Antiproliferative Activity of Pt(IV) Conjugates Containing the Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) Ketoprofen and Naproxen † Article Swipe
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· 2019
· Open Access
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· DOI: https://doi.org/10.3390/ijms20123074
Cisplatin and several non-steroidal anti-inflammatory drugs (NSAIDs) have been proven to act synergistically or at least additively on several tumor cell lines. Dual-action cisplatin-based Pt(IV) combos containing ketoprofen and naproxen offer good antiproliferative performance on a panel of human tumor cell lines, including a malignant pleural mesothelioma (MPM) one, a very chemoresistant tumor. The main reason of the increased activity relies on the enhanced lipophilicity of these Pt(IV) conjugates that in turn promotes increased cellular accumulation. A quick Pt(IV)→Pt(II) reduction generates the active cisplatin metabolite. The NSAID adjuvant action seems to be almost independent from cyclooxygenase-2 (COX-2) expression in the tumor cells under investigation (lung A-549, colon HT-29, HCT 116, SW480, ovarian A2780, and biphasic MPM MSTO-211H), but it seems to rely (at least in part) on the activation of the NSAID activated gene, NAG-1 (a member of the transforming growth factor beta, TGF-β, superfamily), which has been suggested to be involved in NSAID antiproliferative activity.
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- article
- Language
- en
- Landing Page
- https://doi.org/10.3390/ijms20123074
- https://www.mdpi.com/1422-0067/20/12/3074/pdf?version=1561348701
- OA Status
- gold
- Cited By
- 41
- References
- 74
- Related Works
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- OpenAlex ID
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https://openalex.org/W2952260938Canonical identifier for this work in OpenAlex
- DOI
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https://doi.org/10.3390/ijms20123074Digital Object Identifier
- Title
-
Antiproliferative Activity of Pt(IV) Conjugates Containing the Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) Ketoprofen and Naproxen †Work title
- Type
-
articleOpenAlex work type
- Language
-
enPrimary language
- Publication year
-
2019Year of publication
- Publication date
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2019-06-24Full publication date if available
- Authors
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Mauro Ravera, Ilaria Zanellato, Elisabetta Gabano, Elena Perin, Beatrice Rangone, Marco Morelli Coppola, Domenico OsellaList of authors in order
- Landing page
-
https://doi.org/10.3390/ijms20123074Publisher landing page
- PDF URL
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https://www.mdpi.com/1422-0067/20/12/3074/pdf?version=1561348701Direct link to full text PDF
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YesWhether a free full text is available
- OA status
-
goldOpen access status per OpenAlex
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https://www.mdpi.com/1422-0067/20/12/3074/pdf?version=1561348701Direct OA link when available
- Concepts
-
Naproxen, Cisplatin, Ketoprofen, Chemistry, Pharmacology, Adjuvant, Lipophilicity, Metabolite, Diclofenac, Cell growth, Cyclooxygenase, Mechanism of action, Active metabolite, Chemotherapy, Medicine, In vitro, Biochemistry, Immunology, Enzyme, Internal medicine, Pathology, Alternative medicineTop concepts (fields/topics) attached by OpenAlex
- Cited by
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41Total citation count in OpenAlex
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2025: 4, 2024: 6, 2023: 9, 2022: 7, 2021: 13Per-year citation counts (last 5 years)
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74Number of works referenced by this work
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10Other works algorithmically related by OpenAlex
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