Chloroquine, quinine and quinidine inhibit calcium release from macrophage intracellular stores by blocking inositol 1,4,5-trisphosphate binding to its receptor.
Journal Article (Journal Article)
The binding of many ligands to cellular receptors induces a signaling cascade which generates inositol 1,4,5-trisphosphate (IP3). IP3 binding to its receptors in various internal compartments causes a rapid Ca2+ efflux into the cytosol. We now demonstrate that chloroquine blocks ligand-induced Ca2+ mobilization without affecting IP3 synthesis. The effect is independent of the ligand employed and occurred with five unrelated ligands; namely, alpha 2-macroglobulin-methylamine, angiotensin II, bradykinin, carbachol, and epidermal growth factor. Chloroquine, quinidine, and quinine, however, block binding of [3H]IP3 to its receptors by 90%, 88%, and 71%, respectively. These observations suggest a previously undetected mechanism by which these agents may in part function as antimalarials.
Full Text
Duke Authors
Cited Authors
- Misra, UK; Gawdi, G; Pizzo, SV
Published Date
- February 1997
Published In
Volume / Issue
- 64 / 2
Start / End Page
- 225 - 232
PubMed ID
- 9027583
International Standard Serial Number (ISSN)
- 0730-2312
Digital Object Identifier (DOI)
- 10.1002/(sici)1097-4644(199702)64:2<225::aid-jcb6>3.0.co;2-z
Language
- eng
Conference Location
- United States