Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: DrugBank:EXPT01586 (G418)
 2,237 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Store-operated Ca(2+) entry is a major Ca(2+) entry mechanism that is present in most cell types. In immune cells, store-operated Ca(2+) entry is almost exclusively mediated by Ca(2+) release-activated Ca(2+) (CRAC) channels. Ca(2+) entry through these channels and the corresponding cytosolic Ca(2+) signals are required for many immune cell functions, including all aspects of T-cell activation. ORAI proteins are the molecular correlates for the CRAC channels. The three human members, ORAI1, ORAI2 and ORAI3, are activated through the stromal interaction molecules (STIM)1 and 2 following depletion of endoplasmic reticulum Ca(2+) stores. Different combinations of STIM and ORAI can form different CRAC channels with distinct biophysical properties. In this article, we review and discuss mechanistic and functional implications of two important CRAC/ORAI inhibitors, 2-APB and BTP2, and the antibiotic G418 that has also been reported to interfere with ORAI channel function. The use of pharmacological tools should help to assign distinct physiological and pathophysiological functions to different STIM-ORAI protein complexes.
 ...
PMID:Pharmacology of ORAI channels as a tool to understand their physiological functions. 2211 11