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Drug Development Breakthroughs: From Novel Antimicrobials to Targeted Cancer Drugs

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: 30 January 2026 | Viewed by 1107

Special Issue Editor

Special Issue Information

Dear Colleagues,

Transforming a potential drug from an idea to a marketable product on pharmacy shelves is a long, time-consuming, and expensive process. Recent advances in drug discovery and development, particularly with the integration of artificial intelligence, aim to make this process easier, faster, and safer. This Special Issue seeks to showcase the latest advancements in drug discovery and development, with a focus on molecular science. We welcome contributions that highlight, but are not limited to, novel small-molecule inhibitors, biopharmaceuticals, peptides, phytochemicals, and new antimicrobial compounds, alongside research on novel therapies for the treatment of cancer and cardiovascular and autoimmune diseases, among others. Submissions that combine clinical insights with molecular science approaches are especially encouraged, as they provide a deeper understanding of the mechanisms of action and biomolecular basis of drug effects. Pure clinical studies will not be suitable, although we are interested in research which bridges clinical applications with biomolecular findings. We invite comprehensive reviews or original research articles that explore innovative strategies in drug development, elucidating molecular pathways and their therapeutic potential.

Dr. Christos Papaneophytou
Guest Editor

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Keywords

  • drug development
  • molecular science
  • small-molecule inhibitors
  • biopharmaceuticals
  • peptides
  • cancer therapy

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Published Papers (1 paper)

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Research

26 pages, 3114 KB  
Article
Targeting G6PD with Benzimidazole and Thiazole Derivatives Suppresses SIRT 2 and VEGF Expression and Induces Cytotoxicity in Glioma Cells
by Montserrat Vázquez-Bautista, Laura Morales-Luna, Verónica Pérez de la Cruz, Rosa Angélica Castillo-Rodríguez, José Antonio Velázquez-Aragón, Sergio Enríquez-Flores, Luis Antonio Flores-López, Elizabeth Hernández-Urzúa, Víctor Martínez-Rosas, Carlos Wong-Baeza, Isabel Baeza-Ramírez, Gabriel Navarrete-Vázquez, Benjamin Pineda, Beatriz Hernández-Ochoa and Saúl Gómez-Manzo
Int. J. Mol. Sci. 2025, 26(18), 9092; https://doi.org/10.3390/ijms26189092 - 18 Sep 2025
Viewed by 263
Abstract
Hypoxia and activation of the pentose phosphate pathway (PPP), as well as overexpression of glucose-6-phosphate dehydrogenase (G6PD), are hallmark features of glioblastomas (GBM), contributing significantly to tumor progression metabolic adaptation and drug resistance. This study aimed to evaluate the cytotoxic effects of nine [...] Read more.
Hypoxia and activation of the pentose phosphate pathway (PPP), as well as overexpression of glucose-6-phosphate dehydrogenase (G6PD), are hallmark features of glioblastomas (GBM), contributing significantly to tumor progression metabolic adaptation and drug resistance. This study aimed to evaluate the cytotoxic effects of nine synthetic compounds incorporating annulated benzimidazole and nitrothiazole scaffolds in two glioblastoma cell lines (A172 and U87-MG) under both normoxic and hypoxic conditions. Three compounds (BZM-7, BZM-9, and CNZ-3) demonstrated potent anticancer activity, with CNZ-3 exhibiting the highest efficacy, particularly in hypoxia. The study further investigated the effects of these compounds on the expression of the G6PD gene, as well as post-translational regulatory genes SIRT2 and KAT9, and the angiogenesis-related VEGF gene. Transcriptional analyses showed that the nitrothiazole-derived compound CNZ-3 significantly downregulated G6PD, SIRT2, KAT9 and VEGF expression under hypoxic conditions, suggesting selective interference with hypoxia-adaptative pathways. In contrast, BZM-7 and BZM-9 showed distinct expression patterns, indicating diverse mechanisms of action despite structural similarity. In addition, BZM-7, BZM-9, and CNZ-3 were identified as potent inhibitors of recombinant G6PD, demonstrating both enzymatic inhibition and structural alterations, suggesting that G6PD could be a relevant therapeutic target for these compounds. Furthermore, molecular docking analysis revealed favorable binding interactions between the compounds and key amino acids of the G6PD, reinforcing their potential as a direct enzyme inhibitors. These findings highlight the pivotal role of G6PD in gliomas under hypoxic conditions and support its inhibition as a promising therapeutic strategy. Full article
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