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Development of pyrene-based fluorescent ether lipid as inhibitor of SK3 ion channels

Abstract : We report the synthesis of three bioactive pyrene-based fluorescent analogues of Ohmline which is the most efficient and selective inhibitor of SK3 ion channel. The interaction of these Ohmline-pyrene (OP1-3) with liposomes of different composition reveals that only OP2 and OP3 are readily integrated into liposomes. Fluorescence measurements indicate that, depending on their concentration, OP2 and OP3 exist either as monomer or as a mixture of monomer and excimers within the liposome bilayer. Among the three Ohmline Pyrene compounds (OP1-3) only OP2 is able to reduce SK3 currents and is the first efficient fluorescent modulator of SK3 channel as revealed by patch clamp measurements (- 71.3 ± 13.3% at 10 mM) and by its inhibition of SK3-dependent cancer cell migration at (32.5% ± 4.8% at 1 mM). We also report the first fluorescence study on living breast cancer cells (MDA-MB-231) showing that OP2 is rapidly integrated in bio-membranes followed by cell internalization.
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Submitted on : Monday, October 17, 2022 - 8:35:26 AM
Last modification on : Tuesday, October 18, 2022 - 11:37:32 AM


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Alicia Bauduin, Marion Papin, Aurélie Chantôme, Hélène Couthon, Laure Burel-Deschamps, et al.. Development of pyrene-based fluorescent ether lipid as inhibitor of SK3 ion channels. European Journal of Medicinal Chemistry, 2021, 209, pp.112894. ⟨10.1016/j.ejmech.2020.112894⟩. ⟨hal-02997273⟩



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