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Social and Behavioral Sciences Commons™
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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.
Metabolic Parameters And Emotionality Are Little Affected In G-Protein Coupled Receptor 12 (Gpr12) Mutant Mice, Elisabeth Frank, Yizhen Wu, Naomi Piyaratna, William James Body, P Snikeris, Timothy South, Anna-Karin Gerdin, Mikael Bjursell, Mohammad Bohlooly-Y, Leonard H. Storlien, Xu-Feng Huang
Metabolic Parameters And Emotionality Are Little Affected In G-Protein Coupled Receptor 12 (Gpr12) Mutant Mice, Elisabeth Frank, Yizhen Wu, Naomi Piyaratna, William James Body, P Snikeris, Timothy South, Anna-Karin Gerdin, Mikael Bjursell, Mohammad Bohlooly-Y, Leonard H. Storlien, Xu-Feng Huang
Xu-Feng Huang
Background: G-protein coupled receptors (GPR) bear the potential to serve as yet unidentified drug targets for psychiatric and metabolic disorders. GPR12 is of major interest given its putative role in metabolic function and its unique brain distribution, which suggests a role in emotionality and affect. We tested Gpr12 deficient mice in a series of metabolic and behavioural tests and subjected them to a well-established high-fat diet feeding protocol. Methodology/Principal Findings: Comparing the mutant mice with wild type littermates, no significant differences were seen in body weight, fatness or weight gain induced by a high-fat diet. The Gpr12 mutant mice displayed …