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Full-Text Articles in Medicine and Health Sciences
Targeting Urokinase And The Transferrin Receptor With Novel, Anti-Mitotic N-Alkylisatin Cytotoxin Conjugates Causes Selective Cancer Cell Death And Reduces Tumor Growth, K Vine, V. Indira Chandran, J Locke, L Matesic, J Lee, D Skropeta, J Bremner, M Ranson
Targeting Urokinase And The Transferrin Receptor With Novel, Anti-Mitotic N-Alkylisatin Cytotoxin Conjugates Causes Selective Cancer Cell Death And Reduces Tumor Growth, K Vine, V. Indira Chandran, J Locke, L Matesic, J Lee, D Skropeta, J Bremner, M Ranson
Danielle Skropeta
Tumor-specific delivery of ligand-directed prodrugs can increase the therapeutic window of chemotherapeutics by maintaining efficacy whilst decreasing toxic side effects. We have previously described a series of synthetic N-alkylated isatin cytotoxins that destabilize microtubules and induce apoptosis with 10-fold greater potency than conventional anti-mitotics in vitro. Here, we report the characterization, in vitro cytotoxicity and in vivo efficacy of a lead compound, 5,7-dibromo-N-(p-hydroxymethylbenzyl)isatin (N-AI) conjugated via an esterase-labile linker (N-AIE) to two proven targeting ligands, transferrin (Tf) and plasminogen activator inhibitor type 2 (PAI-2/serpinB2). N-AI was released from N-AIE and the targeting ligands Tf/PAI-2 in an esterase-dependent manner at 37 …
Comparison Of Polar Metabolites In Australian Deep-Sea Sponges Using Hplc-Esi-Hrms In Combination With Multivariate Analysis, L Wei, D Skropeta
Comparison Of Polar Metabolites In Australian Deep-Sea Sponges Using Hplc-Esi-Hrms In Combination With Multivariate Analysis, L Wei, D Skropeta
Danielle Skropeta
Abstract of paper that presented at 8th Joint Meeting of AFERP, ASP, GA, PSE and SIF, New York City, July 28 - August 1, 2012.
Selective Release Of Potent N-Alkylisatin Based Cytotoxins Via Hydrolysis Of Ph Sensitive Imine Linkers, D Skropeta, L Matesic, J Locke, K Vine, M Ranson, J Bremner
Selective Release Of Potent N-Alkylisatin Based Cytotoxins Via Hydrolysis Of Ph Sensitive Imine Linkers, D Skropeta, L Matesic, J Locke, K Vine, M Ranson, J Bremner
Danielle Skropeta
No abstract provided.