Specific interactions of new antitumor unsymmetrical bisacridines, UAs, with DNA and ABC proteins and their potential to modulate the enzymatic activity and trancription of nuclear receptor as the elements of their molecular mechanism of action.
Details
- Project's acronym:
- BisMolMechZM2020
- Financial Program Name:
- OPUS
- Organization:
- Narodowe Centrum Nauki (NCN) (National Science Centre)
- Agreement:
- UMO-2019/33/B/NZ7/02534 z dnia 2020-04-02
- Realisation period:
- 2020-04-02 - 2023-04-01
- Project manager:
- prof. dr hab. inż. Zofia Mazerska
- Team members:
-
- Coordination of the studies in the field of biological response of tumor cells. dr hab. Ewa Augustin
- The tasks in the field of enzyme gene expression modulation and cell transport. dr inż. Monika Pawłowska
- Studies on the mechanism of DNA G-quadruplexes stabilisation by the studied compounds. dr hab. inż. Tomasz Laskowski
- The synthesis of the appropriate amounts of the studied bisacridine derivatives/ dr inż. Ewa Paluszkiewicz
- The tasks in the field of drug cytotoxicity, drug metabolism and nuclear receptor induction. dr Joanna Frąckowiak
- The tasks on the cellular level related to metabolism and cellular response. Jolanta Kulesza
- Studies in the field of physicochemical properties and drug metabolism in noncellular systems. Michał Kosno
- Realised in:
- Department of Pharmaceutical Technology and Biochemistry
- External institutions
participating in project: -
- Clinical Research Centre, Medical University of Białystok (Poland)
- Project's value:
- 3 011 700.00 PLN
- Request type:
- National Research Programmes
- Domestic:
- Domestic project
- Verified by:
- Gdańsk University of Technology
Papers associated with that project
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total: 4
Catalog Projects
Year 2025
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Distinct cellular uptake patterns of two anticancer unsymmetrical bisacridines and their metabolic transformation in tumor cells.
PublicationUnsymmetrical bisacridines (UAs) represent a novel class of anticancer agents. Their high cytotoxicity towards multiple human cancer cell lines and inhibition of human tumor xenograft growth in nude mice signal their potential for cancer treatment. Therefore, the mechanism of their strong biological activity is broadly investigated. Here, we explore the efflux and metabolism of UAs, as both strongly contribute to the development...
Year 2022
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Acid–Base Equilibrium and Self-Association in Relation to High Antitumor Activity of Selected Unsymmetrical Bisacridines Established by Extensive Chemometric Analysis
PublicationUnsymmetrical bisacridines (UAs) represent a novel class of anticancer agents previously synthesized by our group. Our recent studies have demonstrated their high antitumor potential against multiple cancer cell lines and human tumor xenografts in nude mice. At the cellular level, these compounds affected 3D cancer spheroid growth and their cellular uptake was selectively modulated by quantum dots. UAs were shown to undergo metabolic...
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c-Myc Protein Level Affected by Unsymmetrical Bisacridines Influences Apoptosis and Senescence Induced in HCT116 Colorectal and H460 Lung Cancer Cells
PublicationUnsymmetrical bisacridines (UAs) are highly active antitumor compounds. They contain in their structure the drugs previously synthesized in our Department: C-1311 and C-1748. UAs exhibit different properties than their monomer components. They do not intercalate to dsDNA but stabilize the G-quadruplex structures, particularly those of the MYC and KRAS genes. Since MYC and KRAS are often mutated and constitutively expressed in cancer...
Year 2021
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Metabolic Profiles of New Unsymmetrical Bisacridine Antitumor Agents in Electrochemical and Enzymatic Noncellular Systems and in Tumor Cells
PublicationNew unsymmetrical bisacridines (UAs) demonstrated high activity not only against a set of tumor cell lines but also against human tumor xenografts in nude mice. Representative UA compounds, named C-2028, C-2045 and C-2053, were characterized in respect to their physicochemical properties and the following studies aimed to elucidate the role of metabolic transformations in UAs action. We demonstrated with phase I and phase II enzymes...
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