2. Academic Validation
  3. Synthesis of bisboron compounds and their strong inhibitory activity on store-operated calcium entry

Synthesis of bisboron compounds and their strong inhibitory activity on store-operated calcium entry

  • Bioorg Med Chem Lett. 2010 Feb 15;20(4):1395-8. doi: 10.1016/j.bmcl.2009.12.108.
Akinobu Z Suzuki 1,  Shoichiro Ozaki,  Jun-Ichi Goto,  Katsuhiko Mikoshiba
Affiliations

Affiliation

  • 1 Laboratory for Developmental Neurobiology, Brain Development Research Group, Brain Science Institute, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan.
PMID: 20097561 DOI: 10.1016/j.bmcl.2009.12.108
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.

Figures