Literature DB >> 24036266

2-Aminoethyl diphenylborinate (2-APB) analogues: regulation of Ca2+ signaling.

Shoichiro Ozaki1, Akinobu Z Suzuki, Peter O Bauer, Etsuko Ebisui, Katsuhiko Mikoshiba.   

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 Ca(2+) concentration and consequent cellular processes more efficiently than with 2-APB.
Copyright © 2013 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  2-APB; 2-APB analogue; Regulator of intracellular Ca(2+) concentration; SOCE

Mesh:

Substances:

Year:  2013        PMID: 24036266     DOI: 10.1016/j.bbrc.2013.08.102

Source DB:  PubMed          Journal:  Biochem Biophys Res Commun        ISSN: 0006-291X            Impact factor:   3.575


  2 in total

1.  The Ca(2+) channel inhibitor 2-APB reverses β-amyloid-induced LTP deficit in hippocampus by blocking BAX and caspase-3 hyperactivation.

Authors:  Wei-Yan Hu; Zhi-Yong He; Lu-Jun Yang; Ming Zhang; Da Xing; Zhi-Cheng Xiao
Journal:  Br J Pharmacol       Date:  2015-02-27       Impact factor: 8.739

2.  Synthesis and Characterization of Store-Operated Calcium Entry Inhibitors Active in the Submicromolar Range.

Authors:  Camille Le Guilcher; Tomas Luyten; Jan B Parys; Mathieu Pucheault; Olivier Dellis
Journal:  Int J Mol Sci       Date:  2020-12-21       Impact factor: 5.923

  2 in total

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