Microbial resistance to antibiotics is an urgent and worldwide concern. Several pyrazole-derived hydrazones were synthesized by using benign reaction conditions. Several of these molecules are potent growth inhibitors of drug-resistant strains of and with minimum inhibitory concentration values as low as 0.39 μg/mL. Furthermore, these molecules are nontoxic to human cells at high concentrations. Some of these molecules were tested for their ability to disrupt the bacterial membrane by using the SYTO-9/propidium iodide (BacLight) assay.
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http://dx.doi.org/10.1021/acsomega.9b01967 | DOI Listing |
In Vivo
December 2024
Immunotherapy Division, Shizuoka Cancer Center Research Institute, Shizuoka, Japan;
Background/aim: Immune checkpoint blockade has achieved great success as a targeted immunotherapy for solid cancers. However, small molecules that inhibit programmed death 1/programmed death ligand 1 (PD-1/PD-L1) binding are still being developed and have several advantages, such as high bioavailability. Previously, we reported a novel PD-1/PD-L1-inhibiting small compound, SCL-1, which showed potent antitumor effects on PD-L1 tumors.
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December 2024
Graduate Program for Bio-health/Innovative Drug Development using Subtropical Bio-Resources, Jeju National University, Jeju, Republic of Korea;
Background/aim: Breast cancer stem cells (BCSCs) are a subpopulation of tumor cells that play a role in therapeutic resistance. In this study, we demonstrated that sertaconazole, an antifungal agent, displayed a potent inhibition on cancer stem cells (CSCs) and investigated the mechanism of action involved in its anti-BCSC effect.
Materials And Methods: The effect of sertaconazole on BCSCs was investigated using a mammosphere formation assay, a colony formation assay, and a cell migration assay.
Anticancer Res
January 2025
Eisai Inc., Cambridge, MA, U.S.A.
Background/aim: Preclinical studies were undertaken to investigate whether eribulin's known cytotoxic antimitotic effects are characterized by immunogenic cell death (ICD) as assessed by three established ICD biomarkers: extracellular released ATP, released HMGB1 and cell surface calreticulin.
Materials And Methods: Using BT-549, Hs578T and MCF-7 breast cancer cell lines, antiproliferative IC's of eribulin, five other microtubule targeting agents (MTAs; ER-076349, vinblastine, vinorelbine, paclitaxel, docetaxel) and three DNA damaging agents (DDAs; doxorubicin, cisplatin, oxaliplatin) were determined.
Results: Treatment of cells with 10×IC concentrations of all drugs in serum-free media resulted in time-dependent induction of cytotoxicity over DMSO controls.
J Chem Inf Model
December 2024
School of Pharmacy, College of Medicine, National Taiwan University, Taipei 10051, Taiwan.
Pulmonary fibrosis is excessive scarring of the lung tissues. Transforming growth factor-beta (TGF-β) has been implicated in pulmonary fibrosis due to its ability to induce the epithelial-to-mesenchymal transition (EMT) and promote epithelial cell migration. Cyclin-dependent kinase 8 (CDK8) can mediate the TGF-β signaling pathways and could function as an alternative therapeutic target for treating pulmonary fibrosis.
View Article and Find Full Text PDFPLoS One
December 2024
Institute of Cell Biology, University of Bern, Bern, Switzerland.
Malaria caused by Plasmodium parasites remains a large health burden. One approach to combat this disease involves vaccinating individuals with whole sporozoites that have been genetically modified to arrest their development at a specific stage in the liver by targeted gene deletion, resulting in a genetically attenuated parasite (GAP). Through a comprehensive phenotyping screen, we identified the hscb gene, encoding a putative iron-sulfur protein assembly chaperone, as crucial for liver stage development, making it a suitable candidate gene for GAP generation.
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