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Differential regulation of BAX and BAK apoptotic activity revealed by small molecules.
Sci Adv
March 2025
Walter and Eliza Hall Institute of Medical Research, Parkville, Victoria, Australia.
Defective apoptosis mediated by B cell lymphoma 2 antagonist/killer (BAK) or B cell lymphoma 2-associated X protein (BAX) underlies various pathologies including autoimmune and degenerative conditions. On mitochondria, voltage-dependent anion channel 2 (VDAC2) interacts with BAK and BAX through a common interface to inhibit BAK or to facilitate BAX apoptotic activity. We identified a small molecule (WEHI-3773) that inhibits interaction between VDAC2 and BAK or BAX revealing contrasting effects on their apoptotic activity.
View Article and Find Full Text PDFSrc inhibition potentiates MCL-1 antagonist activity in acute myeloid leukemia.
Signal Transduct Target Ther
February 2025
Division of Hematology/Oncology, Department of Internal Medicine, Virginia Commonwealth University, Richmond, VA, USA.
The importance of MCL-1 in leukemogenesis has prompted development of MCL-1 antagonists e.g., S63845, MIK665.
View Article and Find Full Text PDFCurcumin chemo-sensitizes intrinsic apoptosis through ROS-mediated mitochondrial hyperpolarization and DNA damage in breast cancer cells.
Cell Signal
April 2025
Vice Chancellor, Era University, Lucknow 226003, Uttar Pradesh, India.
Background: Curcumin (CUR), a polyphenol phyto-compound extracted from turmeric rhizome (Curcuma longa), suppresses cancer by inducing apoptosis while also limiting cell survival and proliferation. This in vitro and in silico research work focuses on the synergistic sensitization of Doxorubicin (DOXO) on regulating ROS-mediated apoptosis of the breast cancer cells (MDA-MB-231 and MCF-7) in DOXO-CUR co-treatment. We observed dose-dependent cytotoxicity, increased ROS production, and mtDNA fragmentation by reduced membrane potential.
View Article and Find Full Text PDFCompared Inhibitory Activities of Tamoxifen and Avenanthramide B on Liver Esterase and Correlation Based on the Superimposed Structure Between Porcine and Human Liver Esterase.
Int J Mol Sci
December 2024
Department of Biological Science, Sungkyunkwan University, Suwon 16419, Republic of Korea.
Exposure to tamoxifen can exert effects on the human liver, and esterases process prodrugs such as antibiotics and convert them to less toxic metabolites. In this study, the porcine liver esterase (PLE)-inhibitory activity of tamoxifen has been investigated. PLE showed inhibition of a PLE isoenzyme (PLE5).
View Article and Find Full Text PDFEffect of Antimicrobial Wipes on Hospital-Associated Bacterial and Fungal Strains.
Infect Chemother
December 2024
Vaccine Bio Research Institute, College of Medicine, The Catholic University of Korea Seoul, Korea.
Background: Healthcare-associated infections (HAI) caused by multidrug-resistant organisms have emerged as a significant global issue, posing substantial challenges to healthcare systems. Low- and intermediate-level disinfectants are extensively utilized for cleaning and disinfecting surfaces in hospitals to mitigate environmental transmission of HAI. Therefore, the need for more effective and environmentally safe disinfectants is increasing.
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