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Full-Text Articles in Physical Sciences and Mathematics
Allosteric Regulation Of Caspase-6 Proteolytic Activity, Elih M. Velazquez-Delgado
Allosteric Regulation Of Caspase-6 Proteolytic Activity, Elih M. Velazquez-Delgado
Open Access Dissertations
Caspases are cysteine proteases best known for their controlling roles in apoptosis and inflammation. Caspase-6 has recently been shown to play a key role in the cleavage of neurodegenerative substrates that causes Huntington and Alzheimer's Disease, heightening interest in caspase-6 and making it a drug target. All thirteen human caspases have related specificities for binding and cleaving substrate, so achieving caspase-specific regulation at the active site has been extremely challenging if not impossible. We have determined the structures of four unliganded forms of caspase-6, which attain a novel helical structure not observed in any other caspases. In this conformation, rotation …
Detection Of Folate Receptor From Fr+ Cells, Gopikrishna Pinnaka
Detection Of Folate Receptor From Fr+ Cells, Gopikrishna Pinnaka
All Capstone Projects
Targeted drug delivery is a newer and less explored arena that has potential scope in tumor targeting because the regular chemotherapy has lethal effects on the normal cells also. Our present Work was an attempt to specifically target receptors on cancerous cells, especially the Folate Receptor (FR). Folate is important for cells for DNA synthesis and the tissues that rapidly divide require folate, cancer cells are no exceptions for this. To cope with the increased demand for the folate the cancer cells express greater FR on the cell surface. This very fact was our basis for the construction of our …
Design, Synthesis, And Biological Evaluation Of Novel Polyamine Transport System Probes And Their Application To Human Cancers, Aaron Muth
Electronic Theses and Dissertations
The mammalian polyamine transport system (PTS) has been of interest due to its roles in cancer and maintaining cellular homeostasis. Polyamines are essential growth factors which are tightly controlled via a balance of biosynthesis, metabolism, import, and export. This work focused on the development and biological testing of polyamine transport probes to help understand the molecular requirements of the PTS. This was mediated through the use of a CHO (PTS active) and CHO-MG* (PTS deficient) screen, where compounds demonstrating high toxicity in CHO and low toxicity in CHO-MG* were considered PTS selective. The first chapter focused on the development of …