Author(s): Suzuki AZ, Ozaki S, Goto J, Mikoshiba K
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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 microM, which were 20-45 times lower than observed with 2-APB. Copyright 2010 Elsevier Ltd. All rights reserved.
This article was published in Bioorg Med Chem Lett
and referenced in Journal of Bioengineering & Biomedical Science