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Full-Text Articles in Medicine and Health Sciences
Ubiquitin Receptor Rpn13 Mediates The Inhibitory Interaction Of Diphenyldihaloketones Clefma And Ef24 With The 26s Proteasome, Geeta Rao, Gregory Nkepang, Jian Xu, Hooman Yari, Hailey Houson, Chengwen Teng Pharm.D., Ph.D., Vibhudutta Awasthi
Ubiquitin Receptor Rpn13 Mediates The Inhibitory Interaction Of Diphenyldihaloketones Clefma And Ef24 With The 26s Proteasome, Geeta Rao, Gregory Nkepang, Jian Xu, Hooman Yari, Hailey Houson, Chengwen Teng Pharm.D., Ph.D., Vibhudutta Awasthi
Faculty Publications
The proteasome is a validated target in drug discovery for diseases associated with unusual proteasomal activity. Here we report that two diphenyldihaloketones, CLEFMA and EF24, inhibit the peptidase activity of the 26S proteasome. The objective of this study was to investigate interaction of these compounds with the proteasome and identify a putative target within the protein components of the 26S proteasome. We employed standard fluorogenic peptide-based proteasome activity assay for trypsin-like, chymotrypsin-like, and caspase-like activities of human purified 26S proteasome in cell-free conditions. GFPu-1 and HUVEC cells were used as proteasome reporter cells. Direct binding studies used purified 19S, 20S, …
Investigating The Synergistic Effects Of Two Curcuminoids And Cisplatin On Cancer Cell Migration, Blaine Patty
Investigating The Synergistic Effects Of Two Curcuminoids And Cisplatin On Cancer Cell Migration, Blaine Patty
Mahurin Honors College Capstone Experience/Thesis Projects
Cisplatin is a common chemotherapy drug used to treat various cancers; however, it is relatively ineffective against many cancers, including several types of lung cancer. One approach that could improve cisplatin’s effect is to combine it with another drug that produces a synergistic response greater than either drug alone. Curcumin, a naturally occurring plant compound, has been investigated for synergisms in conjunction with cisplatin chemotherapy, but curcumin use is hampered by its low bioavailability. This project investigated whether two synthetic curcumin analogs, EF-24 and CLEFMA (curcuminoids), which have greater solubility than curcumin, could, when combined with cisplatin, decrease the migration …
Investigating The Synergistic Effects Of Two Curcuminoids And Cisplatin On Cancer Cell Reactive Oxygen Species, Matthew Millay
Investigating The Synergistic Effects Of Two Curcuminoids And Cisplatin On Cancer Cell Reactive Oxygen Species, Matthew Millay
Mahurin Honors College Capstone Experience/Thesis Projects
Cisplatin is an anticancer drug which can cause the production of reactive oxygen species (ROS) that kill cancer cells. Curcumin is a naturally occurring plant compound that can increase ROS levels in cancer cells and enhance the activity of cisplatin against cancer, but it exhibits poor bioavailability. We investigated whether two synthetic curcumin analogs (curcuminoids), EF-24 and CLEFMA, with anti-cancer activity and improved bioavailability, increased cisplatin’s effect against cancer. A spectrophotometric fluorescent ROS assay was used to determine if cisplatin, the curcuminoids or combinations of cisplatin with a curcuminoid affected the level of ROS in the A549 non-small cell lung …