Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
SHR Neuro Krebs Kardio Lipid Stoffw Microb
Derler, I; Fritsch, R; Schindl, R; Romanin, C.
CRAC inhibitors: identification and potential.
Expert Opin Drug Discov. 2008; 3(7): 787-800.
Doi: 10.1517/17460441.3.7.787
Web of Science
PubMed
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FullText_MUG
- Co-Autor*innen der Med Uni Graz
- Schindl Rainer
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- Abstract:
- Ca(2+) release-activated Ca(2+) (CRAC) channels, a subfamily of store-operated channels, play an essential role in various diseases such as immune disorders and allergic responses. 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. These two proteins and their activation process represent direct targets for the application of specific CRAC inhibitors. 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.
- Find related publications in this database (Keywords)
- Ca2+ release-activated Ca2+
- fluorescence resonance energy transfer
- ORAI
- store-operated channel
- stromal interaction molecule