Design, synthesis and pharmacological characterization of analogs of 2-aminoethyl diphenylborinate (2-APB), a known store-operated calcium channel blocker, for …

A Hofer, G Kovacs, A Zappatini, M Leuenberger…

Index: Hofer, Alexandre; Kovacs, Gergely; Zappatini, Anna; Leuenberger, Michele; Hediger, Matthias A.; Lochner, Martin Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 11 p. 3202 - 3213

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Citation Number: 15

Abstract

2-Aminoethyl diphenylborinate (2-APB) is a known modulator of the IP3 receptor, the calcium ATPase SERCA, the calcium release-activated calcium channel Orai and TRP channels. More recently, it was shown that 2-APB is an efficient inhibitor of the epithelial calcium channel TRPV6 which is overexpressed in prostate cancer. We have conducted a structure–activity relationship study of 2-APB congeners to understand their inhibitory ...