| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1363552 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
Store-operated calcium entry (SOCE) is an important mechanism for replenishing intracellular calcium stores and for sustaining calcium signaling. We developed a method for synthesis of bisboron compounds that have two borinic acids or their esters in one molecule. These compounds are analogues of 2-APB, which is widely used as a membrane-permeable SOCE inhibitor. Further, we examined the effect of the newly synthesized bisboron compounds on SOCE in Jurkat T cells. All the bisboron compounds showed strong inhibitory activity on SOCE, with IC50 values of less than 1 μM, which were 20–45 times lower than observed with 2-APB.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Akinobu Z. Suzuki, Shoichiro Ozaki, Jun-Ichi Goto, Katsuhiko Mikoshiba,