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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.
G-Protein-Coupled Receptor Kinase 4 Polymorphisms Predict Blood Pressure Response To Dietary Modification In Black Patients With Mild-To-Moderate Hypertension, B Rayner, R Ramesar, K Steyn, N Levitt, C Lombard, K Charlton
G-Protein-Coupled Receptor Kinase 4 Polymorphisms Predict Blood Pressure Response To Dietary Modification In Black Patients With Mild-To-Moderate Hypertension, B Rayner, R Ramesar, K Steyn, N Levitt, C Lombard, K Charlton
Karen E. Charlton
No abstract provided.