of calmodulin-dependent and independent cardiac sarcoplasmic reticulum activities by R24571.

Abstract:

:R24571 a derivative of the antimycotic miconazole, appears to be 5 to 8 times more potent than trifluoperazine in its ability to inhibit the calmodulin-dependent phosphorylation of cardiac sarcoplasmic reticulum vesicles. The cAMP-dependent protein kinase mediated phosphorylation of cardiac sarcoplasmic reticulum was not affected by R24571. Sarcoplasmic reticulum Ca-dependent ATPase phosphoprotein intermediate formation was inhibited by R24571 concentrations that were 20 to 30 times greater than those required to inhibit calmodulin-dependent phosphorylation. However, both Ca-dependent and independent ATPase activities, as well as calcium uptake, were inhibited by R24571 concentrations that were similar to, or less than, those concentrations required to inhibit calmodulin-dependent sarcoplasmic reticulum phosphorylation. These results indicate the caution that should be exercised in using this new compound in assessing the possible involvement of calmodulin in other membrane processes.

journal_name

Cell Calcium

journal_title

Cell calcium

authors

Louis CF,Turnquist J,Jarvis B

doi

10.1016/0143-4160(83)90039-8

subject

Has Abstract

pub_date

1983-04-01 00:00:00

pages

107-16

issue

2

eissn

0143-4160

issn

1532-1991

pii

0143-4160(83)90039-8

journal_volume

4

pub_type

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