Cu-GTSM

Cu-GTSM is a copper-containing compound and an analog of Cu-ATSM that has diverse biological activities.^1,2,3,4 It is active against methicillin-sensitive and -resistant S. aureus clinical isolates (IC₅₀s = 0.3-0.6 µM for all).¹ Cu-GTSM inhibits the growth of SK-N-MC neuroepithelioma cells and MRC-5 fibroblasts (IC₅₀s = 0.009 and 0.27 µM, respectively).² It induces the production of reactive oxygen species (ROS) in SK-N-MC cells when used at a concentration of 5 µM. Cu-GTSM (2.5 mg/kg) reduces tumor burden in the transgenic adenocarcinoma of mouse prostate (TRAMP) model but induces weight loss and renal toxicity in the same model.³ Cu-GTSM-containing positron-emitting copper isotopes have been used in PET imaging applications for copper trafficking in the TASTPM transgenic mouse model of Alzheimer’s disease.⁴

1.Haeili, M., Moore, C., Davis, C.J.C., et al.Copper complexation screen reveals compounds with potent antibiotic properties against methicillin-resistant Staphylococcus aureusAntimicrob Agents Chemother.58(7)3727-3736(2014) 2.Stefani, C., Al-Eisawi, Z., Jansson, P.J., et al.Identification of differential anti-neoplastic activity of copper bis(thiosemicarbazones) that is mediated by intracellular reactive oxygen species generation and lysosomal membrane permeabilizationJ. Inorg. Biochem.15220-37(2015) 3.Cater, M.A., Pearson, H.B., Wolyniec, K., et al.Increasing intracellular bioavailable copper selectively targets prostate cancer cellsACS Chem. Biol.8(7)1621-1631(2013) 4.Torres, J.B., Andreozzi, E.M., Dunn, J.T., et al.PET imaging of copper trafficking in a mouse model of alzheimer diseaseJ. Nucl. Med.57(1)109-114(2016)