Synthesis of bisboron compounds and their strong inhibitory activity on store-operated calcium entry.
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.
Suzuki
Akinobu Z
AZ
Laboratory for Developmental Neurobiology, Brain Development Research Group, Brain Science Institute, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan.
Ozaki
Shoichiro
S
Goto
Jun-Ichi
J
Mikoshiba
Katsuhiko
K
D001889:Borinic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001896:Boron Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002118:Calcium / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D015220:Calcium Channels; D006801:Humans; D020128:Inhibitory Concentration 50; D019169:Jurkat Cells; D015394:Molecular Structure; D015398:Signal Transduction / Q000187:drug effects
D001889:Borinic Acids; D001896:Boron Compounds; D015220:Calcium Channels; C109986:2-aminoethoxydiphenyl borate; D002118:Calcium