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In rats peritoneal macrophages, we investigated the effect of sigma-1 receptor inhibitors in Ca2+ signaling in macrophages, as well as disulfide-containing immunomodulators Glutoxim and Molixan. " For the first time, chlorpromazine and trifluoperazine reduce both phases of Ca2+ responses in rats peritoneal macrophages using Fura-2AM microfluorimetry.
Source link: https://doi.org/10.1134/S1990519X22030075
"Despite significant advancements in diagnostic and therapeutic techniques, lung cancer remains the most common cause of cancer-related deaths worldwide. " About 85% of lung cancer cases are due to non-small cell lung cancer. However, the effects of antipsychotic drugs on NSCLC must be investigated further. We investigated the effects of trifluoperazine, a commonly used antipsychotic drug, and its synthetic analogs on human lung cancer cells A549. TFP-related genes and pathways that can be directly linked to improved lung cancer survivors, as shown by the following graphs. Cell migration of A549 cells has been greatly reduced by TFP-dependent/independence colony formation, anchorage-dependent/independence colony formation, and cell migration. The expression of genes linked to A549 cells' apoptosis and survival were affected by treatment with 3dc. In all experiments, including in vitro studies of metastatic lung cancer progression, 3dc had more potent anticancer effects than TFP. ".
Source link: https://doi.org/10.3390/biomedicines10051046
"The protein has been shown as a calmodulin-like calcium-binding protein with an EF-hand motif and as a target of trifluoperazine, a calmodulin antagonist in eukaryotes that reduces mycobacterial growth. " We outlined the recombinant protein of Rv1211 and conducted scientific and biochemical analysis of Rv1211 and its interaction with Ca2+ or trifluoperazine here. Rv1211 has unfolded structure in the subsequent circular dichroism experiments with temperature increase and trifluoroethanol treatment. Rv1211 did bind to trifluoperazine as shown by two-dimensional NMR spectra of 15N-labeled Rv1211. The Kd of trifluoperazine-Rv1211 binding is 41 bcM and the stoichiometry is 1: 2 based on titration calorimetry, according to Isothermal titration calorimetry. Our findings support Rv1211 as a Ca2+-binding calmodulin-like protein, and reveal that Rv1211 is a natively unfolded protein that binds to trifluozine. ".
Source link: https://doi.org/10.1016/j.bbrc.2022.04.045
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