Journal
EXPERT OPINION ON DRUG DISCOVERY
Volume 3, Issue 7, Pages 787-800Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1517/17460441.3.7.787
Keywords
Ca2+ release-activated Ca2+; fluorescence resonance energy transfer; ORAI; store-operated channel; stromal interaction molecule
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Funding
- Austrian Science Fund [P18169, W1201]
- Austrian Science Fund (FWF) [P18169, W1201] Funding Source: Austrian Science Fund (FWF)
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Background: Ca2+ release-activated Ca2+ (CRAC) channels, a subfamily of store-operated channels, play an essential role in various diseases such as immune disorders and allergic responses. Objective: The successful treatment of these diseases requires the identification of specific inhibitors. So far, a variety of chemical compounds blocking CRAC have been identified; however, they have all turned out to be less specific. Recently two proteins, STIM1 and ORAI1, have been identified as the essential components that fully reconstitute CRAC currents with a similar biophysical fingerprint. Method: These two proteins and their activation process represent direct targets for the application of specific CRAC inhibitors. Results/conclusion: For drug development, fluorescence microscopy adaptable for high-throughput screening will provide a powerful assay to mechanistically identify potential CRAC inhibitors that act on various stages within the STIM1/ORAI1 activation pathway visualized by fluorescent-tagged proteins.
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