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Articles 1 - 4 of 4
Full-Text Articles in Social and Behavioral Sciences
Anti-Cancer Activity Of An Acid-Labile N-Alkylisatin Conjugate Targeting The Transferrin Receptor, Vineesh Indira Chandran, Lidia Matesic, Julie Locke, Danielle Skropeta, Marie Ranson, Kara Vine
Anti-Cancer Activity Of An Acid-Labile N-Alkylisatin Conjugate Targeting The Transferrin Receptor, Vineesh Indira Chandran, Lidia Matesic, Julie Locke, Danielle Skropeta, Marie Ranson, Kara Vine
Danielle Skropeta
We have previously reported a series of pH-sensitive imine-linked N-alkylisatin prodrugs that are stable at pH 7.4, but readily cleaved at pH 4.5. Herein, one of the most potent prodrugs, 5,7-dibromo-N-(pmethoxybenzyl) isatin (NAI), was functionalized with a para-phenylpropionic acid linker, and the resulting NAI–imine prodrug conjugated to transferrin (Tf) to form a NAI–imine–Tf conjugate. Cytotoxicity assays revealed the conjugate was equipotent to the free drug against MCF-7 breast cancer cells, with clear selectivity patterns based on TfR levels. These results suggest that this novel isatin-based cytotoxin conjugated to a tumor targeting protein via an acid-labile linker warrants further preclinical testing.
The Effect Of Individual N-Glycans On Enzyme Activity, Danielle Skropeta
The Effect Of Individual N-Glycans On Enzyme Activity, Danielle Skropeta
Danielle Skropeta
No abstract provided.
Synthesis And Anti-Leukaemic Activity Of Pyrrolo[3,2,1-Hi]Indole-1,2- Diones, Pyrrolo[3,2,1-Ij]Quinoline-1,2-Diones And Other Polycyclic Isatin Derivatives, Lidia Matesic, Julie M. Locke, Kara Vine, Marie Ranson, John B. Bremner, Danielle Skropeta
Synthesis And Anti-Leukaemic Activity Of Pyrrolo[3,2,1-Hi]Indole-1,2- Diones, Pyrrolo[3,2,1-Ij]Quinoline-1,2-Diones And Other Polycyclic Isatin Derivatives, Lidia Matesic, Julie M. Locke, Kara Vine, Marie Ranson, John B. Bremner, Danielle Skropeta
Danielle Skropeta
To further expand the structure–cytotoxic activity relationships of isatin derivatives and to reduce flexibility in substituent groups at nitrogen, 20 analogues incorporating a ring system between the N1 and C7 atoms of isatin were prepared using a variety of synthetic strategies. This yielded pyrroloindole-, pyrroloquinoline-, pyrroloacridine-, pyrrolophenanthridine- and benzopyrrolophenanthridine-based systems with embedded isatin moieties, the latter possessing a novel carbon skeleton. These compounds were subsequently assessed for their in vitro cytotoxicity against human U937 lymphoma cells, with the brominated pyrroloacridine dione 27 showing the most promising activity (IC50 3.01 μM) after 24 h.
C-Amp Dependent Protein Kinase A Inhibitory Activity Of Six Algal Extracts From South Eastern Australia And Their Fatty Acid Composition, Ana Zivanovic, Danielle Skropeta
C-Amp Dependent Protein Kinase A Inhibitory Activity Of Six Algal Extracts From South Eastern Australia And Their Fatty Acid Composition, Ana Zivanovic, Danielle Skropeta
Danielle Skropeta
c-AMP dependent protein kinase (protein kinase A, PKA) is an important enzyme involved in the regulation of an increasing number of physiological processes including immune function, cardiovascular disease, memory disorders and cancer. The objective of this study was to evaluate the PKA inhibitory activity of a range of algal extracts, along with their fatty acid composition. Six algal species were investigated including two Chlorophyta (Codium dimorphum and Ulva lactuca), two Phaeophyta (Phyllospora comosa and Sargassum sp.) and two Rhodophyta (Prionitis linearis and Corallina vancouveriensis), with the order of PKA inhibitory activity of their extracts identified as follows: brown seaweeds > red …