2-Aminoethyl diphenylborinate (2-APB) analogues: Regulation of Ca signaling |
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| Authors: | Shoichiro Ozaki Akinobu Z. Suzuki Peter O. Bauer Etsuko Ebisui Katsuhiko Mikoshiba |
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| Affiliation: | 1. Laboratory for Developmental Neurobiology, Brain Science Institute, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan;2. Department of Neuroscience, Mayo Clinic, 4500 San Pablo Road, Jacksonville, FL 32224, USA |
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| Abstract: | In order to obtain compounds with modified 2-APB activities, we synthesized number of 2-APB analogues and analyzed their inhibitory activities for SOCE. The IC50 of 2-APB for SOCE inhibition is 3 μM while IC50 of some of our 2-APB analogues range 0.1–10 μM. The adducts of amino acids with diphenyl borinic acid have strong inhibitory activities. By using these compounds, we will be able to regulate intracellular Ca2+ concentration and consequent cellular processes more efficiently than with 2-APB. |
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| Keywords: | 2-APB 2-APB analogue Regulator of intracellular Ca2+ concentration SOCE |
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