Two novel 2-aminoethyl diphenylborinate (2-APB) analogues differentially activate and inhibit store-operated Ca(2+) entry via STIM proteins.

Cell Calcium
Jun-Ichi GotoK Mikoshiba

Abstract

Store-operated calcium entry (SOCE) or calcium release-activated calcium current (I(CRAC)) is a critical pathway to replenish intracellular calcium stores, and plays indispensable roles in cellular functions such as antigen-induced T lymphocyte activation. Despite the importance of I(CRAC) in cellular functions, lack of potent and specific inhibitor has limited the approaches to the function of I(CRAC) in native cells. 2-Aminoethyl diphenylborinate (2-APB) is a widely used SOCE/I(CRAC) inhibitor, while its effect is rather unspecific. In the attempt to develop more potent and selective compounds here we identified two structurally isomeric 2-APB analogues that are 100-fold more potent than 2-APB itself. One of the 2-APB analogues activates and inhibits endogenous SOCE depending on the concentration while the other only inhibits it. The 2-APB analogue inhibits store depletion-mediated STIM1 clustering as well as heterologously expressed CRAC current. Together with the observation that, unlike 2-APB, the analogue compounds failed to activate CRACM3/Orai3 current in the absence of STIM, our results suggest that inhibition and activation of SOCE/I(CRAC) by the 2-APB analogues is mediated by STIM.

References

Jun 15, 2004·The Journal of Biological Chemistry·Hong-Zhen HuMichael X Zhu
Mar 25, 2005·Physiological Reviews·Anant B Parekh, James W Putney
Jul 12, 2005·Current Biology : CB·Jen LiouTobias Meyer
Apr 26, 2006·The Journal of General Physiology·Mingjiang LiLixia Yue
May 31, 2006·Nature Cell Biology·Christine PeineltJean-Pierre Kinet
Jul 25, 2006·Current Biology : CB·Jonathan SoboloffDonald L Gill
Sep 19, 2006·Current Biology : CB·Monika VigReinhold Penner
Oct 19, 2006·Biochemical and Biophysical Research Communications·Pingyong XuTao Xu
Nov 1, 2006·Proceedings of the National Academy of Sciences of the United States of America·Yoshihiro BabaTomohiro Kurosaki
Dec 5, 2006·Biochemical and Biophysical Research Communications·Hong ZhouKatsuhiko Mikoshiba
May 23, 2007·Cell Calcium·Paul F WorleyShmuel Muallem
May 23, 2007·Proceedings of the National Academy of Sciences of the United States of America·Jen LiouTobias Meyer
Apr 19, 2008·The Journal of Biological Chemistry·Shenyuan L ZhangMichael D Cahalan
May 20, 2008·The Journal of Biological Chemistry·Wayne I DeHavenJames W Putney
May 24, 2008·The Journal of Biological Chemistry·Rainer SchindlChristoph Romanin
Apr 21, 2009·Proceedings of the National Academy of Sciences of the United States of America·Youjun WangDonald L Gill

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Citations

Jul 7, 2012·Purinergic Signalling·Sriram Govindan, Colin W Taylor
Feb 9, 2011·Proceedings of the National Academy of Sciences of the United States of America·Andrea Maul-PavicicStephan Ehl
Jan 5, 2011·The Journal of Biological Chemistry·Megumi YamashitaMurali Prakriya
Oct 29, 2010·Cold Spring Harbor Perspectives in Biology·Colin W Taylor, Stephen C Tovey
Aug 24, 2010·Molecular Interventions·James W Putney
Oct 4, 2011·High Altitude Medicine & Biology·Demosthenes G PapamatheakisSean M Wilson
Nov 8, 2011·Biochemical and Biophysical Research Communications·Peter O BauerNobuyuki Nukina
Jan 26, 2010·Bioorganic & Medicinal Chemistry Letters·Akinobu Z SuzukiKatsuhiko Mikoshiba
Feb 1, 2011·Experimental Physiology·Jaime ChávezLuis M Montaño
Oct 17, 2015·The Journal of Physical Chemistry. B·Hao DongMichael L Klein
Mar 19, 2014·British Journal of Pharmacology·Huma SaleemColin W Taylor
Dec 17, 2014·Advances in Biological Regulation·Katsuhiko Mikoshiba
Jun 13, 2015·BioMed Research International·Ingrid LajdovaAlzbeta Marcek Chorvatova
Oct 11, 2013·Channels·Marc FahrnerChristoph Romanin
Jun 29, 2013·Channels·Amit Jairaman, Murali Prakriya
Sep 17, 2013·Biochemical and Biophysical Research Communications·Shoichiro OzakiKatsuhiko Mikoshiba
May 6, 2016·Future Medicinal Chemistry·Chengsen TianMinyong Li
May 1, 2010·Expert Review of Clinical Pharmacology·Ivan BogeskiChristine Peinelt
Oct 21, 2011·Physiological Reviews·Alberto DarszonClaudia L Treviño
Sep 27, 2019·Current Drug Targets·Sampath Bhuvaneshwari, Kavitha Sankaranarayanan
Jul 1, 2016·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Selvakumar SubramaniamNaim Akhtar Khan
Oct 28, 2019·Current Molecular Pharmacology·Melvin N RosalezMarvin A Soriano-Ursúa
Aug 1, 2020·Frontiers in Pharmacology·Sendoa Tajada, Carlos Villalobos
Sep 25, 2015·Physiological Reviews·Murali Prakriya, Richard S Lewis
May 28, 2020·International Journal of Molecular Sciences·Megan NoblePeter B Stathopulos
Jan 1, 2016·Cancer Research·Noël J-M RaynalJean-Pierre J Issa
Sep 24, 2020·Annual Review of Pharmacology and Toxicology·Daniel BakowskiAnant B Parekh
Dec 18, 2020·Journal of Cell Science·Anthony J Morgan, Antony Galione
Dec 29, 2020·Expert Opinion on Drug Discovery·Jessica GambardellaGaetano Santulli
Dec 30, 2020·International Journal of Molecular Sciences·Camille Le GuilcherOlivier Dellis
Jan 1, 2020·Expert Review of Precision Medicine and Drug Development·Husain Yar KhanAsfarSohail Azmi
Apr 16, 2021·ACS Medicinal Chemistry Letters·Silvio AprileTracey Pirali
May 4, 2021·Frontiers in Cell and Developmental Biology·Heba ShawerMarc A Bailey
Jun 15, 2021·Frontiers in Pharmacology·Xiaojing LiangWeidong Han
Aug 8, 2021·International Journal of Molecular Sciences·Adéla Tiffner, Isabella Derler
Aug 26, 2021·Journal of Cell Science·Anthony J Morgan, Antony Galione

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