{
"@context": "http://schema.org",
"@type": "ScholarlyArticle",
"@id": "https://doi.org/10.6084/m9.figshare.19195489",
"url": "https://tandf.figshare.com/articles/journal_contribution/Short_divalent_ethacrynic_amides_as_pro-inhibitors_of_glutathione_i_S_i_-transferase_isozyme_Mu_and_potent_sensitisers_of_cisplatin-resistant_ovarian_cancers/19195489",
"additionalType": "Journal contribution",
"name": "Short divalent ethacrynic amides as pro-inhibitors of glutathione S-transferase isozyme Mu and potent sensitisers of cisplatin-resistant ovarian cancers",
"author": [
{
"name": "Bangtian Xu",
"givenName": "Bangtian",
"familyName": "Xu"
},
{
"name": "Tingting Tong",
"givenName": "Tingting",
"familyName": "Tong"
},
{
"name": "Xin Wang",
"givenName": "Xin",
"familyName": "Wang"
},
{
"name": "Fang Liu",
"givenName": "Fang",
"familyName": "Liu"
},
{
"name": "Xiang Zhang",
"givenName": "Xiang",
"familyName": "Zhang"
},
{
"name": "Xiaolei Hu",
"givenName": "Xiaolei",
"familyName": "Hu"
},
{
"name": "Xinpeng Li",
"givenName": "Xinpeng",
"familyName": "Li"
},
{
"name": "Xiaolan Yang",
"givenName": "Xiaolan",
"familyName": "Yang"
},
{
"name": "Fei Liao",
"givenName": "Fei",
"familyName": "Liao"
}
],
"description": "The linking of ethacrynic acid with ethylenediamine and 1,4-butanediamine gave EDEA and BDEA, respectively, as membrane-permeable divalent pro-inhibitors of glutathione S-transferase (GST). Their divalent glutathione conjugates showed subnanomolar inhibition and divalence-binding to GSTmu (GSTM) (PDB: 5HWL) at ∼0.35 min−1. In cisplatin-resistant SK-OV-3, COC1, SGC7901 and A549 cells, GSTM activities probed by 15 nM BDEA or EDEA revealed 5-fold and 1.0-fold increases in cisplatin-resistant SK-OV-3 and COC1 cells, respectively, in comparison with the susceptible parental cells. Being tolerable by HEK293 and LO2 cells, BDEA at 0.2 μM sensitised resistant SK-OV-3 and COC1 cells by ∼3- and ∼5-folds, respectively, released cytochrome c and increased apoptosis; EDEA at 1.0 μM sensitised resistant SK-OV-3 and A549 cells by ∼5- and ∼7-fold, respectively. EDEA at 1.7 μg/g sensitised resistant SK-OV-3 cells to cisplatin at 3.3 μg/g in nude mouse xenograft model. BDEA and EDEA are promising leads for probing cellular GSTM and sensitising cisplatin-resistant ovarian cancers.",
"license": "https://creativecommons.org/licenses/by/4.0/legalcode",
"keywords": "Biophysics, Biochemistry, Microbiology, FOS: Biological sciences, Cell Biology, Genetics, Molecular Biology, Pharmacology, Biotechnology, Evolutionary Biology, Chemical Sciences not elsewhere classified, Immunology, FOS: Clinical medicine, Biological Sciences not elsewhere classified, Cancer, Hematology, Virology",
"contentSize": "2465141 Bytes",
"dateCreated": "2022-02-18",
"datePublished": "2022",
"dateModified": "2024-03-21",
"@reverse": {
"isBasedOn": {
"@id": "https://doi.org/10.1080/14756366.2022.2038591",
"@type": "ScholarlyArticle"
}
},
"schemaVersion": "http://datacite.org/schema/kernel-4",
"publisher": {
"@type": "Organization",
"name": "Taylor & Francis"
},
"provider": {
"@type": "Organization",
"name": "datacite"
}
}