Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca²⁺ entry in MDA-MB-231 breast cancer cells using a Fluorescence Imaging Plate Reader assay

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• 作者：Iman Azimi^a ; ^b ; ^c ; ¹ ; Jack U. Flanagan^d ; ^e ; ¹ ; Ralph J. Stevenson^d ; Marco Inserra^f ; ^g ; Irina Vetter^f ; ^g ; Gregory R. Monteith^a ; ^b ; ^c ; William A. Denny^d ; ^e ; ^{b.denny@auckland.ac.nz}
• 关键词：Calcium signalling ; Store-operated calcium entry (SOCE) ; Pharmacological inhibitors ; Pharmacophore modelling ; Orai1 ; Breast cancer
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：1 January 2017
• 年：2017
• 卷：25
• 期：1
• 页码：440-449
• 全文大小：4332 K
• 卷排序：25

文摘

A Fluorescence Imaging Plate Reader assay for calcium channel inhibitors. Inhibitors of the Orai1 SOCE Ca2+ channel that do not affect Ca2+ store release. Similarity-based screening assay to identify triazole-based Orai1 inhibitors.