Biological Activity
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
References
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)
