title: 2-Aminoethyl diphenylborinate (2-APB) analogues: regulation of Ca2+ signaling.
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.
authors.affiliation: Laboratory for Developmental Neurobiology, Brain Science Institute, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan. Electronic address: ozaki-0991@m.jcnnet.jp.
authors.forename: Shoichiro
authors.initials: S
authors.lastname: Ozaki
authors.forename: Akinobu Z
authors.initials: AZ
authors.lastname: Suzuki
authors.forename: Peter O
authors.initials: PO
authors.lastname: Bauer
authors.forename: Etsuko
authors.initials: E
authors.lastname: Ebisui
authors.forename: Katsuhiko
authors.initials: K
authors.lastname: Mikoshiba
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy / Q000378:metabolism; D000818:Animals; D001896:Boron Compounds / Q000737:chemistry* / Q000494:pharmacology*; D016466:CHO Cells; D020013:Calcium Signaling / Q000187:drug effects*; D003412:Cricetulus; D006331:Heart Diseases / Q000188:drug therapy / Q000378:metabolism
chemical_list: C538758:2-aminoethyl diphenylborinate; D001896:Boron Compounds
keywords: 2-APB; 2-APB analogue; Regulator of intracellular Ca(2+) concentration; SOCE