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Tytuł:
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Antiproliferative effects of sulphonamide carbonic anhydrase inhibitors C18, SLC-0111 and acetazolamide on bladder, glioblastoma and pancreatic cancer cell lines.
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Autorzy:
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Mussi S; Experimental Oncology and Immunology, Department of Molecular and Translational Medicine, University of Brescia, Brescia, Italy.
Rezzola S; Experimental Oncology and Immunology, Department of Molecular and Translational Medicine, University of Brescia, Brescia, Italy.
Chiodelli P; Experimental Oncology and Immunology, Department of Molecular and Translational Medicine, University of Brescia, Brescia, Italy.
Nocentini A; NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, University of Florence, Sesto Fiorentino, Florence, Italy.
Supuran CT; NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, University of Florence, Sesto Fiorentino, Florence, Italy.
Ronca R; Experimental Oncology and Immunology, Department of Molecular and Translational Medicine, University of Brescia, Brescia, Italy.
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Źródło:
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Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2022 Dec; Vol. 37 (1), pp. 280-286.
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Typ publikacji:
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Journal Article
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Język:
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English
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Imprint Name(s):
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Original Publication: Basingstoke, UK : Taylor & Francis, c2002-
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MeSH Terms:
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Acetazolamide/*pharmacology
Antineoplastic Agents/*pharmacology
Carbonic Anhydrase Inhibitors/*pharmacology
Carbonic Anhydrases/*metabolism
Sulfonamides/*pharmacology
Acetazolamide/chemical synthesis ; Acetazolamide/chemistry ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Carbonic Anhydrase Inhibitors/chemical synthesis ; Carbonic Anhydrase Inhibitors/chemistry ; Cell Movement/drug effects ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Humans ; Molecular Structure ; Structure-Activity Relationship ; Sulfonamides/chemical synthesis ; Sulfonamides/chemistry ; Tumor Cells, Cultured
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References:
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Contributed Indexing:
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Keywords: Carbonic anhydrase inhibitors; SLC-0111; bladder cancer; glioblastoma; pancreatic cancer
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Substance Nomenclature:
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0 (Antineoplastic Agents)
0 (Carbonic Anhydrase Inhibitors)
0 (Sulfonamides)
EC 4.2.1.1 (Carbonic Anhydrases)
O3FX965V0I (Acetazolamide)
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Entry Date(s):
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Date Created: 20211213 Date Completed: 20220223 Latest Revision: 20221028
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Update Code:
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20240105
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PubMed Central ID:
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PMC8667884
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DOI:
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10.1080/14756366.2021.2004592
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PMID:
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34894950
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Carbonic anhydrase IX/XII (CA IX/XII), are cell-surface enzymes typically expressed by cancer cells as a form of adaptation to hypoxia and acidosis. It has been widely reported that these proteins play pivotal roles in cancer progression fostering cell migration, aggressiveness and resistance to first line chemo- and radiotherapies. CA IX has emerged as a promising target in cancer therapy and several approaches and families of compounds were characterised in the attempt to find optimal targeting by inhibiting of the high catalytic activity of the enzyme. In the present work, different cell lines representing glioblastoma, bladder and pancreatic cancer have been exploited to compare the inhibitory and antiproliferative effect of primary sulphonamide acetazolamide (AAZ), the Phase Ib/II clinical grade sulphonamide SLC-0111, and a membrane-impermeant positively charged, pyridinium-derivative (C18). New hints regarding the possibility to exploit CA inhibitors in these cancer types are proposed.