Boron Neutron Capture Therapy (BNCT) is a cancer treatment which combines tumor-selective boron delivery agents with thermal neutrons in order to selectively eradicate cancer cells. In this work, we focus on the early-stage development of carbohydrate delivery agents for BNCT. In more detail, we expand upon our previous GLUT-targeting approach by synthesizing and evaluating the potential embedded in a representative set of fluorinated carbohydrates bearing a boron cluster. Our findings indicate that these species may have advantages over the boron delivery agents in current clinical use, e.g., significantly improved boron delivery capacity at the cellular level. Simultaneously, the carbohydrate delivery agents were found to bind strongly to plasma proteins, which may be a concern requiring further action before progression to in vivo studies. Altogether, this work brings new insights into factors which need to be accounted for if attempting to develop theranostic agents for BNCT based on carbohydrates in the future.
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http://dx.doi.org/10.3390/molecules29174263 | DOI Listing |
AAPS PharmSciTech
January 2025
Department of Pharmaceutics, School of Pharmaceutical Science, Siksha 'O' Anusandhan University, Bhubaneswar, 751003, Odisha, India.
Transdermal drug delivery (TDD) represents a transformative paradigm in drug administration, offering advantages such as controlled drug release, enhanced patient adherence, and circumvention of hepatic first-pass metabolism. Despite these benefits, the inherent barrier function of the skin, primarily attributed to the stratum corneum, remains a significant impediment to the efficient permeation of therapeutic agents. Recent advancements have focused on macromolecular-assisted permeation enhancers, including carbohydrates, lipids, amino acids, nucleic acids, and cell-penetrating peptides, which modulate skin permeability by transiently altering its structural integrity.
View Article and Find Full Text PDFMed Oncol
January 2025
Department of Research Outreach, Rubber Research Institute of Nigeria, PMB 1049, Benin City, Edo State, Nigeria.
Platinum nanoparticles (PtNPs) offer significant promise in cancer therapy by enhancing the therapeutic effects of platinum-based chemotherapies like cisplatin. These nanoparticles improve tumor targeting, reduce off-target effects, and help overcome drug resistance. PtNPs exert their anti-cancer effects primarily through the generation of reactive oxygen species (ROS), which induce oxidative stress and apoptosis in cancer cells.
View Article and Find Full Text PDFInt J Pharm
January 2025
Centre for Transgenic Plant Development, Department of Biotechnology, School of Chemical and Life Sciences, Jamia Hamdard, New Delhi 110062, India. Electronic address:
Malaria remains the fifth deadliest parasitic infection worldwide, despite significant advancements in technology. A major challenge in combating this disease lies in the growing resistance of malaria parasites to antimalarial drugs and insect vectors to insecticides. The emerging inefficacy of artemisinin-based combination therapies (ACTs) further exacerbates the issue.
View Article and Find Full Text PDFEur J Med Chem
December 2024
Department of Oral and Maxillofacial-Head and Neck Oncology, Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine, College of Stomatology, Shanghai Jiao Tong University, National Center for Stomatology, National Clinical Research Center for Oral Diseases, Shanghai Key Laboratory of Stomatology, Shanghai Research Institute of Stomatology, Shanghai, 200011, China; Digital Diagnosis and Treatment Innovation Center for Cancer, Institute of Translational Medicine, Shanghai Jiao Tong University, Shanghai, 200240, China. Electronic address:
Head and neck squamous cell carcinoma (HNSCC) is one of the most common malignant tumors, but clinical drug treatments are limited. The natural product diphyllin was identified as a lead compound suppressing the proliferation of HNSCC cells through phenotypic screening of natural product library. However, further developments of diphyllin as an anti-HNSCC agent were restricted by the weak bioactivity and poor metabolic stability.
View Article and Find Full Text PDFBioorg Chem
January 2025
Department of Chemistry, Indian Institute of Technology Indore, Indore 453552 India; Department of Biosciences and Biomedical Engineering, Indian Institute of Technology Indore, Indore 453552 India. Electronic address:
Prostate cancer (PCa) has emerged to be the second leading cause of cancer-related deaths in men. Molecular imaging of PCa using targeted radiopharmaceuticals specifically to PCa cells promises accurate staging of primary disease, detection of localized and metastasized tumours, and helps predict the progression of the disease. Glutamate urea heterodimers have been popularly used as high-affinity small molecules in the binding pockets of popular and well-characterized PCa biomarker, prostate specific membrane antigen (PSMA).
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