双硼化合物的合成及其对钙库操纵性钙内流的强抑制活性。
Synthesis of bisboron compounds and their strong inhibitory activity on store-operated calcium entry.
机构信息
Laboratory for Developmental Neurobiology, Brain Development Research Group, Brain Science Institute, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan.
出版信息
Bioorg Med Chem Lett. 2010 Feb 15;20(4):1395-8. doi: 10.1016/j.bmcl.2009.12.108. Epub 2010 Jan 11.
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.
钙库操纵性钙内流（SOCE）是一种重要的机制，用于补充细胞内钙库并维持钙信号。我们开发了一种合成双硼化合物的方法，这些化合物在一个分子中具有两个硼酸或其酯。这些化合物是 2-APB 的类似物，2-APB 广泛用作膜通透 SOCE 抑制剂。此外，我们研究了新合成的双硼化合物对 Jurkat T 细胞中 SOCE 的影响。所有双硼化合物对 SOCE 均表现出强烈的抑制活性，IC50 值均小于 1μM，比观察到的 2-APB 低 20-45 倍。
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