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  1. Article ; Online: G-quadruplex ligands as therapeutic agents against cancer, neurological disorders and viral infections.

    Yan, Mock Phooi / Wee, Chua Eng / Yen, Khor Poh / Stevens, Aaron / Wai, Lam Kok

    Future medicinal chemistry

    2023  Volume 15, Issue 21, Page(s) 1987–2009

    Abstract: G-quadruplexes (G4s) within the human genome have undergone extensive molecular investigation, with a strong focus on telomeres, gene promoters and repetitive regulatory sequences. G4s play central roles in regulating essential biological processes, ... ...

    Abstract G-quadruplexes (G4s) within the human genome have undergone extensive molecular investigation, with a strong focus on telomeres, gene promoters and repetitive regulatory sequences. G4s play central roles in regulating essential biological processes, including telomere maintenance, replication, transcription and translation. Targeting these molecular processes with G4-binding ligands holds substantial therapeutic potential in anticancer treatments and has also shown promise in treating neurological, skeletal and muscular disorders. The presence of G4s in bacterial and viral genomes also suggests that G4-binding ligands could be a critical tool in fighting infections. This review provides an overview of the progress and applications of G4-binding ligands, their proposed mechanisms of action, challenges faced and prospects for their utilization in anticancer treatments, neurological disorders and antiviral activities.
    MeSH term(s) Humans ; G-Quadruplexes ; Virus Diseases/drug therapy ; Neoplasms/drug therapy ; Nervous System Diseases/drug therapy ; Ligands ; Telomere
    Chemical Substances Ligands
    Language English
    Publishing date 2023-11-07
    Publishing country England
    Document type Journal Article ; Review ; Research Support, Non-U.S. Gov't
    ISSN 1756-8927
    ISSN (online) 1756-8927
    DOI 10.4155/fmc-2023-0202
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Biomimetic amphiphilic chitosan nanoparticles: Synthesis, characterization and antimicrobial activity

    Ahmad, Nuraziemah / Wee, Chua Eng / Wai, Lam Kok / Zin, Noraziah Mohamad / Azmi, Fazren

    Carbohydrate polymers. 2021 Feb. 15, v. 254

    2021  

    Abstract: Naturally derived antimicrobial peptides (AMPs) are an attractive source of new antimicrobial agents. However, clinical application of AMPs is associated with poor bioavailability and toxicity. In this study, we address these limitations by designing a ... ...

    Abstract Naturally derived antimicrobial peptides (AMPs) are an attractive source of new antimicrobial agents. However, clinical application of AMPs is associated with poor bioavailability and toxicity. In this study, we address these limitations by designing a new series of chitosan derivatives to mimic the amphiphilic topology of AMPs. The synthesized chitosan derivatives were found to self-assemble into nanoparticles in the aqueous environment. Among the compounds, a chitosan derivative grafted with arginine and oleic acid (CH-Arg-OA) exhibited the most potent antimicrobial activity, especially against Gram-negative bacteria. It also caused minimal cell death when tested in HEK293 and HepG2 cell lines, thus confirming the role of cationicity and lipophilicity for selective bacteria targeting. CH-Arg-OA exhibited its antimicrobial activity by disrupting bacterial membranes and causing the leakage of cytoplasmic contents. Thus, amphiphilic chitosan nanoparticles offer a great promise as a new class of AMPs mimics that is effective against Gram-negative bacteria.
    Keywords antimicrobial peptides ; antimicrobial properties ; arginine ; bioavailability ; biomimetics ; cell death ; chitosan ; human cell lines ; lipophilicity ; oleic acid ; topology ; toxicity
    Language English
    Dates of publication 2021-0215
    Publishing place Elsevier Ltd
    Document type Article
    ZDB-ID 1501516-6
    ISSN 1879-1344 ; 0144-8617
    ISSN (online) 1879-1344
    ISSN 0144-8617
    DOI 10.1016/j.carbpol.2020.117299
    Database NAL-Catalogue (AGRICOLA)

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  3. Article ; Online: Biomimetic amphiphilic chitosan nanoparticles: Synthesis, characterization and antimicrobial activity.

    Ahmad, Nuraziemah / Wee, Chua Eng / Wai, Lam Kok / Zin, Noraziah Mohamad / Azmi, Fazren

    Carbohydrate polymers

    2020  Volume 254, Page(s) 117299

    Abstract: Naturally derived antimicrobial peptides (AMPs) are an attractive source of new antimicrobial agents. However, clinical application of AMPs is associated with poor bioavailability and toxicity. In this study, we address these limitations by designing a ... ...

    Abstract Naturally derived antimicrobial peptides (AMPs) are an attractive source of new antimicrobial agents. However, clinical application of AMPs is associated with poor bioavailability and toxicity. In this study, we address these limitations by designing a new series of chitosan derivatives to mimic the amphiphilic topology of AMPs. The synthesized chitosan derivatives were found to self-assemble into nanoparticles in the aqueous environment. Among the compounds, a chitosan derivative grafted with arginine and oleic acid (CH-Arg-OA) exhibited the most potent antimicrobial activity, especially against Gram-negative bacteria. It also caused minimal cell death when tested in HEK293 and HepG2 cell lines, thus confirming the role of cationicity and lipophilicity for selective bacteria targeting. CH-Arg-OA exhibited its antimicrobial activity by disrupting bacterial membranes and causing the leakage of cytoplasmic contents. Thus, amphiphilic chitosan nanoparticles offer a great promise as a new class of AMPs mimics that is effective against Gram-negative bacteria.
    MeSH term(s) Anti-Bacterial Agents/chemistry ; Antimicrobial Cationic Peptides/chemistry ; Arginine/chemistry ; Bacterial Outer Membrane/drug effects ; Biomimetic Materials/chemistry ; Biomimetics/methods ; Carbodiimides/chemistry ; Cell Survival/drug effects ; Chitosan/chemistry ; Erythrocytes/drug effects ; Gram-Negative Bacteria/drug effects ; Gram-Negative Bacteria/metabolism ; HEK293 Cells ; Hemolysis/drug effects ; Hep G2 Cells ; Humans ; Microbial Sensitivity Tests ; Nanoparticles/chemistry ; Oleic Acid/chemistry ; Surface-Active Agents/chemistry
    Chemical Substances Anti-Bacterial Agents ; Antimicrobial Cationic Peptides ; Carbodiimides ; Surface-Active Agents ; Oleic Acid (2UMI9U37CP) ; Chitosan (9012-76-4) ; Arginine (94ZLA3W45F)
    Language English
    Publishing date 2020-10-23
    Publishing country England
    Document type Journal Article
    ZDB-ID 1501516-6
    ISSN 1879-1344 ; 0144-8617
    ISSN (online) 1879-1344
    ISSN 0144-8617
    DOI 10.1016/j.carbpol.2020.117299
    Database MEDical Literature Analysis and Retrieval System OnLINE

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