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2-Methoxyestradiol and its derivatives inhibit store-operated Ca2+ entry in T cells: identification of a new and potent inhibitor

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2-Methoxyestradiol and its derivatives inhibit store-operated Ca2+ entry in T cells: identification of a new and potent inhibitor. / Löhndorf, Anke; Hosang, Leon; Dohle, Wolfgang; Odoardi, Francesca; Waschkowski, Sissy-Alina; Rosche, Anette; Bauche, Andreas; Winzer, Riekje; Tolosa, Eva; Windhorst, Sabine; Marry, Stephen; Flügel, Alexander; Potter, Barry V L; Diercks, Björn-Philipp; Guse, Andreas H.

In: BBA-MOL CELL RES, Vol. 1868, No. 6, 05.2021, p. 118988.

Research output: SCORING: Contribution to journal › SCORING: Journal article › Research › peer-review

Harvard

Löhndorf, A, Hosang, L, Dohle, W, Odoardi, F, Waschkowski, S-A, Rosche, A, Bauche, A, Winzer, R, Tolosa, E, Windhorst, S, Marry, S, Flügel, A, Potter, BVL, Diercks, B-P & Guse, AH 2021, '2-Methoxyestradiol and its derivatives inhibit store-operated Ca2+ entry in T cells: identification of a new and potent inhibitor', BBA-MOL CELL RES, vol. 1868, no. 6, pp. 118988. https://doi.org/10.1016/j.bbamcr.2021.118988

APA

Löhndorf, A., Hosang, L., Dohle, W., Odoardi, F., Waschkowski, S-A., Rosche, A., Bauche, A., Winzer, R., Tolosa, E., Windhorst, S., Marry, S., Flügel, A., Potter, B. V. L., Diercks, B-P., & Guse, A. H. (2021). 2-Methoxyestradiol and its derivatives inhibit store-operated Ca2+ entry in T cells: identification of a new and potent inhibitor. BBA-MOL CELL RES, 1868(6), 118988. https://doi.org/10.1016/j.bbamcr.2021.118988

Vancouver

Löhndorf A, Hosang L, Dohle W, Odoardi F, Waschkowski S-A, Rosche A et al. 2-Methoxyestradiol and its derivatives inhibit store-operated Ca2+ entry in T cells: identification of a new and potent inhibitor. BBA-MOL CELL RES. 2021 May;1868(6):118988. https://doi.org/10.1016/j.bbamcr.2021.118988

Bibtex

@article{e2247746618f47b78f62d4df49f272b6,
title = "2-Methoxyestradiol and its derivatives inhibit store-operated Ca2+ entry in T cells: identification of a new and potent inhibitor",
abstract = "T cell activation starts with formation of second messengers that release Ca2+ from the endoplasmic reticulum (ER) and thereby activate store-operated Ca2+ entry (SOCE), one of the essential signals for T cell activation. Recently, the steroidal 2-methoxyestradiol was shown to inhibit nuclear translocation of the nuclear factor of activated T cells (NFAT). We therefore investigated 2-methoxyestradiol for inhibition of Ca2+ entry in T cells, screened a library of 2-methoxyestradiol analogues, and characterized the derivative 2-Ethyl-3-sulfamoyloxy-17β-cyanomethylestra-1,3,5(10)-triene (STX564) as a novel, potent and specific SOCE inhibitor. STX564 inhibits Ca2+ entry via SOCE without affecting other ion channels and pumps involved in Ca2+ signaling in T cells. Downstream effects such as cytokine expression and cell proliferation were also inhibited by both 2-methoxyestradiol and STX564, which has potential as a new chemical biology tool.",
author = "Anke L{\"o}hndorf and Leon Hosang and Wolfgang Dohle and Francesca Odoardi and Sissy-Alina Waschkowski and Anette Rosche and Andreas Bauche and Riekje Winzer and Eva Tolosa and Sabine Windhorst and Stephen Marry and Alexander Fl{\"u}gel and Potter, {Barry V L} and Bj{\"o}rn-Philipp Diercks and Guse, {Andreas H}",
note = "Copyright {\textcopyright} 2021. Published by Elsevier B.V.",
year = "2021",
month = may,
doi = "10.1016/j.bbamcr.2021.118988",
language = "English",
volume = "1868",
pages = "118988",
journal = "BBA-MOL CELL RES",
issn = "0167-4889",
publisher = "Elsevier",
number = "6",

}

RIS

TY - JOUR

T1 - 2-Methoxyestradiol and its derivatives inhibit store-operated Ca2+ entry in T cells: identification of a new and potent inhibitor

AU - Löhndorf, Anke

AU - Hosang, Leon

AU - Dohle, Wolfgang

AU - Odoardi, Francesca

AU - Waschkowski, Sissy-Alina

AU - Rosche, Anette

AU - Bauche, Andreas

AU - Winzer, Riekje

AU - Tolosa, Eva

AU - Windhorst, Sabine

AU - Marry, Stephen

AU - Flügel, Alexander

AU - Potter, Barry V L

AU - Diercks, Björn-Philipp

AU - Guse, Andreas H

N1 - Copyright © 2021. Published by Elsevier B.V.

PY - 2021/5

Y1 - 2021/5

N2 - T cell activation starts with formation of second messengers that release Ca2+ from the endoplasmic reticulum (ER) and thereby activate store-operated Ca2+ entry (SOCE), one of the essential signals for T cell activation. Recently, the steroidal 2-methoxyestradiol was shown to inhibit nuclear translocation of the nuclear factor of activated T cells (NFAT). We therefore investigated 2-methoxyestradiol for inhibition of Ca2+ entry in T cells, screened a library of 2-methoxyestradiol analogues, and characterized the derivative 2-Ethyl-3-sulfamoyloxy-17β-cyanomethylestra-1,3,5(10)-triene (STX564) as a novel, potent and specific SOCE inhibitor. STX564 inhibits Ca2+ entry via SOCE without affecting other ion channels and pumps involved in Ca2+ signaling in T cells. Downstream effects such as cytokine expression and cell proliferation were also inhibited by both 2-methoxyestradiol and STX564, which has potential as a new chemical biology tool.

AB - T cell activation starts with formation of second messengers that release Ca2+ from the endoplasmic reticulum (ER) and thereby activate store-operated Ca2+ entry (SOCE), one of the essential signals for T cell activation. Recently, the steroidal 2-methoxyestradiol was shown to inhibit nuclear translocation of the nuclear factor of activated T cells (NFAT). We therefore investigated 2-methoxyestradiol for inhibition of Ca2+ entry in T cells, screened a library of 2-methoxyestradiol analogues, and characterized the derivative 2-Ethyl-3-sulfamoyloxy-17β-cyanomethylestra-1,3,5(10)-triene (STX564) as a novel, potent and specific SOCE inhibitor. STX564 inhibits Ca2+ entry via SOCE without affecting other ion channels and pumps involved in Ca2+ signaling in T cells. Downstream effects such as cytokine expression and cell proliferation were also inhibited by both 2-methoxyestradiol and STX564, which has potential as a new chemical biology tool.

U2 - 10.1016/j.bbamcr.2021.118988

DO - 10.1016/j.bbamcr.2021.118988

M3 - SCORING: Journal article

C2 - 33581218

VL - 1868

SP - 118988

JO - BBA-MOL CELL RES

JF - BBA-MOL CELL RES

SN - 0167-4889

IS - 6

ER -