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Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
GlcNAc Conjugated Atorvastatin with Enhanced Water Solubility and Cellular Internalization.
Bioconjugate Chemistry 2017 August 17
Targeting ligands facilitate cell specific drug delivery and improve pharmaceutical properties. Herein, we designed two ligand drug conjugates by conjugating GlcNAc (N-acetylglucosamine) with atorvastatin. These two conjugates, termed G-AT and G-K-AT, exhibited enhanced water solubility and cellular uptake. Moreover, both G-AT and G-K-AT were able to release atorvastatin and consequently achieve significant inhibition against 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase.
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